INCB053914 phosphate

Chemical Structure : INCB053914 phosphate

CAS No.: 2088852-47-3

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货号: PC-22079Not For Human Use, Lab Use Only.

INCB053914 (Uzansertib) phosphate is a novel potent, and selective ATP-competitive, pan-PIM kinase inhibitor with IC50 of 0.24/30.0/0.12 nM for PIM1/2/3, respectively.

规格	价格	库存
5 mg	￥2880	In stock
10 mg	￥4780	In stock
25 mg	￥7980	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

INCB053914 (Uzansertib) phosphate is a novel potent, and selective ATP-competitive, pan-PIM kinase inhibitor with IC50 of 0.24/30.0/0.12 nM for PIM1/2/3, respectively.
INCB053914 is highly selective against a panel of more than 50 kinases (>475-fold selectivity) with exception of RSK2 (IC50=7.1 uM).
INCB053914 inhibits cellular proliferation in a panel of cell lines derived from hematologic malignancies including AML, MM, DLBCL, MCL, and T-ALL with GI50 of <100 nM, inhibits proliferation in all MM cell lines with GI5050 of 13.2-230.0 nM.
INCB053914 inhibits PIM kinase-mediated phosphorylation of BAD in MOLM-16 and KMS-12-BM cells with IC50 of 4 and 27 nM, also increases PIM2 expression in KG-1a (AML), Pfeiffer, and KMS12-PE cells.
INCB053914 inhibits Bcl-2-associated death promoter protein phosphorylation and dose-dependently inhibited tumor growth in acute myeloid leukemia and multiple myeloma xenografts.

物理化学性质&存储条件

分子量	611.51
分子式	C26H29F3N5O7P
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	10 mM in DMSO
Chemical Name/SMILES	2-Pyridinecarboxamide, N-[(7R)-4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methyl-1-piperidinyl]-6,7-dihydro-7-hydroxy-5H-cyclopenta[b]pyridin-3-yl]-6-(2,6-difluorophenyl)-5-fluoro-, phosphate (1:1)

参考文献

1. Koblish H, et al. PLoS One. 2018 Jun 21;13(6):e0199108.