Chiauranib | Multikinase inhibitor | Probechem Biochemicals

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.

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10 mg	￥2480	In stock
25 mg	￥3980	In stock
50 mg	￥5980	In stock
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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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