Axitinib
别名: AG 013736 中文名称：阿西替尼,阿昔替尼
Axitinib是一种多靶点抑制剂，作用于 VEGFR1，VEGFR2，VEGFR3，PDGFRβ和c-Kit，在猪主动脉内皮细胞中IC50分别为0.1 nM，0.2 nM，0.1-0.3 nM，1.6 nM和1.7 nM。
Axitinib Chemical Structure
CAS: 319460-85-0
客户使用Selleck的Axitinib发表文献171篇
产品质控
批次：
纯度：
99.96%
99.96
Axitinib相关产品
| 相关靶点 | VEGFR1 VEGFR2 VEGFR3 | 点击展开 |
|---|---|---|
| 相关化合物库 | 激酶抑制剂库 酪氨酸激酶抑制剂分子库 PI3K/Akt 抑制剂库 细胞周期化合物库 血管生成相关化合物库 | 点击展开 |
相关信号通路图
VEGFR抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| MCF7 | Antiproliferative assay | 5 days | Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 0.97 μM. | 23829549 | |
| MDA-MB-468 | Antiproliferative assay | 5 days | Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 1.3 μM. | 23829549 | |
| HCC1954 | Antiproliferative assay | 5 days | Antiproliferative activity against human HCC1954 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 2.7 μM. | 23829549 | |
| SKBR3 | Antiproliferative assay | 5 days | Antiproliferative activity against human SKBR3 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 3.8 μM. | 23829549 | |
| MDA-MB-231 | Antiproliferative assay | 5 days | Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 7.3 μM. | 23829549 | |
| MCF7 | Cytotoxicity assay | 5 days | Cytotoxicity against human MCF7 cells after 5 days by SRB assay, GI50 = 2.3 μM. | 24867403 | |
| MDA-MB-468 | Cytotoxicity assay | 5 days | Cytotoxicity against human MDA-MB-468 cells after 5 days by SRB assay, GI50 = 2.8 μM. | 24867403 | |
| SKBR3 | Cytotoxicity assay | 5 days | Cytotoxicity against human SKBR3 cells after 5 days by SRB assay, GI50 = 4.6 μM. | 24867403 | |
| MDA-MB-231 | Cytotoxicity assay | 5 days | Cytotoxicity against human MDA-MB-231 cells after 5 days by SRB assay, GI50 = 11 μM. | 24867403 | |
| HUVEC | Antiproliferative assay | 1 hr | Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as reduction in cell viability preincubated for 1 hr followed by addition of VEGF measured after 72 hrs by MTT assay, IC50 = 0.0005 μM. | ChEMBL | |
| HUVEC | Antiproliferative assay | 1 hr | Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as reduction in cell viability preincubated for 1 hr followed by addition of VEGF measured after 72 hrs in presence of albumin by MTT assay, IC50 = 0.0027 μM. | ChEMBL | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against VEGF-stimulated human A549 cells after 48 hrs by CCK8 assay, IC50 = 22.4 μM. | ChEMBL | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against VEGF-stimulated human HepG2 cells after 48 hrs by CCK8 assay, IC50 = 38.7 μM. | ChEMBL | |
| HEC-1 | Growth Inhibition Assay | IC50=8.78439 μM | SANGER | ||
| 8505C | Growth Inhibition Assay | IC50=8.64824 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=8.51534 μM | SANGER | ||
| TE-1 | Growth Inhibition Assay | IC50=8.44316 μM | SANGER | ||
| D-423MG | Growth Inhibition Assay | IC50=8.2172 μM | SANGER | ||
| NCI-H2228 | Growth Inhibition Assay | IC50=8.15783 μM | SANGER | ||
| COLO-800 | Growth Inhibition Assay | IC50=7.94492 μM | SANGER | ||
| MDA-MB-415 | Growth Inhibition Assay | IC50=7.89186 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=7.6961 μM | SANGER | ||
| IA-LM | Growth Inhibition Assay | IC50=7.68613 μM | SANGER | ||
| SW1088 | Growth Inhibition Assay | IC50=7.65826 μM | SANGER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=7.64934 μM | SANGER | ||
| SK-N-FI | Growth Inhibition Assay | IC50=7.63033 μM | SANGER | ||
| HCC2998 | Growth Inhibition Assay | IC50=7.60743 μM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=7.60644 μM | SANGER | ||
| HCC1419 | Growth Inhibition Assay | IC50=7.53 μM | SANGER | ||
| SK-PN-DW | Growth Inhibition Assay | IC50=7.4815 μM | SANGER | ||
| IGROV-1 | Growth Inhibition Assay | IC50=7.32386 μM | SANGER | ||
