TAE684 (NVP-TAE684)
TAE684 (NVP-TAE684) 是一种有效的，选择性 ALK 抑制剂，能阻断ALCL来源的ALK依赖性细胞系的生长，IC50 介于2nM到10nM之间，作用于ALK比作用于InsR选择性高100倍。TAE684 (NVP-TAE684) 可诱导细胞周期阻滞和凋亡。
TAE684 (NVP-TAE684) Chemical Structure
CAS: 761439-42-3
客户使用Selleck的TAE684 (NVP-TAE684)发表文献81篇
产品质控
批次：
纯度：
99.73%
99.73
TAE684 (NVP-TAE684)相关产品
| 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 |
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相关信号通路图
ALK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 |
|---|---|---|---|---|---|
| SCC-3 | Growth Inhibition Assay | IC50=0.0000603 μM | SANGER | ||
| SF539 | Growth Inhibition Assay | IC50=0.000564 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=0.000927 μM | SANGER | ||
| NB1 | Growth Inhibition Assay | IC50=0.00162 μM | SANGER | ||
| SR | Growth Inhibition Assay | IC50=0.00277 μM | SANGER | ||
| KARPAS-299 | Growth Inhibition Assay | IC50=0.02384 μM | SANGER | ||
| MHH-CALL-2 | Growth Inhibition Assay | IC50=0.02952 μM | SANGER | ||
| SU-DHL-1 | Growth Inhibition Assay | IC50=0.04865 μM | SANGER | ||
| A4-Fuk | Growth Inhibition Assay | IC50=0.05565 μM | SANGER | ||
| EW-1 | Growth Inhibition Assay | IC50=0.10256 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=0.10294 μM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=0.10568 μM | SANGER | ||
| TE-11 | Growth Inhibition Assay | IC50=0.16096 μM | SANGER | ||
| SW982 | Growth Inhibition Assay | IC50=0.16478 μM | SANGER | ||
| LAN-6 | Growth Inhibition Assay | IC50=0.17443 μM | SANGER | ||
| MZ1-PC | Growth Inhibition Assay | IC50=0.17835 μM | SANGER | ||
| KS-1 | Growth Inhibition Assay | IC50=0.19343 μM | SANGER | ||
| PSN1 | Growth Inhibition Assay | IC50=0.19631 μM | SANGER | ||
| LC-2-ad | Growth Inhibition Assay | IC50=0.19692 μM | SANGER | ||
| COLO-320-HSR | Growth Inhibition Assay | IC50=0.19776 μM | SANGER | ||
| OPM-2 | Growth Inhibition Assay | IC50=0.22669 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=0.23524 μM | SANGER | ||
| ALL-PO | Growth Inhibition Assay | IC50=0.24524 μM | SANGER | ||
| CMK | Growth Inhibition Assay | IC50=0.2553 μM | SANGER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=0.27855 μM | SANGER | ||
| SIG-M5 | Growth Inhibition Assay | IC50=0.29159 μM | SANGER | ||
| TGBC24TKB | Growth Inhibition Assay | IC50=0.30218 μM | SANGER | ||
| DOHH-2 | Growth Inhibition Assay | IC50=0.31204 μM | SANGER | ||
| NB69 | Growth Inhibition Assay | IC50=0.31787 μM | SANGER | ||
| MFH-ino | Growth Inhibition Assay | IC50=0.32523 μM | SANGER | ||
| KP-N-RT-BM-1 | Growth Inhibition Assay | IC50=0.33123 μM | SANGER | ||
| MONO-MAC-6 | Growth Inhibition Assay | IC50=0.33291 μM | SANGER | ||
| ATN-1 | Growth Inhibition Assay | IC50=0.33303 μM | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=0.33396 μM | SANGER | ||
| L-540 | Growth Inhibition Assay | IC50=0.36988 μM | SANGER | ||
| GB-1 | Growth Inhibition Assay | IC50=0.38867 μM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=0.39446 μM | SANGER | ||
| KG-1 | Growth Inhibition Assay | IC50=0.39561 μM | SANGER | ||
| OVCAR-4 | Growth Inhibition Assay | IC50=0.40569 μM | SANGER | ||
