Carfilzomib (PR-171)
中文名称：卡非佐米
Carfilzomib (PR-171) 是一种不可逆proteasome抑制剂，在ANBL-6细胞中IC50为<5 nM，在体外优先抑制β5亚基的ChT-L活性，对PGPH和T-L活性很弱或没有作用。Carfilzomib 可激活自噬并诱导细胞凋亡。
Carfilzomib (PR-171) Chemical Structure
CAS: 868540-17-4
产品质控
批次：
纯度：
99.75%
99.75
Carfilzomib (PR-171)相关产品
| 相关靶点 | 20S proteasome | 点击展开 |
|---|---|---|
| 相关产品 | MG132 Epoxomicin (BU-4061T) Celastrol Oprozomib ONX-0914 (PR-957) Delanzomib VR23 Marizomib (Salinosporamide A) PI-1840 | 点击展开 |
| 相关化合物库 | FDA药物库 天然产物库 已知活性药物库-I 蛋白酶抑制剂库 泛素化化合物库 | 点击展开 |
相关信号通路图
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 |
|---|---|---|---|---|---|
| UMSCC-1 | Apoptosis Asssay | 200 nM | 24 h | induce the cell apoptosis co-treatment with ONX 0912 | 22929803 |
| 1483 | Apoptosis Asssay | 200 nM | 24 h | induce the cell apoptosis co-treatment with ONX 0912 | 22929803 |
| UMSCC-22B | Apoptosis Asssay | 200 nM | 24 h | induce the cell apoptosis co-treatment with ONX 0912 | 22929803 |
| UMSCC-22A | Apoptosis Asssay | 200 nM | 24 h | induce the cell apoptosis co-treatment with ONX 0912 | 22929803 |
| Jurkat | Apoptosis Asssay | 8 nM | 24/48 h | induces apoptosis, caspase activation, and PARP cleavage co-treatment with vorinostat | 24801128 |
| Jurkat | Growth Inhibition Assay | 1-11nM | 48 h | inhibits the cell proliferation co-treatment with vorinostat | 24801128 |
| U2932 | Apoptosis Asssay | 2.5–3.5 nM | 48 h | enhances the cell death co-treatment with ACY1215 | 25239935 |
| SUDHL14 | Apoptosis Asssay | 2.5–3.5 nM | 48 h | enhances the cell death co-treatment with ACY1215 | 25239935 |
| SUDHL16 | Apoptosis Asssay | 2.5–3.5 nM | 48 h | enhances the cell death co-treatment with ACY1215 | 25239935 |
| NCI-H929 | Growth Inhibition Assay | 0-100 nM | 48 h | IC50 = 14 nM | 25312543 |
| MM.1S | Growth Inhibition Assay | 0-100 nM | 48 h | IC50 = 10 nM | 25312543 |
| SUDHL16 | Apoptosis Asssay | 2.0-4.0 nM | 48 h | induces cell death co-treatment with obatoclax | 22411899 |
| SUDHL16 | Function Assay | 2.5 nM | 24 h | activates JNK, inactivates AKT, up-regulates Noxa, and induces γH2A.X co-treatment with obatoclax | 22411899 |
| Granta | Growth Inhibition Assay | 0-4 nM | 48 h | induce cell death co-treatment with HADCIs | 21750224 |
| SUDHL16 | Growth Inhibition Assay | 1-4 nM | 36 h | induce cell death co-treatment with HADCIs | 20233973 |
| MCF7 | Function assay | 35 nM | 4 hrs | Inhibition of 26S proteasome in human MCF7 cells assessed as accumulation of high molecular weight polyubiquitin-conjugated proteins at 35 nM after 4 hrs by Western blot analysis | 27994734 |
| MDA-MB-468 | Function assay | 35 nM | 4 hrs | Inhibition of 26S proteasome in human MDA-MB-468 cells assessed as accumulation of high molecular weight polyubiquitin-conjugated proteins at 35 nM after 4 hrs by Western blot analysis | 27994734 |
| MOLT4 | Function assay | 1 hr | Inhibition of chymotrypsin-like activity of 20S proteasome in human MOLT4 cells after 1 hr by CellTiter-Glo luminescent assay, IC50 = 0.0051 μM. | 19348473 | |
| MESSA | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay, IC50 = 0.018 μM. | 19348473 | |
| MESSA | Cytotoxicity assay | 72 hrs | Cytotoxicity against multidrug resistance transporter expressing doxorubicin resistant human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay, IC50 = 0.413 μM. | 19348473 | |