| KP-N-YS | Growth Inhibition Assay | IC50=7.2072 μM | SANGER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=7.19345 μM | SANGER | ||
| SNU-449 | Growth Inhibition Assay | IC50=7.01072 μM | SANGER | ||
| OC-314 | Growth Inhibition Assay | IC50=6.91159 μM | SANGER | ||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=6.54572 μM | SANGER | ||
| HCC1569 | Growth Inhibition Assay | IC50=6.53737 μM | SANGER | ||
| S-117 | Growth Inhibition Assay | IC50=6.50267 μM | SANGER | ||
| HUTU-80 | Growth Inhibition Assay | IC50=6.41688 μM | SANGER | ||
| D-502MG | Growth Inhibition Assay | IC50=6.28857 μM | SANGER | ||
| MKN45 | Growth Inhibition Assay | IC50=6.26016 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=6.11248 μM | SANGER | ||
| NCI-H1048 | Growth Inhibition Assay | IC50=6.10599 μM | SANGER | ||
| A704 | Growth Inhibition Assay | IC50=6.10574 μM | SANGER | ||
| OAW-42 | Growth Inhibition Assay | IC50=5.98821 μM | SANGER | ||
| NCI-H82 | Growth Inhibition Assay | IC50=5.92771 μM | SANGER | ||
| KM-H2 | Growth Inhibition Assay | IC50=5.92395 μM | SANGER | ||
| COLO-829 | Growth Inhibition Assay | IC50=5.91504 μM | SANGER | ||
| NCI-H28 | Growth Inhibition Assay | IC50=5.87918 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=5.84325 μM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=5.75583 μM | SANGER | ||
| JVM-3 | Growth Inhibition Assay | IC50=5.72325 μM | SANGER | ||
| D-392MG | Growth Inhibition Assay | IC50=5.57849 μM | SANGER | ||
| EFM-19 | Growth Inhibition Assay | IC50=5.41737 μM | SANGER | ||
| NCI-H1155 | Growth Inhibition Assay | IC50=5.38185 μM | SANGER | ||
| KM12 | Growth Inhibition Assay | IC50=5.29827 μM | SANGER | ||
| NBsusSR | Growth Inhibition Assay | IC50=5.03514 μM | SANGER | ||
| CAS-1 | Growth Inhibition Assay | IC50=4.99908 μM | SANGER | ||
| A3-KAW | Growth Inhibition Assay | IC50=4.97352 μM | SANGER | ||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=4.89048 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=4.81418 μM | SANGER | ||
| HOS | Growth Inhibition Assay | IC50=4.6977 μM | SANGER | ||
| SNU-423 | Growth Inhibition Assay | IC50=4.6079 μM | SANGER | ||
| SW1573 | Growth Inhibition Assay | IC50=4.55163 μM | SANGER | ||
| EW-1 | Growth Inhibition Assay | IC50=4.53014 μM | SANGER | ||
| Hs-578-T | Growth Inhibition Assay | IC50=4.31468 μM | SANGER | ||
| HGC-27 | Growth Inhibition Assay | IC50=4.2966 μM | SANGER | ||
| 8-MG-BA | Growth Inhibition Assay | IC50=4.26658 μM | SANGER | ||
| CAL-27 | Growth Inhibition Assay | IC50=4.24344 μM | SANGER | ||
| ONS-76 | Growth Inhibition Assay | IC50=4.24192 μM | SANGER | ||
| LC-2-ad | Growth Inhibition Assay | IC50=4.22177 μM | SANGER | ||
| HCC1187 | Growth Inhibition Assay | IC50=4.21597 μM | SANGER | ||
| JEG-3 | Growth Inhibition Assay | IC50=4.15916 μM | SANGER | ||
| DU-145 | Growth Inhibition Assay | IC50=4.12825 μM | SANGER | ||
| HCC1395 | Growth Inhibition Assay | IC50=3.99484 μM | SANGER | ||
| NCI-H526 | Growth Inhibition Assay | IC50=3.99126 μM | SANGER | ||
| ABC-1 | Growth Inhibition Assay | IC50=3.93911 μM | SANGER | ||
| KMOE-2 | Growth Inhibition Assay | IC50=3.91808 μM | SANGER | ||
| ES1 | Growth Inhibition Assay | IC50=3.83094 μM | SANGER | ||
| COR-L105 | Growth Inhibition Assay | IC50=3.63334 μM | SANGER | ||
| EW-11 | Growth Inhibition Assay | IC50=3.63022 μM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=3.62616 μM | SANGER | ||
| SCC-4 | Growth Inhibition Assay | IC50=3.50396 μM | SANGER | ||
| ES8 | Growth Inhibition Assay | IC50=3.34999 μM | SANGER | ||
| SW982 | Growth Inhibition Assay | IC50=3.33875 μM | SANGER | ||
| SF126 | Growth Inhibition Assay | IC50=3.30017 μM | SANGER | ||
