货号:A140158 同义名: KPT-330;ATG-010
KPT-330, analog of KPT-185, is an orally bioavailable selective CRM1 inhibitor.
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产品名称 | CRM1 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
KPT-185 | ✔ | 98+% | |||||||||||||||||
Verdinexor | ✔ | 99%+ | |||||||||||||||||
KPT-276 | ✔ | 99%+ | |||||||||||||||||
Selinexor | ✔ | 99%+ | |||||||||||||||||
Piperlongumine | ✔ | 99%+ | |||||||||||||||||
Eltanexor | ✔ | 99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
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描述 | Chromosome region maintenance 1 (CRM1) is a major nuclear export receptor that mediates the transport of proteins and mRNAs. KPT-330 is a selective inhibitor of CRM1 which shows cytotoxic activity with a median IC50 value of 123 nM in a characterized cell penal with 23 cell lines[1]. In both STO and MesoII cells, the treatment of 1 μM KPT-330 markedly increased the accumulation of G1phase at 48 hours after the exposure, and reached a maximum at 72 hours. STO cells demonstrated a high sensitivity to KPT-330 with an IC50 of 0.7 μM, whereas MesoII cells with IC50 of 0.35 μM[2]. KPT-330 at the concentration between 0.1 μM–1 μM induced growth inhibition dose-dependently in eleven NSCLC cell lines. KPT-330 at 1 μM also stimulated the activation of caspase-3 and caspase-9, as well as the protein levels of several pro-apoptotic mediators, including Bax, Bim, and Puma in NSCLC cells. When evaluating the tumor volume of H1975 NSCLC cells engrafted in NOD/SCID mice, KPT-330 treatment (10 mg/kg, twice weekly for 4 weeks) markedly inhibited tumor growth compared with vehicle-treated controls[3]. |
作用机制 | KPT-330 inactivates CRM1 by modifying the critical CRM1-binding residue, thereby irreversibly inhibiting CRM1-mediated nuclear export of proteins and mRNAs[4]. |
Dose | Rat[5]: 0.25 mg/kg - 10 mg/kg (p.o.), 5 mg/kg(i.v.) Monkey[5]: 0.1 mg/kg - 1 mg/kg (p.o.), 2 mg/kg(i.v.) Mice: 3 mg/kg - 30 mg/kg[6] (p.o.) |
Administration | p.o., i.v. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.26mL 0.45mL 0.23mL |
11.28mL 2.26mL 1.13mL |
22.56mL 4.51mL 2.26mL |
CAS号 | 1393477-72-9 |
分子式 | C17H11F6N7O |
分子量 | 443.306 |
别名 | KPT-330;ATG-010 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,2-8°C |
溶解度 |
DMSO: 50 mg/mL(112.79 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |
IP 2% DMSO+2% Tween80+40% PEG300+water 13 mg/mL clear PO 0.5% CMC-Na 30 mg/mL suspension |