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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Metabolic Enzyme & Protease > CarfilzomibCAS：868540-17-4
Molecular Formula：C40H57N5O7
Molecular Weight：719.91
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 868540-17-4 |
| Name | Carfilzomib |
| Molecular Formula | C40H57N5O7 |
| Molecular Weight | 719.91 |
| Solubility | Soluble in DMSO |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 692-054-2 |
| MDL | MFCD11040997 |
| SMILES | C[C@@]1(C([C@H](CC(C)C)NC([C@@H](NC([C@H](CC(C)C)NC([C@@H](NC(CN2CCOCC2)=O)CCC3=CC=CC=C3)=O)=O)CC4=CC=CC=C4)=O)=O)OC1 |
| InChIKey | BLMPQMFVWMYDKT-NZTKNTHTSA-N |
| InChI | InChI=1S/C40H57N5O7/c1-27(2)22-32(36(47)40(5)26-52-40)42-39(50)34(24-30-14-10-7-11-15-30)44-38(49)33(23-28(3)4)43-37(48)31(17-16-29-12-8-6-9-13-29)41-35(46)25-45-18-20-51-21-19-45/h6-15,27-28,31-34H,16-26H2,1-5H3,(H,41,46)(H,42,50)(H,43,48)(H,44,49)/t31-,32-,33-,34-,40+/m0/s1 |
| PubChem CID | 11556711 |
| Target Point | Proteasome |
| Passage | Metabolic Enzyme&Protease |
| Background | Carfilzomib is an irreversible proteasome inhibitor. |
| Biological Activity | Carfilzomib是不可逆的蛋白酶体 (proteasome) 抑制剂，其在ANBL-6和RPMI 8226细胞中的 IC50 为5 nM。[1-2] |
| In Vitro | 卡非佐米显示出对β5亚基中ChT-L活性的优先体外抑制效力，在10nM及以上的剂量下具有超过80％的抑制，并且在高达100nM的剂量下对PGPH和TL活性的影响很小或没有影响。 Carfilzomib降低了ANBL-6，RPMI 8226细胞，U266和KAS-6/1细胞的活力，IC50小于5 nM。 Carfilzomib克服了Dex抗性，因为MM1.R细胞显示IC50为15.2 nM，低于亲本MM1.S细胞的29.3 nM [1]。与卡非佐米和HDACI共处理导致在各种套细胞淋巴瘤细胞系和原代套细胞淋巴瘤细胞中协同诱导细胞死亡。卡非佐米或ONX0912与伏立诺他在HF-4B和Granta细胞中联合治疗可显著增加caspase激活，PARP裂解，JNK激活，MnSOD2诱导和DNA损伤[2]。 |
| In Vivo | 与70mg/kg伏立诺他合并的卡非佐米(2.0mg/kg，iv)实际上消除了格兰 - 荧光素细胞异种移植物侧翼模型中的肿瘤生长。与用单一药剂或对照治疗的动物相比，联合治疗导致生物发光显著减少，毒性最小[2]。 |
| Cell Experiment | WST-1用于根据制造商的方案确定蛋白酶体抑制剂对细胞增殖的影响。对于单独接受载体并在KaleidaGraph 3.0.1或Excel 2000中制表的平行对照细胞计算增殖抑制。使用XLfit 4软件使用线性样条函数内插中值抑制浓度(IC 50)。使用下式计算电阻度(DOR)：DOR = IC50(抗性细胞)/ IC50(敏感细胞)。 |
| Animal Experiment | 使用Beige-nude-XID小鼠进行动物研究。沉淀10×106个Granta514细胞，用1X PBS洗涤两次，皮下注射到右侧腹侧。一旦肿瘤可见，用卡非佐米±伏立诺他治疗5至6只小鼠，并监测肿瘤生长或消退的进展。将伏立诺他和卡非佐米原液分别溶于10mM柠檬酸盐缓冲液pH的DMSO和10％磺基丁基醚β-环糊精中。将它们以小等分试样储存在-80℃下并在注射前稀释。 |
| Data Literature Source | [1]. Kuhn DJ，et al. Potent activity of carfilzomib，a novel，irreversible inhibitor of the ubiquitin-proteasome pathway，against preclinical models of multiple myeloma. Blood. 2007 Nov 1;110(9):3281-90. [2]. Dasmahapatra G，et al. Carfilzomib interacts synergistically with histone deacetylase inhibitors in mantle cell lymphoma cells in vitro and in vivo. Mol Cancer Ther. 2011 Sep;10(9):1686-97. |
| Unit | Bottle |
| Specification | 5mg 10mg 20mg |
Carfilzomib是不可逆的蛋白酶体 (proteasome) 抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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