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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-p21-activated Kinase (PAK)-KPT-9274
KPT-9274

Chemical Structure : KPT-9274

CAS No.: 1643913-93-2

KPT-9274 (KPT9274, Padnarsertib)

货号: PC-43212Not For Human Use, Lab Use Only.

KPT-9274 (Padnarsertib) is a potent, specific, dual NAMPT and PAK4 inhibitor with IC50 of 120 nM (NAMPT), also is an orally bioavailable PAK4 allosteric modulator with IC50 of 30 nM in MS-751 cell MTT assay.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

KPT-9274 (Padnarsertib) is a potent, specific, dual NAMPT and PAK4 inhibitor with IC50 of 120 nM (NAMPT), also is an orally bioavailable PAK4 allosteric modulator with IC50 of 30 nM in MS-751 cell MTT assay.
KPT-9274 (Padnarsertib) attenuates the PAK4/β-catenin pathway, results in NAD depletion, and attenuates viability, invasion, and migration in several RCC cell lines (IC50=600 nM for Caki-1 cells).
KPT-9274 (Padnarsertib) attenuates G2/M transit and induces apoptosis, shows specificity for attenuation of NAD biosynthesis targets preferentially in RCC cells.
KPT-9274 (Padnarsertib) decreases tumor growth in xenograft model of RCC.

物理化学性质&存储条件

分子量 610.625
分子式 C35H29F3N4O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 32 mg/mL

Chemical Name/SMILES

2-Propenamide, 3-(6-amino-3-pyridinyl)-N-[[5-[4-[(4,4-difluoro-1-piperidinyl)carbonyl]phenyl]-7-(4-fluorophenyl)-2-benzofuranyl]methyl]-, (2E)-

参考文献

1. Abu Aboud O, et al. Mol Cancer Ther. 2016 Sep;15(9):2119-29.

2. Aboukameel A, et al. Mol Cancer Ther. 2017 Jan;16(1):76-87.

3. Fulciniti M, et al. Blood. 2017 Apr 20;129(16):2233-2245.

4. Rane C, et al. Sci Rep. 2017 Feb 15;7:42555.

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