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| Cas No.: | 1633350-06-7 |
| Synonyms: | BGB3111; BGB 3111 |
| SMILES: | NC(C1=C2N(N=C1C3=CC=C(OC4=CC=CC=C4)C=C3)C(C5CCN(C(C=C)=O)CC5)CCN2)=O |
| Formula: | C27H29N5O3 |
| M.Wt: | 471.55 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | In both biochemical and cellular assays, BGB-3111 demonstrates nanomolar Btk inhibition activity. In several MCL and DLBCL cell lines, BGB-3111 inhibits BCR aggregation-triggered Btk autophosphorylation, blocks downstream PLC-γ2 signaling, and potently inhibits cell proliferation. In comparison with ibrutinib, BGB-3111 shows much more restricted off-target activities against a panel of kinases, including ITK. BGB-3111 is at least 10-fold weaker than ibrutinib in inhibiting rituximab induced ADCC, consistent with its weak ITK inhibition activity.BGB-3111 induces dose-dependent anti-tumor effects against REC-1 MCL xenografts engrafted either subcutaneously or systemically via tail vein injection in mice. In the subcutaneous xenografts. Preliminary 14-day toxicity study in rats shows that BGB-3111 is very well tolerated and maximal tolerate dose (MTD) is not reached when it is dosed up to 250mg/kg/day. |