| HCC1806 | Growth Inhibition Assay | IC50=3.27657 μM | SANGER | ||
| NCI-H446 | Growth Inhibition Assay | IC50=3.22805 μM | SANGER | ||
| NCI-H1563 | Growth Inhibition Assay | IC50=3.15005 μM | SANGER | ||
| SF295 | Growth Inhibition Assay | IC50=3.02597 μM | SANGER | ||
| DMS-273 | Growth Inhibition Assay | IC50=2.90207 μM | SANGER | ||
| CHP-212 | Growth Inhibition Assay | IC50=2.82091 μM | SANGER | ||
| MHH-NB-11 | Growth Inhibition Assay | IC50=2.70299 μM | SANGER | ||
| DMS-114 | Growth Inhibition Assay | IC50=2.66345 μM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=2.59169 μM | SANGER | ||
| GOTO | Growth Inhibition Assay | IC50=2.53013 μM | SANGER | ||
| T-24 | Growth Inhibition Assay | IC50=2.48037 μM | SANGER | ||
| A4-Fuk | Growth Inhibition Assay | IC50=2.47168 μM | SANGER | ||
| HuH-7 | Growth Inhibition Assay | IC50=2.42165 μM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=2.28061 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=2.24957 μM | SANGER | ||
| ACN | Growth Inhibition Assay | IC50=2.23875 μM | SANGER | ||
| DK-MG | Growth Inhibition Assay | IC50=2.23834 μM | SANGER | ||
| YH-13 | Growth Inhibition Assay | IC50=2.21671 μM | SANGER | ||
| HCE-T | Growth Inhibition Assay | IC50=2.20598 μM | SANGER | ||
| A172 | Growth Inhibition Assay | IC50=2.13606 μM | SANGER | ||
| RT-112 | Growth Inhibition Assay | IC50=2.13424 μM | SANGER | ||
| GCT | Growth Inhibition Assay | IC50=2.00916 μM | SANGER | ||
| HSC-4 | Growth Inhibition Assay | IC50=1.93839 μM | SANGER | ||
| HD-MY-Z | Growth Inhibition Assay | IC50=1.86281 μM | SANGER | ||
| PA-1 | Growth Inhibition Assay | IC50=1.82725 μM | SANGER | ||
| UACC-257 | Growth Inhibition Assay | IC50=1.82163 μM | SANGER | ||
| ALL-PO | Growth Inhibition Assay | IC50=1.80015 μM | SANGER | ||
| HMV-II | Growth Inhibition Assay | IC50=1.70488 μM | SANGER | ||
| NCI-H292 | Growth Inhibition Assay | IC50=1.66383 μM | SANGER | ||
| SW780 | Growth Inhibition Assay | IC50=1.65158 μM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=1.60556 μM | SANGER | ||
| BT-549 | Growth Inhibition Assay | IC50=1.56909 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=1.43996 μM | SANGER | ||
| D-566MG | Growth Inhibition Assay | IC50=1.40683 μM | SANGER | ||
| NCI-H1581 | Growth Inhibition Assay | IC50=1.39042 μM | SANGER | ||
| NB10 | Growth Inhibition Assay | IC50=1.32557 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=1.25457 μM | SANGER | ||
| ES5 | Growth Inhibition Assay | IC50=1.17248 μM | SANGER | ||
| G-402 | Growth Inhibition Assay | IC50=1.14694 μM | SANGER | ||
| AGS | Growth Inhibition Assay | IC50=1.11395 μM | SANGER | ||
| ES7 | Growth Inhibition Assay | IC50=1.11334 μM | SANGER | ||
| A427 | Growth Inhibition Assay | IC50=1.10381 μM | SANGER | ||
| AN3-CA | Growth Inhibition Assay | IC50=1.08389 μM | SANGER | ||
| SK-OV-3 | Growth Inhibition Assay | IC50=1.06633 μM | SANGER | ||
| H4 | Growth Inhibition Assay | IC50=1.06422 μM | SANGER | ||
| NB14 | Growth Inhibition Assay | IC50=1.01801 μM | SANGER | ||
| A2780 | Growth Inhibition Assay | IC50=1.01146 μM | SANGER | ||
| SW756 | Growth Inhibition Assay | IC50=0.99846 μM | SANGER | ||
| NEC8 | Growth Inhibition Assay | IC50=0.72113 μM | SANGER | ||
| BE-13 | Growth Inhibition Assay | IC50=0.51008 μM | SANGER | ||
| MFM-223 | Growth Inhibition Assay | IC50=0.44776 μM | SANGER | ||
| MEG-01 | Growth Inhibition Assay | IC50=0.42361 μM | SANGER | ||
| K5 | Growth Inhibition Assay | IC50=0.42127 μM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=0.3932 μM | SANGER | ||
| KG-1 | Growth Inhibition Assay | IC50=0.37642 μM | SANGER | ||
| G-361 | Growth Inhibition Assay | IC50=0.32325 μM | SANGER | ||
