Chiauranib (Ibcasertib, CS2164) | Multikinase inhibitor

Chemical Structure : Chiauranib

CAS No.: 1256349-48-0

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Chiauranib (Ibcasertib, CS2164, CS-2164)

货号: PC-20795Not For Human Use, Lab Use Only.

Chiauranib (Ibcasertib, CS2164) is a potent multi-kinase inhibitor, inhibits VEGFR2, Aurora B and CSF-1R kinases with IC50 values of 7, 9 and 7 nM, respectively.

规格	价格	库存
5 mg	￥1280	In stock
10 mg	￥1980	In stock
25 mg	￥3480	In stock
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100 mg		Get quote

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生物&药学活性

Chiauranib (Ibcasertib, CS2164) is a potent multi-kinase inhibitor, inhibits VEGFR2, Aurora B and CSF-1R kinases with IC50 values of 7, 9 and 7 nM, respectively.
CS2164 interacts with each active ATP-binding pocket of VEGFR2, Aurora B and CSF-1R kinases, respectively.
CS2164 also displays inhibitory activities with single digital nanomolar IC50 against several angiogenesis-related kinases, including VEGFR1, VEGFR3, PDGFRα and c-Kit.
CS2164 only shows moderate inhibitory activities (100 nM < IC50 < 500 nM) in 4 kinases (c-RAF, DDR2, PLK1 and PLK3), little activity (IC50 > 500 nM) in 33 kinases, and almost no activity (IC50 > 10 μM) in over 120 kinases, including 76 GPCR and 8 ion channels tested.
CS2164 potently inhibits VEGF-induced proliferation of HUVEC cells and PDGF‐induced proliferation of NIH-3T3 cells with GI50 values of 20.70 and 44.16 nM, respectively.
CS2164 is a potent inhibitor of tumor angiogenesis through targeting the corresponding tyrosine receptor signaling pathways, induces G2/M cell cycle arrest by inhibition of Aurora B/p-H3.
CS2164 inhibits CSF-1R signaling and reduces tissue CSF-1R expression.
CS2164 exhibits broad and potent in vivo anti-tumor activities, CS2164 (40 mg/kg) induces dose-dependent inhibition of tumor growth in human non‐small cell lung cancer cell line A549-derived xenograft model.

物理化学性质&存储条件

分子量	435.48
分子式	C27H21N3O3
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	N-(2-aminophenyl)-6-[(7-methoxy-4-quinolinyl)oxy]-1-naphthalenecarboxamide

参考文献

1. Zhou Y, et al. Cancer Sci. 2017 Mar;108(3):469-477.

Chiauranib (Ibcasertib, CS2164, CS-2164)

生物&药学活性

物理化学性质&存储条件

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Chiauranib (Ibcasertib, CS2164, CS-2164)

生物&药学活性

物理化学性质&存储条件

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