| NEC8 | Growth Inhibition Assay | IC50=0.41292 μM | SANGER | ||
| SK-MM-2 | Growth Inhibition Assay | IC50=0.41609 μM | SANGER | ||
| TE-8 | Growth Inhibition Assay | IC50=0.4288 μM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=0.43215 μM | SANGER | ||
| NB14 | Growth Inhibition Assay | IC50=0.43826 μM | SANGER | ||
| GDM-1 | Growth Inhibition Assay | IC50=0.47116 μM | SANGER | ||
| HUTU-80 | Growth Inhibition Assay | IC50=0.47375 μM | SANGER | ||
| HL-60 | Growth Inhibition Assay | IC50=0.48142 μM | SANGER | ||
| OCI-AML2 | Growth Inhibition Assay | IC50=0.48328 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=0.49031 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=0.49109 μM | SANGER | ||
| NCI-H747 | Growth Inhibition Assay | IC50=0.4989 μM | SANGER | ||
| RL95-2 | Growth Inhibition Assay | IC50=0.50112 μM | SANGER | ||
| TE-15 | Growth Inhibition Assay | IC50=0.51124 μM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=0.53349 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=0.54549 μM | SANGER | ||
| LB831-BLC | Growth Inhibition Assay | IC50=0.55023 μM | SANGER | ||
| NCI-H1355 | Growth Inhibition Assay | IC50=0.55184 μM | SANGER | ||
| CTV-1 | Growth Inhibition Assay | IC50=0.55624 μM | SANGER | ||
| RXF393 | Growth Inhibition Assay | IC50=0.55794 μM | SANGER | ||
| SW872 | Growth Inhibition Assay | IC50=0.56724 μM | SANGER | ||
| MPP-89 | Growth Inhibition Assay | IC50=0.57884 μM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=0.63526 μM | SANGER | ||
| LS-1034 | Growth Inhibition Assay | IC50=0.6358 μM | SANGER | ||
| SJSA-1 | Growth Inhibition Assay | IC50=0.63725 μM | SANGER | ||
| HOP-62 | Growth Inhibition Assay | IC50=0.65033 μM | SANGER | ||
| KGN | Growth Inhibition Assay | IC50=0.66168 μM | SANGER | ||
| D-336MG | Growth Inhibition Assay | IC50=0.66169 μM | SANGER | ||
| LS-411N | Growth Inhibition Assay | IC50=0.67462 μM | SANGER | ||
| TE-1 | Growth Inhibition Assay | IC50=0.69074 μM | SANGER | ||
| LB996-RCC | Growth Inhibition Assay | IC50=0.69389 μM | SANGER | ||
| TE-10 | Growth Inhibition Assay | IC50=0.71496 μM | SANGER | ||
| NCI-SNU-16 | Growth Inhibition Assay | IC50=0.72664 μM | SANGER | ||
| ES8 | Growth Inhibition Assay | IC50=0.74975 μM | SANGER | ||
| COLO-800 | Growth Inhibition Assay | IC50=0.76695 μM | SANGER | ||
| ES6 | Growth Inhibition Assay | IC50=0.77559 μM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=0.82375 μM | SANGER | ||
| NMC-G1 | Growth Inhibition Assay | IC50=0.83233 μM | SANGER | ||
| LU-134-A | Growth Inhibition Assay | IC50=0.83912 μM | SANGER | ||
| SF268 | Growth Inhibition Assay | IC50=0.84042 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=0.84263 μM | SANGER | ||
| TGW | Growth Inhibition Assay | IC50=0.85863 μM | SANGER | ||
| CHP-126 | Growth Inhibition Assay | IC50=0.85957 μM | SANGER | ||
| MOLT-16 | Growth Inhibition Assay | IC50=0.87589 μM | SANGER | ||
| LB771-HNC | Growth Inhibition Assay | IC50=0.89757 μM | SANGER | ||
| NALM-6 | Growth Inhibition Assay | IC50=0.90739 μM | SANGER | ||