| JAR | Growth Inhibition Assay | IC50=0.23989 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=0.17665 μM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=0.16816 μM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=0.16577 μM | SANGER | ||
| H-EMC-SS | Growth Inhibition Assay | IC50=0.11005 μM | SANGER | ||
| HOP-62 | Growth Inhibition Assay | IC50=0.10836 μM | SANGER | ||
| A204 | Growth Inhibition Assay | IC50=0.00992 μM | SANGER | ||
| CGTH-W-1 | Growth Inhibition Assay | IC50=0.00722 μM | SANGER | ||
| KASUMI-1 | Growth Inhibition Assay | IC50=0.00682 μM | SANGER | ||
| NCI-H1703 | Growth Inhibition Assay | IC50=0.000902 μM | SANGER | ||
| EoL-1-cell | Growth Inhibition Assay | IC50=0.0000513 μM | SANGER | ||
| TE-11 | Growth Inhibition Assay | IC50=8.99551 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=9.01433 μM | SANGER | ||
| TGBC11TKB | Growth Inhibition Assay | IC50=9.02241 μM | SANGER | ||
| NB17 | Growth Inhibition Assay | IC50=9.1887 μM | SANGER | ||
| Becker | Growth Inhibition Assay | IC50=9.41944 μM | SANGER | ||
| SN12C | Growth Inhibition Assay | IC50=9.45234 μM | SANGER | ||
| COLO-320-HSR | Growth Inhibition Assay | IC50=9.60237 μM | SANGER | ||
| D-283MED | Growth Inhibition Assay | IC50=9.63072 μM | SANGER | ||
| D-263MG | Growth Inhibition Assay | IC50=9.83384 μM | SANGER | ||
| MEL-JUSO | Growth Inhibition Assay | IC50=9.90127 μM | SANGER | ||
| T98G | Growth Inhibition Assay | IC50=9.90203 μM | SANGER | ||
| HLE | Growth Inhibition Assay | IC50=9.90909 μM | SANGER | ||
| Ca9-22 | Growth Inhibition Assay | IC50=10.0665 μM | SANGER | ||
| OS-RC-2 | Growth Inhibition Assay | IC50=10.1045 μM | SANGER | ||
| T47D | Growth Inhibition Assay | IC50=10.155 μM | SANGER | ||
| GI-1 | Growth Inhibition Assay | IC50=10.3533 μM | SANGER | ||
| NUGC-3 | Growth Inhibition Assay | IC50=10.4402 μM | SANGER | ||
| MDA-MB-361 | Growth Inhibition Assay | IC50=10.4432 μM | SANGER | ||
| SCC-15 | Growth Inhibition Assay | IC50=10.4718 μM | SANGER | ||
| KS-1 | Growth Inhibition Assay | IC50=10.6301 μM | SANGER | ||
| CAL-12T | Growth Inhibition Assay | IC50=10.6361 μM | SANGER | ||
| OVCAR-4 | Growth Inhibition Assay | IC50=10.7068 μM | SANGER | ||
| HuP-T4 | Growth Inhibition Assay | IC50=11.0328 μM | SANGER | ||
| NCI-H358 | Growth Inhibition Assay | IC50=11.2657 μM | SANGER | ||
| HO-1-N-1 | Growth Inhibition Assay | IC50=11.3398 μM | SANGER | ||
| NH-12 | Growth Inhibition Assay | IC50=11.5378 μM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=11.5985 μM | SANGER | ||
| K-562 | Growth Inhibition Assay | IC50=11.7248 μM | SANGER | ||
| ES6 | Growth Inhibition Assay | IC50=11.8581 μM | SANGER | ||
| RO82-W-1 | Growth Inhibition Assay | IC50=11.9064 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=11.932 μM | SANGER | ||
| 23132-87 | Growth Inhibition Assay | IC50=12.0821 μM | SANGER | ||
| A549 | Growth Inhibition Assay | IC50=12.3285 μM | SANGER | ||
| NCI-H23 | Growth Inhibition Assay | IC50=12.5026 μM | SANGER | ||
| H9 | Growth Inhibition Assay | IC50=12.5577 μM | SANGER | ||
| LB771-HNC | Growth Inhibition Assay | IC50=12.765 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=12.8258 μM | SANGER | ||
| HSC-3 | Growth Inhibition Assay | IC50=12.9276 μM | SANGER | ||
| PFSK-1 | Growth Inhibition Assay | IC50=12.9507 μM | SANGER | ||
| ETK-1 | Growth Inhibition Assay | IC50=13.0779 μM | SANGER | ||
| SW1710 | Growth Inhibition Assay | IC50=13.3641 μM | SANGER | ||
| COLO-684 | Growth Inhibition Assay | IC50=13.4541 μM | SANGER | ||
| RPMI-7951 | Growth Inhibition Assay | IC50=13.5136 μM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=13.5349 μM | SANGER | ||
| KE-37 | Growth Inhibition Assay | IC50=13.5887 μM | SANGER | ||
