PIM-Kinase Inhibitor X, CX-6258 - Calbiochem

PIM-Kinase Inhibitor X, CX-6258 - Calbiochem 구조식 이미지
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PIM-Kinase Inhibitor X, CX-6258 - Calbiochem
동의어(영문):
PIM-Kinase Inhibitor X, CX-6258 - Calbiochem
CBNumber:
CB84817772
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0
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Mol file

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PIM-Kinase Inhibitor X, CX-6258 - Calbiochem C화학적 특성, 용도, 생산

일반 설명

An orally bioavailable oxindolo-furanyl compound that acts as a potent, reversible and ATP-competitive inhibitor of pan PIM-kinases (IC50 = 5, 25 and 16 nM for PIM-1, PIM-2 and PIM-3, respectively; Ki = 5 nM for PIM-1) with excellent selectivity over 107 kinases (IC80 >500 nM). Shown to arrest the proliferation of several human cancer cells (IC50 = 20 and 452 nM for MV-4-11 and PC3 cells) and block phosphorylation of Bad-Ser112, 4E-BP1-Ser65 and Thr37/46 with an IC50 of ~ 1.0 μM. Displays favorable pharmacokinetic profile and efficacy in mice, and suppresses tumor growth in MV-4-11 and PC3 xenograft murine model (50 mg/kg, p.o.). Further, potentiates doxorubicin (Cat. No. 324380) and paclitaxel (Cat. No. 580555) toxicity in PC3 cells.

Biochem/physiol Actions

Cell permeable: yes

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PIM-Kinase Inhibitor X, CX-6258 - Calbiochem 공급 업체

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공급자 전화 이메일 국가 제품 수 이점
Sigma-Aldrich 021-61415566 800-8193336
orderCN@merckgroup.com China 51471 80

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