| RPMI8226 | Cytotoxicity assay | 72 hrs | Cytotoxic activity against human RPMI8226 cells after 72 hrs by MTS assay, IC50 = 0.01319 μM. | 24767818 | |
| NCI-H929 | Cytotoxicity assay | 72 hrs | Cytotoxic activity against human NCI-H929 cells after 72 hrs by MTS assay, IC50 = 0.02132 μM. | 24767818 | |
| CCRF-CEM | Antiproliferative assay | 72 hrs | Antiproliferative activity against human CCRF-CEM cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0061 μM. | 26231162 | |
| RPMI8266 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human RPMI8266 cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0139 μM. | 26231162 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0193 μM. | 26231162 | |
| A431 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A431 cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0238 μM. | 26231162 | |
| TOV21G | Antiproliferative assay | 72 hrs | Antiproliferative activity against human TOV21G cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0238 μM. | 26231162 | |
| RKO | Antiproliferative assay | 72 hrs | Antiproliferative activity against human RKO cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0271 μM. | 26231162 | |
| MM1S | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MM1S cells measured after 72 hrs by MTS assay, IC50 = 0.0015 μM. | 27765408 | |
| RPMI8226 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human RPMI8226 cells measured after 72 hrs by MTS assay, IC50 = 0.0132 μM. | 27765408 | |
| LCL | Cytotoxicity assay | 48 hrs | Cytotoxicity against human LCL cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.03 μM. | 27994734 | |
| RD-ES | Cytotoxicity assay | 48 hrs | Cytotoxicity against human RD-ES cells harboring p53 mutant assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.043 μM. | 27994734 | |
| U266 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human U266 cells harboring mutant p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.06 μM. | 27994734 | |
| WE68 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human WE68 cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.08 μM. | 27994734 | |
| IMR90 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human IMR90 cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.13 μM. | 27994734 | |
| MCF10A | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF10A cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.32 μM. | 27994734 | |
| SKOV3 | Cytotoxicity assay | 48 hrs | Cytotoxicity against p53 deficient human SKOV3 cells assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.32 μM. | 27994734 | |
| MDA-MB-468 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-468 cells harboring mutant p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.33 μM. | 27994734 | |
| HNDF | Cytotoxicity assay | 48 hrs | Cytotoxicity against HNDF cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.35 μM. | 27994734 | |
| KGN | Cytotoxicity assay | 48 hrs | Cytotoxicity against human KGN cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.45 μM. | 27994734 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 4.5 μM. | 27994734 | |