| SiHa | Growth Inhibition Assay | IC50=13.8346 μM | SANGER | ||
| NCI-H226 | Growth Inhibition Assay | IC50=13.8808 μM | SANGER | ||
| DB | Growth Inhibition Assay | IC50=13.9928 μM | SANGER | ||
| HT-1197 | Growth Inhibition Assay | IC50=14.0809 μM | SANGER | ||
| SBC-5 | Growth Inhibition Assay | IC50=14.1362 μM | SANGER | ||
| VMRC-RCZ | Growth Inhibition Assay | IC50=14.5774 μM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=14.627 μM | SANGER | ||
| OMC-1 | Growth Inhibition Assay | IC50=14.7888 μM | SANGER | ||
| SKG-IIIa | Growth Inhibition Assay | IC50=14.8001 μM | SANGER | ||
| DOK | Growth Inhibition Assay | IC50=14.9933 μM | SANGER | ||
| NCI-H2029 | Growth Inhibition Assay | IC50=15.3602 μM | SANGER | ||
| NCI-H2009 | Growth Inhibition Assay | IC50=15.5095 μM | SANGER | ||
| LK-2 | Growth Inhibition Assay | IC50=15.6449 μM | SANGER | ||
| NCI-H661 | Growth Inhibition Assay | IC50=15.9075 μM | SANGER | ||
| GT3TKB | Growth Inhibition Assay | IC50=16.0676 μM | SANGER | ||
| GP5d | Growth Inhibition Assay | IC50=16.342 μM | SANGER | ||
| SK-MEL-2 | Growth Inhibition Assay | IC50=16.4485 μM | SANGER | ||
| SK-UT-1 | Growth Inhibition Assay | IC50=16.565 μM | SANGER | ||
| NB7 | Growth Inhibition Assay | IC50=16.6971 μM | SANGER | ||
| NCI-H460 | Growth Inhibition Assay | IC50=16.7326 μM | SANGER | ||
| 8305C | Growth Inhibition Assay | IC50=16.7877 μM | SANGER | ||
| CaR-1 | Growth Inhibition Assay | IC50=16.8111 μM | SANGER | ||
| D-247MG | Growth Inhibition Assay | IC50=16.8625 μM | SANGER | ||
| LoVo | Growth Inhibition Assay | IC50=16.9488 μM | SANGER | ||
| NCI-H2405 | Growth Inhibition Assay | IC50=17.1908 μM | SANGER | ||
| AU565 | Growth Inhibition Assay | IC50=17.225 μM | SANGER | ||
| OCI-AML2 | Growth Inhibition Assay | IC50=17.5317 μM | SANGER | ||
| 22RV1 | Growth Inhibition Assay | IC50=17.5884 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=17.6598 μM | SANGER | ||
| HuO9 | Growth Inhibition Assay | IC50=17.7031 μM | SANGER | ||
| Daoy | Growth Inhibition Assay | IC50=17.7184 μM | SANGER | ||
| SJRH30 | Growth Inhibition Assay | IC50=17.8489 μM | SANGER | ||
| CHL-1 | Growth Inhibition Assay | IC50=17.9249 μM | SANGER | ||
| J82 | Growth Inhibition Assay | IC50=17.9635 μM | SANGER | ||
| COR-L23 | Growth Inhibition Assay | IC50=18.0011 μM | SANGER | ||
| SNU-C2B | Growth Inhibition Assay | IC50=18.2276 μM | SANGER | ||
| NCI-H1770 | Growth Inhibition Assay | IC50=18.4615 μM | SANGER | ||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=18.5697 μM | SANGER | ||
| ES3 | Growth Inhibition Assay | IC50=18.5883 μM | SANGER | ||
| MDA-MB-231 | Growth Inhibition Assay | IC50=18.6502 μM | SANGER | ||
| MN-60 | Growth Inhibition Assay | IC50=19.0592 μM | SANGER | ||
| EPLC-272H | Growth Inhibition Assay | IC50=19.3708 μM | SANGER | ||
| SW948 | Growth Inhibition Assay | IC50=19.3934 μM | SANGER | ||
| MOLT-13 | Growth Inhibition Assay | IC50=19.4546 μM | SANGER | ||
| HL-60 | Growth Inhibition Assay | IC50=20.2141 μM | SANGER | ||
| CP50-MEL-B | Growth Inhibition Assay | IC50=20.4748 μM | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=20.4978 μM | SANGER | ||
| KINGS-1 | Growth Inhibition Assay | IC50=20.7967 μM | SANGER | ||
| DOHH-2 | Growth Inhibition Assay | IC50=20.906 μM | SANGER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=20.9285 μM | SANGER | ||
| NB12 | Growth Inhibition Assay | IC50=21.0394 μM | SANGER | ||
| KY821 | Growth Inhibition Assay | IC50=21.582 μM | SANGER | ||
| PSN1 | Growth Inhibition Assay | IC50=21.6453 μM | SANGER | ||
| EGI-1 | Growth Inhibition Assay | IC50=21.7454 μM | SANGER | ||
| CTV-1 | Growth Inhibition Assay | IC50=22.3031 μM | SANGER | ||
| TI-73 | Growth Inhibition Assay | IC50=22.3498 μM | SANGER | ||
