(±)-Zanubrutinib
CAS No. : 1633350-06-7
(Synonyms: (±)-BGB-3111)
| Size | Price | Stock |
|---|---|---|
| 5mg | $120 | In-stock |
| 10mg | $190 | In-stock |
| 50mg | $550 | In-stock |
| 100mg | $790 | In-stock |
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| Cat. No. : | HY-101474 |
| M.Wt: | 471.55 |
| Formula: | C27H29N5O3 |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 30 mg/mL;Ethanol : ≥ 10 mg/mL |
(±)-Zanubrutinib ((±)-BGB-3111) is the racemate of Zanubrutinib (HY-101474A). (±)-Zanubrutinib inhibits Bruton's tyrosine kinase (Btk) with an IC50 of 0.63 nM[1]. In Vitro:In both biochemical and cellular assays, (±)-Zanubrutinib ((±)-BGB-3111) demonstrates nanomolar Btk inhibition activity. In several MCL and DLBCL cell lines, (±)-Zanubrutinib inhibits BCR aggregation-triggered Btk autophosphorylation, blocks downstream PLC-γ2 signaling, and potently inhibits cell proliferation. In comparison with PCI-32765, (±)-Zanubrutinib shows much more restricted off-target activities against a panel of kinases, including ITK[1]. In Vivo:(±)-Zanubrutinib 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 (±)-Zanubrutinib is very well tolerated and maximal tolerate dose (MTD) is not reached when it is dosed up to 250mg/kg/day[1].
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