ARQ-531 |CAS:2095393-15-8 Probechem Biochemicals

Chemical Structure : ARQ-531

CAS No.: 2095393-15-8

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ARQ-531 (Nemtabrutinib, ARQ531)

货号: PC-35328Not For Human Use, Lab Use Only.

Nemtabrutinib (ARQ531) is a potent, reversible, orally available inhibitor of both wild type and C481S-mutant BTK kinase with IC50 of 0.85 and 0.39 nM, respectively.

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10 mg	￥1980	In stock
25 mg	￥3280	In stock
50 mg	￥5280	In stock
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1 g		Get quote

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生物&药学活性

Nemtabrutinib (ARQ531) is a potent, reversible, orally available inhibitor of both wild type and C481S-mutant BTK kinase with IC50 of 0.85 and 0.39 nM, respectively.
ARQ531 also ptently inhibits 45 kinases with >50% inhibition at 200 nM (TEC, BMX, LCK, TRK family kinases etc.).
ARQ531 does not require the C481S residue to bind to BTK, inhibits CD69 expression on CD20+ B-cells with IC50 of 42 nM (Ibrutinib, IC50=3 nM).
ARQ531 inhibits proliferation of malignant cells both sensitive and resistant to ibrutinib (SUDHL6 Cell GI50=80 nM).
ARQ 531 is superior to Ibrutinib in a TCL1 highly predictive adoptive transfer model of CLL.

物理化学性质&存储条件

分子量	478.933
分子式	C25H23ClN4O4
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-chloro-4-phenoxyphenyl)(4-(((3R,6S)-6-(hydroxymethyl)tetrahydro-2H-pyran-3-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)methanone

参考文献

1. Reiff SD, et al. Cancer Discov. 2018 Aug 9. pii: CD-17-1409. doi: 10.1158/2159-8290.CD-17-1409.

ARQ-531 (Nemtabrutinib, ARQ531)

生物&药学活性

物理化学性质&存储条件

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ARQ-531 (Nemtabrutinib, ARQ531)

生物&药学活性

物理化学性质&存储条件

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