PF-06939999 | PRMT5 inhibitor | Probechem Biochemicals

Chemical Structure : PF-06939999

CAS No.: 2159123-14-3

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PF-06939999 (PF06939999)

货号: PC-72513Not For Human Use, Lab Use Only.

PF-06939999 (PF06939999) is a potent, selective, S-adenosylmethionine (SAM) competitive PRMT5 inhibitor with SPR Kd of 5.8 pM.

规格	价格	库存
2 mg	￥1880	In stock
5 mg	￥2980	In stock
10 mg	￥4780	In stock
25 mg		Get quote
100 mg		Get quote

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生物&药学活性

PF-06939999 (PF06939999) is a potent, selective, S-adenosylmethionine (SAM) competitive PRMT5 inhibitor with SPR Kd of 5.8 pM.
PF-06939999 displays at least one million-fold selective for PRMT5 over a panel of protein methyltransferases and 20 diverse protein kinases.
PF-06939999 demonstrates dose-dependent reduction of symmetric dimethyl arginine (SDMA) and an antiproliferative response in A2780 cells (IC50=3.3 nM).
PF-06939999 showed dose-dependent loss of SDMA on several proteins, with a cellular IC50 1.1 nM in A427 cells.
PF-06939999 demonstrates tumor growth inhibition in splicing mutant NSCLC (oral 3, 10, and 30 mg/kg).

物理化学性质&存储条件

分子量	448.446
分子式	C22H23F3N4O3
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	(1S,2S,5R)-3-((6-(difluoromethyl)-5-fluoro-1,2,3,4-tetrahydroisoquinolin-8-yl)oxy)-5-(4-methyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclopentane-1,2-diol

参考文献

1. Kristen Jensen-Pergakes, et al. Mol Cancer Ther. 2022 Jan;21(1):3-15.

PF-06939999 (PF06939999)

生物&药学活性

物理化学性质&存储条件

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PF-06939999 (PF06939999)

生物&药学活性

物理化学性质&存储条件

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