| GCIY | Growth Inhibition Assay | IC50=0.95526 μM | SANGER | ||
| IST-MES1 | Growth Inhibition Assay | IC50=0.98824 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=0.9884 μM | SANGER | ||
| BL-70 | Growth Inhibition Assay | IC50=0.99535 μM | SANGER | ||
| NB17 | Growth Inhibition Assay | IC50=1.00639 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=1.03076 μM | SANGER | ||
| TK10 | Growth Inhibition Assay | IC50=1.05063 μM | SANGER | ||
| K5 | Growth Inhibition Assay | IC50=1.06274 μM | SANGER | ||
| NCI-H716 | Growth Inhibition Assay | IC50=1.07259 μM | SANGER | ||
| HCE-T | Growth Inhibition Assay | IC50=1.08819 μM | SANGER | ||
| GI-1 | Growth Inhibition Assay | IC50=1.09798 μM | SANGER | ||
| KARPAS-422 | Growth Inhibition Assay | IC50=1.10022 μM | SANGER | ||
| TE-9 | Growth Inhibition Assay | IC50=1.11328 μM | SANGER | ||
| SF126 | Growth Inhibition Assay | IC50=1.11568 μM | SANGER | ||
| BB30-HNC | Growth Inhibition Assay | IC50=1.13112 μM | SANGER | ||
| NCI-H1304 | Growth Inhibition Assay | IC50=1.13338 μM | SANGER | ||
| HEL | Growth Inhibition Assay | IC50=1.14895 μM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=1.15283 μM | SANGER | ||
| SK-LMS-1 | Growth Inhibition Assay | IC50=1.15974 μM | SANGER | ||
| SW954 | Growth Inhibition Assay | IC50=1.19567 μM | SANGER | ||
| D-283MED | Growth Inhibition Assay | IC50=1.22379 μM | SANGER | ||
| NCI-H1882 | Growth Inhibition Assay | IC50=1.2389 μM | SANGER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=1.25208 μM | SANGER | ||
| SK-PN-DW | Growth Inhibition Assay | IC50=1.26348 μM | SANGER | ||
| C2BBe1 | Growth Inhibition Assay | IC50=1.29117 μM | SANGER | ||
| A704 | Growth Inhibition Assay | IC50=1.32689 μM | SANGER | ||
| KALS-1 | Growth Inhibition Assay | IC50=1.3408 μM | SANGER | ||
| ETK-1 | Growth Inhibition Assay | IC50=1.34489 μM | SANGER | ||
| LB647-SCLC | Growth Inhibition Assay | IC50=1.34986 μM | SANGER | ||
| OCUB-M | Growth Inhibition Assay | IC50=1.36143 μM | SANGER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=1.36378 μM | SANGER | ||
| NB13 | Growth Inhibition Assay | IC50=1.37293 μM | SANGER | ||
| GR-ST | Growth Inhibition Assay | IC50=1.38757 μM | SANGER | ||
| DU-4475 | Growth Inhibition Assay | IC50=1.45853 μM | SANGER | ||
| HCC2157 | Growth Inhibition Assay | IC50=1.46659 μM | SANGER | ||
| RKO | Growth Inhibition Assay | IC50=1.49922 μM | SANGER | ||
| LS-123 | Growth Inhibition Assay | IC50=1.51594 μM | SANGER | ||
| NCI-H69 | Growth Inhibition Assay | IC50=1.55811 μM | SANGER | ||
| SW962 | Growth Inhibition Assay | IC50=1.5613 μM | SANGER | ||
| PF-382 | Growth Inhibition Assay | IC50=1.5696 μM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=1.57113 μM | SANGER | ||
| NB10 | Growth Inhibition Assay | IC50=1.57392 μM | SANGER | ||
| NB5 | Growth Inhibition Assay | IC50=1.58476 μM | SANGER | ||
| HCE-4 | Growth Inhibition Assay | IC50=1.6085 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=1.6319 μM | SANGER | ||
| NCI-H524 | Growth Inhibition Assay | IC50=1.64307 μM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=1.6866 μM | SANGER | ||