| LCLC-103H | Growth Inhibition Assay | IC50=22.4752 μM | SANGER | ||
| D-542MG | Growth Inhibition Assay | IC50=22.5558 μM | SANGER | ||
| ATN-1 | Growth Inhibition Assay | IC50=22.6439 μM | SANGER | ||
| SK-MEL-1 | Growth Inhibition Assay | IC50=22.8368 μM | SANGER | ||
| HDLM-2 | Growth Inhibition Assay | IC50=23.1478 μM | SANGER | ||
| UM-UC-3 | Growth Inhibition Assay | IC50=23.1944 μM | SANGER | ||
| NCI-H1573 | Growth Inhibition Assay | IC50=23.4681 μM | SANGER | ||
| NCI-H520 | Growth Inhibition Assay | IC50=23.4948 μM | SANGER | ||
| ESS-1 | Growth Inhibition Assay | IC50=23.8059 μM | SANGER | ||
| COR-L88 | Growth Inhibition Assay | IC50=23.9475 μM | SANGER | ||
| TGBC24TKB | Growth Inhibition Assay | IC50=24.0312 μM | SANGER | ||
| HCC1937 | Growth Inhibition Assay | IC50=24.1 μM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=24.142 μM | SANGER | ||
| HCC38 | Growth Inhibition Assay | IC50=24.2394 μM | SANGER | ||
| RPMI-2650 | Growth Inhibition Assay | IC50=24.6162 μM | SANGER | ||
| P12-ICHIKAWA | Growth Inhibition Assay | IC50=24.6258 μM | SANGER | ||
| YAPC | Growth Inhibition Assay | IC50=24.8214 μM | SANGER | ||
| NB13 | Growth Inhibition Assay | IC50=25.2611 μM | SANGER | ||
| SK-N-AS | Growth Inhibition Assay | IC50=25.8584 μM | SANGER | ||
| SK-N-DZ | Growth Inhibition Assay | IC50=26.049 μM | SANGER | ||
| LS-411N | Growth Inhibition Assay | IC50=26.2038 μM | SANGER | ||
| NCI-H810 | Growth Inhibition Assay | IC50=26.3112 μM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=26.5454 μM | SANGER | ||
| HH | Growth Inhibition Assay | IC50=26.5529 μM | SANGER | ||
| U-2-OS | Growth Inhibition Assay | IC50=26.7382 μM | SANGER | ||
| SF539 | Growth Inhibition Assay | IC50=26.8018 μM | SANGER | ||
| NCI-H2052 | Growth Inhibition Assay | IC50=27.086 μM | SANGER | ||
| A673 | Growth Inhibition Assay | IC50=27.2102 μM | SANGER | ||
| WM-115 | Growth Inhibition Assay | IC50=27.7767 μM | SANGER | ||
| SW48 | Growth Inhibition Assay | IC50=27.8005 μM | SANGER | ||
| NOMO-1 | Growth Inhibition Assay | IC50=27.8532 μM | SANGER | ||
| PC-3 | Growth Inhibition Assay | IC50=27.8941 μM | SANGER | ||
| UMC-11 | Growth Inhibition Assay | IC50=27.9343 μM | SANGER | ||
| U-118-MG | Growth Inhibition Assay | IC50=28.0123 μM | SANGER | ||
| NCI-H2452 | Growth Inhibition Assay | IC50=28.0822 μM | SANGER | ||
| CAMA-1 | Growth Inhibition Assay | IC50=28.8564 μM | SANGER | ||
| MC-IXC | Growth Inhibition Assay | IC50=29.2366 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=29.3172 μM | SANGER | ||
| BHT-101 | Growth Inhibition Assay | IC50=29.321 μM | SANGER | ||
| KP-4 | Growth Inhibition Assay | IC50=29.516 μM | SANGER | ||
| CAL-54 | Growth Inhibition Assay | IC50=29.5445 μM | SANGER | ||
| 5637 | Growth Inhibition Assay | IC50=29.6421 μM | SANGER | ||
| MOLT-16 | Growth Inhibition Assay | IC50=29.7269 μM | SANGER | ||
| Ca-Ski | Growth Inhibition Assay | IC50=29.946 μM | SANGER | ||
| AsPC-1 | Growth Inhibition Assay | IC50=30.0212 μM | SANGER | ||
| MSTO-211H | Growth Inhibition Assay | IC50=30.15 μM | SANGER | ||
| L-428 | Growth Inhibition Assay | IC50=30.405 μM | SANGER | ||
| SW1463 | Growth Inhibition Assay | IC50=30.5383 μM | SANGER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=30.5574 μM | SANGER | ||
| CAKI-1 | Growth Inhibition Assay | IC50=30.7702 μM | SANGER | ||
| YKG-1 | Growth Inhibition Assay | IC50=31.0263 μM | SANGER | ||
| A2058 | Growth Inhibition Assay | IC50=31.1164 μM | SANGER | ||
| A375 | Growth Inhibition Assay | IC50=31.1696 μM | SANGER | ||
| SNB75 | Growth Inhibition Assay | IC50=31.2435 μM | SANGER | ||
| SK-HEP-1 | Growth Inhibition Assay | IC50=31.4271 μM | SANGER | ||
