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Chemical Structure : BGB-8035
Catalog No.: PC-20324Not For Human Use, Lab Use Only.
BGB-8035 (BGB8035) is a potent, highly selective BTK inhibitor with IC50 of 1.1 nM, potently inhibits BTK Tyr223 phosphorylation in BTK pY223 cellular assays with IC50 of 13.9 nM.
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BGB-8035 (BGB8035) is a potent, highly selective BTK inhibitor with IC50 of 1.1 nM, potently inhibits BTK Tyr223 phosphorylation in BTK pY223 cellular assays with IC50 of 13.9 nM.
BGB-8035 shows IC50 of 10.4 nM in Rec-1-cell viability assays.
BGB-8035 is quite clean in the Cerep panel, and against a panel of 369 human kinases was evaluated displays < 70% inhibition against 359 kinases and>70% inhibition against 10 kinases, including BTK, a panel of 369 human kinases at 2 uM.
BGB-8035 (7.5 mg/kg BID) showed similar activity as ibrutinib at 50 mg/kg QD in the REC-1 xenograft model, showed tuomor growth inhibition.
BGB-8035 (10 mg/kg BID, oral) prevented the CIA model-associated body weight, induced dose-dependent inhibition of paw swelling in the collagen antibody-induced arthritis (CAIA) mouse model.
| M.Wt | 453.54 | |
| Formula | C24H31N5O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Yunhang Guo, et al. J Med Chem. 2023 Mar 23;66(6):4025-4044.
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