| KURAMOCHI | Growth Inhibition Assay | IC50=1.69573 μM | SANGER | ||
| NCI-H187 | Growth Inhibition Assay | IC50=1.70036 μM | SANGER | ||
| U-266 | Growth Inhibition Assay | IC50=1.73842 μM | SANGER | ||
| BL-41 | Growth Inhibition Assay | IC50=1.76272 μM | SANGER | ||
| SK-N-DZ | Growth Inhibition Assay | IC50=1.78309 μM | SANGER | ||
| Daudi | Growth Inhibition Assay | IC50=1.78967 μM | SANGER | ||
| CPC-N | Growth Inhibition Assay | IC50=1.85096 μM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=1.851 μM | SANGER | ||
| HCC1187 | Growth Inhibition Assay | IC50=1.86241 μM | SANGER | ||
| LP-1 | Growth Inhibition Assay | IC50=1.87143 μM | SANGER | ||
| CAS-1 | Growth Inhibition Assay | IC50=1.98299 μM | SANGER | ||
| NB7 | Growth Inhibition Assay | IC50=2.00555 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=2.01513 μM | SANGER | ||
| SNU-C2B | Growth Inhibition Assay | IC50=2.03351 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=2.06786 μM | SANGER | ||
| NCI-H1581 | Growth Inhibition Assay | IC50=2.11559 μM | SANGER | ||
| IST-SL2 | Growth Inhibition Assay | IC50=2.12445 μM | SANGER | ||
| NOMO-1 | Growth Inhibition Assay | IC50=2.17683 μM | SANGER | ||
| TE-6 | Growth Inhibition Assay | IC50=2.1905 μM | SANGER | ||
| NCI-H526 | Growth Inhibition Assay | IC50=2.19141 μM | SANGER | ||
| MSTO-211H | Growth Inhibition Assay | IC50=2.20041 μM | SANGER | ||
| LS-513 | Growth Inhibition Assay | IC50=2.22269 μM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=2.33256 μM | SANGER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=2.37493 μM | SANGER | ||
| GT3TKB | Growth Inhibition Assay | IC50=2.39972 μM | SANGER | ||
| OS-RC-2 | Growth Inhibition Assay | IC50=2.42341 μM | SANGER | ||
| NCI-H2126 | Growth Inhibition Assay | IC50=2.43674 μM | SANGER | ||
| SK-UT-1 | Growth Inhibition Assay | IC50=2.47467 μM | SANGER | ||
| DMS-114 | Growth Inhibition Assay | IC50=2.61524 μM | SANGER | ||
| ONS-76 | Growth Inhibition Assay | IC50=2.63641 μM | SANGER | ||
| 8-MG-BA | Growth Inhibition Assay | IC50=2.65414 μM | SANGER | ||
| BOKU | Growth Inhibition Assay | IC50=2.72764 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=2.79912 μM | SANGER | ||
| ES1 | Growth Inhibition Assay | IC50=2.81804 μM | SANGER | ||
| NCI-H1395 | Growth Inhibition Assay | IC50=2.82012 μM | SANGER | ||
| A388 | Growth Inhibition Assay | IC50=2.9617 μM | SANGER | ||
| NCCIT | Growth Inhibition Assay | IC50=3.08862 μM | SANGER | ||
| HD-MY-Z | Growth Inhibition Assay | IC50=3.13203 μM | SANGER | ||
| NCI-H510A | Growth Inhibition Assay | IC50=3.18943 μM | SANGER | ||
| NCI-N87 | Growth Inhibition Assay | IC50=3.2002 μM | SANGER | ||
| SCLC-21H | Growth Inhibition Assay | IC50=3.26859 μM | SANGER | ||
| SH-4 | Growth Inhibition Assay | IC50=3.28797 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=3.32849 μM | SANGER | ||
| KM12 | Growth Inhibition Assay | IC50=3.33544 μM | SANGER | ||
| ST486 | Growth Inhibition Assay | IC50=3.53883 μM | SANGER | ||