| ME-180 | Growth Inhibition Assay | IC50=31.6542 μM | SANGER | ||
| NCI-H209 | Growth Inhibition Assay | IC50=31.8247 μM | SANGER | ||
| HC-1 | Growth Inhibition Assay | IC50=32.1446 μM | SANGER | ||
| LB373-MEL-D | Growth Inhibition Assay | IC50=32.1971 μM | SANGER | ||
| SNU-387 | Growth Inhibition Assay | IC50=32.3191 μM | SANGER | ||
| C32 | Growth Inhibition Assay | IC50=32.3353 μM | SANGER | ||
| EW-13 | Growth Inhibition Assay | IC50=32.9408 μM | SANGER | ||
| BFTC-905 | Growth Inhibition Assay | IC50=33.5136 μM | SANGER | ||
| NCI-H1299 | Growth Inhibition Assay | IC50=33.5621 μM | SANGER | ||
| LU-135 | Growth Inhibition Assay | IC50=33.801 μM | SANGER | ||
| NCI-H2122 | Growth Inhibition Assay | IC50=33.9966 μM | SANGER | ||
| SK-LMS-1 | Growth Inhibition Assay | IC50=34.4107 μM | SANGER | ||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=34.8515 μM | SANGER | ||
| NCI-H1092 | Growth Inhibition Assay | IC50=35.2747 μM | SANGER | ||
| MS-1 | Growth Inhibition Assay | IC50=35.3038 μM | SANGER | ||
| KYSE-510 | Growth Inhibition Assay | IC50=35.5042 μM | SANGER | ||
| NCI-H1793 | Growth Inhibition Assay | IC50=35.6545 μM | SANGER | ||
| MIA-PaCa-2 | Growth Inhibition Assay | IC50=36.0496 μM | SANGER | ||
| EW-22 | Growth Inhibition Assay | IC50=36.4072 μM | SANGER | ||
| IGR-1 | Growth Inhibition Assay | IC50=36.8184 μM | SANGER | ||
| HT-1080 | Growth Inhibition Assay | IC50=37.125 μM | SANGER | ||
| M14 | Growth Inhibition Assay | IC50=37.1642 μM | SANGER | ||
| 786-0 | Growth Inhibition Assay | IC50=37.2794 μM | SANGER | ||
| MZ2-MEL | Growth Inhibition Assay | IC50=37.4501 μM | SANGER | ||
| NCI-H510A | Growth Inhibition Assay | IC50=37.9412 μM | SANGER | ||
| LAN-6 | Growth Inhibition Assay | IC50=37.9582 μM | SANGER | ||
| SW620 | Growth Inhibition Assay | IC50=38.4974 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=39.8205 μM | SANGER | ||
| Detroit562 | Growth Inhibition Assay | IC50=40.1268 μM | SANGER | ||
| HN | Growth Inhibition Assay | IC50=40.1782 μM | SANGER | ||
| HCT-15 | Growth Inhibition Assay | IC50=40.5907 μM | SANGER | ||
| C2BBe1 | Growth Inhibition Assay | IC50=40.9157 μM | SANGER | ||
| A498 | Growth Inhibition Assay | IC50=41.3015 μM | SANGER | ||
| SK-MEL-24 | Growth Inhibition Assay | IC50=41.4725 μM | SANGER | ||
| OVCAR-5 | Growth Inhibition Assay | IC50=41.7767 μM | SANGER | ||
| NCI-H1792 | Growth Inhibition Assay | IC50=41.9821 μM | SANGER | ||
| KOSC-2 | Growth Inhibition Assay | IC50=42.2699 μM | SANGER | ||
| Mo-T | Growth Inhibition Assay | IC50=42.8958 μM | SANGER | ||
| CFPAC-1 | Growth Inhibition Assay | IC50=43.4944 μM | SANGER | ||
| CAL-51 | Growth Inhibition Assay | IC50=43.5605 μM | SANGER | ||
| RH-18 | Growth Inhibition Assay | IC50=43.805 μM | SANGER | ||
| EC-GI-10 | Growth Inhibition Assay | IC50=43.8347 μM | SANGER | ||
| HSC-2 | Growth Inhibition Assay | IC50=44.009 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=45.2621 μM | SANGER | ||
| KNS-81-FD | Growth Inhibition Assay | IC50=45.7365 μM | SANGER | ||
| NB6 | Growth Inhibition Assay | IC50=46.111 μM | SANGER | ||
| MCF7 | Growth Inhibition Assay | IC50=46.5533 μM | SANGER | ||
| P30-OHK | Growth Inhibition Assay | IC50=46.8117 μM | SANGER | ||
| BPH-1 | Growth Inhibition Assay | IC50=46.9805 μM | SANGER | ||
| U251 | Growth Inhibition Assay | IC50=46.994 μM | SANGER | ||
| MKN1 | Growth Inhibition Assay | IC50=47.5137 μM | SANGER | ||
| A431 | Growth Inhibition Assay | IC50=47.8338 μM | SANGER | ||
| C8166 | Growth Inhibition Assay | IC50=49.2039 μM | SANGER | ||
| HEL | Growth Inhibition Assay | IC50=49.4064 μM | SANGER | ||
| RMG-I | Growth Inhibition Assay | IC50=49.4444 μM | SANGER | ||
| CAL-72 | Growth Inhibition Assay | IC50=49.6075 μM | SANGER | ||