| MM1S | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MM1S cells measured after 72 hrs by MTS assay, IC50 = 0.0015 μM. | 28027531 | |
| RPMI8226 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human RPMI8226 cells measured after 72 hrs by MTS assay, IC50 = 0.0132 μM. | 28027531 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.0041 μM. | 30165344 | |
| MDA-MB-231 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 0.0044 μM. | 30165344 | |
| RPMI8226 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human RPMI8226 cells after 48 hrs by MTT assay, IC50 = 0.0067 μM. | 30165344 | |
| UMSCC-22A | Growth Inhibition Assay | IC50=38.7 ± 1.0 nM | 22929803 | ||
| R-Cal33 | Growth Inhibition Assay | IC50=1112 nM | 24915039 | ||
| P-Cal33 | Growth Inhibition Assay | IC50=17.3 nM | 24915039 | ||
| R-UMSCC-1 | Growth Inhibition Assay | IC50=2294 nM | 24915039 | ||
| P-UMSCC-1 | Growth Inhibition Assay | IC50=11.2 nM | 24915039 | ||
| UMSCC-22B | Growth Inhibition Assay | IC50=30.7 ± 9.3 nM | 22929803 | ||
| 1483 | Growth Inhibition Assay | IC50=50.5 ± 11.9 nM | 22929803 | ||
| UMSCC-1 | Growth Inhibition Assay | IC50=34.6 ± 2.6 nM | 22929803 | ||
| Cal33 | Growth Inhibition Assay | IC50=49.3 ± 8.9 nM | 22929803 | ||
| PCI-15A | Growth Inhibition Assay | IC50=70.4 ± 22.6 nM | 22929803 | ||
| PCI-15B | Growth Inhibition Assay | IC50=39.5 ± 11.0 nM | 22929803 | ||
| OSC-19 | Growth Inhibition Assay | IC50=18.3 ± 4.2 nM | 22929803 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| 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-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH 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 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 29435139 | ||
| fibroblast cells | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 29435139 | ||
| fibroblast cells | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells | 29435139 | ||
| Daoy | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for Daoy cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D caspase screen for TC32 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for TC32 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for MG 63 (6-TG R) 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 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for RD cells | 29435139 | ||
| ANBL-6 | Function assay | Inhibition of 20S proteasome activity in human ANBL-6 cells, IC50 = 0.01 μM. | 29652143 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Carfilzomib (PR-171) 是一种不可逆proteasome抑制剂，在ANBL-6细胞中IC50为<5 nM，在体外优先抑制β5亚基的ChT-L活性，对PGPH和T-L活性很弱或没有作用。Carfilzomib 可激活自噬并诱导细胞凋亡。 | ||
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| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Carfilzomib抑制多种细胞系和源自患者的肿瘤细胞的增殖，包括多发性骨髓瘤。Carfilzomib诱导内在和外在的凋亡信号传导途径并激活c-Jun N-末端激酶(JNK)。Carfilzomib协同地塞米松(Dex)表现增强的抗MM活性，并克服了药物的抗性。 Carfilzomib有选择地抑制β5亚基的CHT- L活性，在10 nM剂量时抑制超过80％的活性。低剂量Carfilzomib短期处理导致优先结合特异性的β5组成20S蛋白酶体和β5i免疫蛋白酶体亚基。在Carfilzomib刺激的ANBL -6细胞中检测caspase活性，结果显示caspase- 8和caspase -9和caspase-3活性在8小时后大幅增加，和对照8小时后的细胞相比分别增加了3.2 ， 3.9和6.9倍。在carfilzomib处理过的细胞中，线粒体膜的完整性减少到41%(Q1 + Q2)，而在对照细胞中这一比例为75％。[1] 在另一项研究中，Carfilzomib也表现出对血液和实体肿瘤的临床前有效性。[2] Carfilzomib直接一直破骨形成和骨吸收。[3] |
