BLU2864 | PRKACA inhibitor | Probechem Biochemicals

Chemical Structure : BLU2864

CAS No.: 2810747-89-6

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BLU2864 (BLU-2864)

货号: PC-26712Not For Human Use, Lab Use Only.

BLU2864 is a potent, selective and orally acitve protein kinase A (PKA) alpha catalytic subunit (PRKACA) inhibitor with IC50 of 0.3 nM and Kd of 3.3 nM.

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5 mg	￥1380	In stock
10 mg	￥2180	In stock
25 mg	￥3780	In stock
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100 mg		Get quote

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生物&药学活性

BLU2864 is a potent, selective and orally acitve protein kinase A (PKA) alpha catalytic subunit (PRKACA) inhibitor with IC50 of 0.3 nM and Kd of 3.3 nM.
BLU2864 exhibits good to moderate selectivity against closely related AGC kinase family members and excellent overall kinome selectivity profiles.
BLU2864 exhibits cellular IC50 value of 36.6 nM for inhibition of VASP Ser157 phosphorylation in forskolin-stimulated Huh7 cells.
BLU2864 treatment led to a dose-dependent reduction in phosphorylated VASP in FLC PDX spheroid cultures.
BLU2864 at 30 mg/kg once daily (QD) inhibits PRKACA in vivo, inhibits tumor growth in mice harboring FLC PDX tumors.

物理化学性质&存储条件

分子量	452.43
分子式	C24H19F3N4O2
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-((1R,2S)-5-(difluoromethyl)-7-fluoro-2-hydroxy-2,3-dihydro-1H-inden-1-yl)-6-(3-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)nicotinamide

参考文献

1. Schalm SS, et al. Gastro Hep Adv. 2022 Nov 8;2(3):307-321.

2. Stefanie S. Schalm, et al. bioRxiv 2022.01.31.477690.

BLU2864 (BLU-2864)

生物&药学活性

物理化学性质&存储条件

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BLU2864 (BLU-2864)

生物&药学活性

物理化学性质&存储条件

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