| HC-1 | Growth Inhibition Assay | IC50=3.62028 μM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=3.64088 μM | SANGER | ||
| EW-24 | Growth Inhibition Assay | IC50=3.66434 μM | SANGER | ||
| LU-65 | Growth Inhibition Assay | IC50=3.6871 μM | SANGER | ||
| ECC4 | Growth Inhibition Assay | IC50=3.7756 μM | SANGER | ||
| ARH-77 | Growth Inhibition Assay | IC50=4.11067 μM | SANGER | ||
| BC-3 | Growth Inhibition Assay | IC50=4.13068 μM | SANGER | ||
| SNB75 | Growth Inhibition Assay | IC50=4.2619 μM | SANGER | ||
| MEG-01 | Growth Inhibition Assay | IC50=4.27419 μM | SANGER | ||
| NCI-H1417 | Growth Inhibition Assay | IC50=4.28443 μM | SANGER | ||
| MDA-MB-134-VI | Growth Inhibition Assay | IC50=4.30601 μM | SANGER | ||
| Becker | Growth Inhibition Assay | IC50=4.47336 μM | SANGER | ||
| DMS-153 | Growth Inhibition Assay | IC50=4.66475 μM | SANGER | ||
| TGBC1TKB | Growth Inhibition Assay | IC50=4.68515 μM | SANGER | ||
| EW-3 | Growth Inhibition Assay | IC50=4.76248 μM | SANGER | ||
| KE-37 | Growth Inhibition Assay | IC50=4.86196 μM | SANGER | ||
| NCI-H23 | Growth Inhibition Assay | IC50=4.87227 μM | SANGER | ||
| MC116 | Growth Inhibition Assay | IC50=4.94126 μM | SANGER | ||
| NH-12 | Growth Inhibition Assay | IC50=4.96439 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=4.97721 μM | SANGER | ||
| KM-H2 | Growth Inhibition Assay | IC50=5.05323 μM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=5.1183 μM | SANGER | ||
| NCI-H2141 | Growth Inhibition Assay | IC50=5.14268 μM | SANGER | ||
| EB-3 | Growth Inhibition Assay | IC50=5.17504 μM | SANGER | ||
| NCI-H1522 | Growth Inhibition Assay | IC50=5.26322 μM | SANGER | ||
| MRK-nu-1 | Growth Inhibition Assay | IC50=5.43633 μM | SANGER | ||
| no-11 | Growth Inhibition Assay | IC50=5.47087 μM | SANGER | ||
| CESS | Growth Inhibition Assay | IC50=5.58034 μM | SANGER | ||
| KMOE-2 | Growth Inhibition Assay | IC50=5.58659 μM | SANGER | ||
| REH | Growth Inhibition Assay | IC50=6.25618 μM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=6.42791 μM | SANGER | ||
| SK-N-FI | Growth Inhibition Assay | IC50=6.60674 μM | SANGER | ||
| MMAC-SF | Growth Inhibition Assay | IC50=7.06492 μM | SANGER | ||
| RCC10RGB | Growth Inhibition Assay | IC50=7.22977 μM | SANGER | ||
| NCI-H322M | Growth Inhibition Assay | IC50=7.33335 μM | SANGER | ||
| NB6 | Growth Inhibition Assay | IC50=7.54899 μM | SANGER | ||
| MN-60 | Growth Inhibition Assay | IC50=7.69215 μM | SANGER | ||
| NCI-H1092 | Growth Inhibition Assay | IC50=8.01734 μM | SANGER | ||
| EKVX | Growth Inhibition Assay | IC50=8.47066 μM | SANGER | ||
| D-263MG | Growth Inhibition Assay | IC50=8.55396 μM | SANGER | ||
| NCI-H209 | Growth Inhibition Assay | IC50=8.64006 μM | SANGER | ||
| IST-SL1 | Growth Inhibition Assay | IC50=8.89892 μM | SANGER | ||
| ACN | Growth Inhibition Assay | IC50=9.19157 μM | SANGER | ||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=9.21219 μM | SANGER | ||
| EW-11 | Growth Inhibition Assay | IC50=9.65396 μM | SANGER | ||
| KASUMI-1 | Growth Inhibition Assay | IC50=9.7877 μM | SANGER | ||