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| 激酶实验 | 酶联免疫吸附试验分析carfilzomib亚基 | |||
| ANBL -6细胞（2 ×106/孔）接种于96孔板中并用Carfilzomib（0.001至10μM）处理 1小时。然后将细胞裂解（20mM的Tris-HCl， 0.5 mM EDTA），并裂解物上清转移到聚合酶链反应（PCR）平板上。使用起始浓度为6 μg/μL处理ANBL - 6细胞得到的裂解物做标准曲线。活性位点探针[生物素-(CH2)4-Leu-Leu-Leu-环氧酮; 20 μM]加入并于室温温育1小时。在细胞裂解液中添加1％十二烷基硫酸钠（SDS）和加热至100℃变性 ，随后在96孔的多屏DV板中每孔和20μL链霉亲和琼脂糖高性能珠混合并孵育1小时。这些珠粒用酶联免疫吸附试验(ELISA)缓冲液（PBS，1％牛血清白蛋白和0.1 ％吐温-20）洗涤细胞，并温育过夜，在4℃在板振荡器上与抗体的蛋白酶体亚基反应。所用抗体包括鼠单克隆抗- β1 ，抗-β2 ，抗β1i和抗β5i ，山羊多克隆抗β2i ，和兔多克隆抗- β5 （针对KLH- CWIRVSSDNVADLHDKYS肽亲和纯化的抗血清）。珠粒洗涤后用以辣根过氧化物酶标记的二羊抗兔，羊抗鼠或兔antigoat抗体温育2小时。洗涤后，将珠粒用SuperSignal ELISA picochemiluminescence底物反应，而后进行荧光检测。荧光信号通过与标准曲线比较转换为μg/mL，表示为抑制相对于对照的％。使用以下nonsigmoidal剂量 - 反应方程生成拟合曲线：Y = Bottom + (Top-Bottom)/(1 + 10̂((LogEC50 − X) × HillSlope))，其中X是浓度的对数， Y是抑制％，EC 50是表示50％的效果的剂量。 | ||||
| 细胞实验 | 细胞系 | WST-1, ANBL-6细胞 | ||
| 浓度 | 100 nM | |||
| 孵育时间 | 1小时 | |||
| 方法 | WST-1被用于确定蛋白酶体抑制剂Carfilzomib对细胞增殖的影响。增殖的抑制作用是与对照细胞比较所得。线性样条函数是用来使用XLfit4软件进行计算半数抑制浓度（IC50）。抗性程度(DOR)的计算公式是IC50（抗性细胞）/ IC50（敏感细胞）。 ANBL-6细胞用100nM carfilzomib短暂处理，洗涤并悬浮于含有5μg/mL JC-1PBS中，它显示出在线粒体电位依赖性积聚。用FACScan分析线粒体膜电位依赖性颜色转变（从525到590 nM），数据用CellQuest软件分析。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | pERK / ERK / pSTAT5 / STAT5 / pPI3K / PI3K caspase-9 / caspase-8 c-PARP / PARP / caspase-3 Bcl-2 / Bcl-Xl / Mcl-1 / Bik / Bim / Bax / Bak Atg5 / Atg12 / Beclin-1 / LC3-II Noxa / Bik / Puma / Mcl-1 EGFR / HER2 / ER alpha / p-Akt(Ser473) / Akt / p-ERK / ERK / p53 BDP1 / HER2(Tyr1248) / HER2(Tyr1221/Tyr1222) / PARP1 / caspase-7 / p53 Mut HLA class I |
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24590311 | |
| Growth inhibition assay | Cell viability |
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27655642 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Carfilzomib适度降低了体内异种移植物模型中肿瘤的生长。在持续或短暂处理下， Carfilzomib有效地降低多发性骨髓瘤细胞活力。 Carfilzomib增加骨小梁体积，减少骨吸收，并提高非肿瘤小鼠的骨形成。[3] |
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| 动物实验 | Animal Models | Beige-nude-XID小鼠 |
| Dosages | 2.0 mg/kg | |
| Administration | 静脉注射 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05552976 | Recruiting | Relapsed or Refractory Multiple Myeloma |
Bristol-Myers Squibb |
January 10 2023 | Phase 3 |
| NCT05675449 | Recruiting | Multiple Myeloma |
Pfizer |
December 14 2022 | Phase 1 |
| NCT05041933 | Unknown status | Hematological Diseases |
University Hospital Limoges |
September 15 2021 | -- |
化学信息&溶解度
| 分子量 | 719.91 | 分子式 | C40H57N5O7 |
| CAS号 | 868540-17-4 | SDF | Download Carfilzomib (PR-171) SDF |
| Smiles | CC(C)CC(C(=O)C1(CO1)C)NC(=O)C(CC2=CC=CC=C2)NC(=O)C(CC(C)C)NC(=O)C(CCC3=CC=CC=C3)NC(=O)CN4CCOCC4 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 100 mg/mL ( (138.9 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 50 mg/mL (69.45 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解配方 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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常见问题及建议解决方法
问题 1:
How should I prepare solution of Carfilzomib for ongoing in vivo study?
回答：
This compound can be dissolved in 2% DMSO/30% PEG 300/dd H2O at 10 mg/ml as a suspension, and can be dissolved in 2% DMSO/ castor oil at 10 mg/ml as a clear solution.
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