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Chemical Structure : ARQ-531
CAS No.: 2095393-15-8
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $198 | In stock | |
| 25 mg | $328 | In stock | |
| 50 mg | $528 | In stock | |
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| 200 mg | Get quote | ||
| 1 g | Get quote |
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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.
| M.Wt | 478.933 | |
| Formula | C25H23ClN4O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Reiff SD, et al. Cancer Discov. 2018 Aug 9. pii: CD-17-1409. doi: 10.1158/2159-8290.CD-17-1409.
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