| Identification | Back Directory | [Name]
7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide | [CAS]
1633350-06-7 | [Synonyms]
BGB-3111
EOS-61237
BGB3111; BGB 3111
Zanubrutinib Racemate
(±)Zanubrutinib,(±) Zanubrutinib
7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide
Pyrazolo[1,5-a]pyrimidine-3-carboxamide, 4,5,6,7-tetrahydro-7-[1-(1-oxo-2-propen-1-yl)-4-piperidinyl]-2-(4-phenoxyphenyl)- | [Molecular Formula]
C27H29N5O3 | [MDL Number]
MFCD30738015 | [MOL File]
1633350-06-7.mol | [Molecular Weight]
471.55 |
| Chemical Properties | Back Directory | [Boiling point ]
713.4±60.0 °C(Predicted) | [density ]
1.33±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : ≥ 30 mg/mL (63.62 mM);Ethanol : ≥ 10 mg/mL (21.21 mM) | [form ]
Solid | [pka]
15.35±0.40(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
(±)-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 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]. | [References]
[1] Na L, et al. BGB-3111 is a novel and highly selective Bruton's tyrosine kinase (BTK) inhibitor. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 2597. doi:10.1158/1538-7445.AM2015-2597 |
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