| SW962 | Growth Inhibition Assay | IC50=49.9332 μM | SANGER | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Axitinib是一种多靶点抑制剂，作用于 VEGFR1，VEGFR2，VEGFR3，PDGFRβ和c-Kit，在猪主动脉内皮细胞中IC50分别为0.1 nM，0.2 nM，0.1-0.3 nM，1.6 nM和1.7 nM。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | Axitinib与目前使用的sorafenib相比，作为二代治疗法，更有效。 | |||||||||||
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | Axitinib是受体激酶抑制剂，作用于VEGFR-1, VEGFR-2，VEGFR-3， PDGFR-β和c-KIT时IC50分别为0.1 , 0.2, 0.1-0.3, 1.6 和1.7 nM 。[1]Axitinib可以阻断VEGFR的自磷酸化作用，VEGF调节的内皮细胞活力，微管形成，及下游信号。Axitinib抑制多种细胞系的增殖，如作用于IGR-N91, IGR-NB8, SH-SY5Y ，无VEGF刺激的HUVEC时IC50分别为>1000 nM, 849 nM, 274 nM和573 nM。[2] | |||
|---|---|---|---|---|
| 激酶实验 | 细胞受体激酶磷酸化实验 | |||
| 生成过量表达全长VEGFR-2, PDGFR-β, 和KIT的PAE 细胞，及过量表达鼠VEGFR-2 (Flk-1) 或 PDGFR-α的NIH-3T3细胞。用2.5 µg/mL VEGFR-2抗体, 0.75 µg/mL anti-PDGFR-β 抗体, 0.25 µg/mL anti-PDGFR-α 抗体, 及0.5 µg/mL anti-KIT 抗体包被96孔板，每孔100ul。或者用1.20 µg/mL Flk-1抗体制成酶联免疫吸附（ELISA）捕获板。通过ELISA测定RTK的磷酸化作用。 | ||||
| 细胞实验 | 细胞系 | HUVEC,SH-SY5Y, IGR-N91，和IGR-NB8细胞 | ||
| 浓度 | 1 nM 到10 µM | |||
| 孵育时间 | 72小时 | |||
| 方法 | HUVEC, SH-SY5Y, IGR-N91和IGR-NB8细胞系按5x104密度接种在96孔板上，培养24小时。加入浓度不等（1 nM到10 µM）的Axitinib。72小时后，通过 MTS四唑基底物测定细胞活力，计算IC50值。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-c-kit / c-kit / p-AKT / AKT / p-ERK / ERK / p-STAT3 / STAT3 / p-STAT5 / STAT5 / p-S6K / S6K / p-S6 / S6 PARP / cleaved PARP / caspase-3 / cleaved caspase-3 |
|
31205508 | |
| Immunofluorescence | alpha-tubulin |
|
26474283 | |
| Growth inhibition assay | Cell viability |
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26474283 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Axitinib抑制常位移植模型，如M24met (黑色素瘤), HCT-116 (结肠直肠癌), 和SN12C (肾细胞癌)。[1]活体研究显示，按动物体重，每千克口服处理30mg Axitinib，与没有Axitinib处理的对照组相比，实验组推迟肿瘤生长达到11.4天；且用于IGR-N91侧腹移植瘤时，与对照组（密度为49）相比实验组（密度降为21）降低血管密度。[2]Axitinib在多种肿瘤包括肾细胞癌，甲状腺癌，非小细胞肺癌，黑色素瘤中显示出单一药效活性。 | |
|---|---|---|
| 动物实验 | Animal Models | BT474胸腺癌细胞皮下移植到雌性免疫缺陷小鼠内(Nu/nu;8-12周大） |
| Dosages | 10, 30或100 mg/kg | |
| Administration | 每天口服处理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06161558 | Not yet recruiting | Neoplasms |
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
January 12 2024 | Phase 1 |
| NCT05969496 | Recruiting | Renal Cancer|Kidney Cancer|Renal Cell Carcinoma|Inferior Vena Cava Thrombosis |
University of Colorado Denver|Cancer League of Colorado |
December 14 2023 | Phase 2 |
| NCT05949632 | Not yet recruiting | Advanced Solid Tumors |
Incyte Corporation |
December 15 2023 | Phase 1|Phase 2 |
| NCT05904730 | Enrolling by invitation | Breast Cancer|Ovarian Cancer|Breast Neoplasms|Ovarian Neoplasms|BRCA Mutation|HER2-positive Breast Cancer|HER2-negative Breast Cancer|HER-2 Protein Overexpression |
Lynkcell Europe |
July 11 2023 | Phase 1 |
| NCT05817903 | Recruiting | Metastatic Renal Cell Carcinoma |
Consorzio Oncotech|Pfizer |
April 18 2023 | Phase 2 |
化学信息&溶解度
| 分子量 | 386.47 | 分子式 | C22H18N4OS |
| CAS号 | 319460-85-0 | SDF | Download Axitinib SDF |
| Smiles | CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(=NN3)C=CC4=CC=CC=N4 | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 26 mg/mL ( (67.27 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
技术支持
在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。
如果有其他问题，请给我们留言。
* 必填项
常见问题及建议解决方法
问题 1:
We would like to store at -80℃ after it dissolved in CMC. Do you have any infomation about the suggested concentration in CMC?
回答：
Axitinib in 0.5% CMC at up to 30mg/ml is a suspension for oral gavage administration only. We don't suggest customer to freeze down the solution but to make fresh if possible. Customer can store it for 1-2 weeks at 4 degree for continuous use.
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