| KINGS-1 | Growth Inhibition Assay | IC50=10.2347 μM | SANGER | ||
| EVSA-T | Growth Inhibition Assay | IC50=10.3192 μM | SANGER | ||
| DSH1 | Growth Inhibition Assay | IC50=10.3972 μM | SANGER | ||
| COLO-824 | Growth Inhibition Assay | IC50=10.8669 μM | SANGER | ||
| K052 | Growth Inhibition Assay | IC50=10.9322 μM | SANGER | ||
| SK-MEL-2 | Growth Inhibition Assay | IC50=10.9939 μM | SANGER | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | TAE684 (NVP-TAE684) 是一种有效的，选择性 ALK 抑制剂，能阻断ALCL来源的ALK依赖性细胞系的生长，IC50 介于2nM到10nM之间，作用于ALK比作用于InsR选择性高100倍。TAE684 (NVP-TAE684) 可诱导细胞周期阻滞和凋亡。 | ||
|---|---|---|---|
| 特性 | NVP-TAE684 作为治疗难治愈和复发的ALK阳性淋巴癌的一种策略，但是还没进行临床实验。 | ||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | NVP-TAE684选择性有效抑制ALK激酶，作用于其他激酶则没有明显的交叉反应。NVP-TAE684 有效抑制Ba/F3 NPM-ALK 细胞增殖，IC50 为3 nM, 1 μM NVP-TAE684对Ba/F3 细胞存活没有效果。NVP-TAE684 也抑制表达NPM-ALK人类ALCL细胞系的增殖，包括Karpas-299和SU-DHL-1，IC50为2-5 nM。分子模型显示L258 可能为NVP-TAE684的主要激酶选择性影响因素之一。用NVP-TAE684处理，快速且持久地抑制NPM-ALK的磷酸化作用。NVP-TAE684 作用于表达NPM-ALK的 Ba/F3 细胞和ALCL病患细胞系，诱导细胞凋亡，且使细胞周期停在G1期。[1] NVP-TAE684 作用于H3122 CR细胞，显著克服细胞抗Crizotinib的特性, 含有融合致癌基因EML4-ALK, 降低细胞生长，抑制ALK磷酸化作用和诱导细胞凋亡。[2] 30 nM NVP-TAE684可抑制mALK R1279Q 突变表达诱导的神经突增生。[3] |
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|---|---|---|---|---|
| 激酶实验 | 体外酶实验 | |||
| 使用同质时间分辨荧光法测定NVP-TAE684作用于InsR和IGF1R的IC50 值。ATP (10 mM)和20 mg/ml 生物素PolyEY (Glu, Tyr 4:1)，与50 nL NVP-TAE684连续稀释液 (10-500 nM) ，和4 ng InsR 酶，和激酶反应buffer (包括20 mM Tris×HCl, pH 为7.5 /10 mM MgCl2/3 mM MnCl2/1 mM DTT/10 mM NaVO4/0.1 mg/ml of BSA)混合。在室温下温育1小时。加入10 mL检测液终止反应，检测液含50 mM EDTA, 500 mM KF, 0.5 mg/ml of BSA, 5 mg/ml Eu3+ 穴状化合物标记的磷酸酪氨酸抗体PT66-K,及5 mg/ml 链霉亲和素-XLent。反应进行半小时，在Analyst GT上读取荧光信号。 | ||||
| 细胞实验 | 细胞系 | 表达Luciferase的Karpas-299, SU-DHL-1,和Ba/F3 细胞，及稳定表达Ba/F3转变的 NPM-ALK, BCR-ABL,或TEL激酶融合构成。 | ||
| 浓度 | 1 nM-10 μM | |||
| 孵育时间 | 2到3天 | |||
| 方法 | 细胞按每孔2.5×104个接种在384孔板上，和NVP-TAE684的连续稀释液或DMSO温育2到3天。使用Luciferase表达系统测定细胞增殖和存活，然后用Bright-Glo Luciferase 实验系统测评。使用XLFit 软件测定IC50值。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Growth inhibition assay | Cell viability |
|
18594010 | |
| Western blot | p-ROS1 / ROS1 p-ALK / ALK / p-STAT3 / STAT3 / p-ERK / ERK / p-AKT / AKT / Survivin / BIM / PARP |
|
25351743 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 |
3和10 mg/kg NVP-TAE684处理4周后,明显减慢淋巴癌生长转移，作用于Karpas-299淋巴癌模型没有毒性。用NVP-TAE684处理Karpas-299 淋巴癌也诱导疾病衰退和下调CD30表达。[1] NVP-TAE684 作用于H3122 CR移植瘤显示出明显的抗癌活性。[2] 用NVP-TAE684处理也提升ALK突变的表现型,尤其是ALKR1275Q, 然而Crizotinib 对表现型没有影响。[3] |
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|---|---|---|
| 动物实验 | Animal Models | 4到6周大的携带Karpas-299移植瘤的雌性Fox Chase SCIDBeige 鼠 |
| Dosages | 1, 3, 和 10 mg/kg | |
| Administration | 每天口服饲喂，持续3周。 | |
化学信息&溶解度
| 分子量 | 614.2 | 分子式 | C30H40ClN7O3S |
| CAS号 | 761439-42-3 | SDF | Download TAE684 (NVP-TAE684) SDF |
| Smiles | CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCC(CC4)N5CCN(CC5)C)OC | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 10 mg/mL ( (16.28 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。
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