racemic-Zanubrutinib-racemic-BGB-3111-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemE()-ZanubrutinibCat. No.: HY-101474CAS No.: 1633350-06-7Synonyms: ()-BGB-3111分式: CHNO分量: 471.55作靶點: Btk作通路: Protein Tyrosine Kinase/RTK儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 30 mg/m

2、L (63.62 mM)Ethanol : 10 mg/mL (21.21 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.1207 mL 10.6033 mL 21.2067 mL5 mM 0.4241 mL 2.1207 mL 4.2413 mL10 mM 0.2121 mL 1.0603 mL 2.1207 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙?/p>

3、案，配制前請先配制澄清的儲備液，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.30 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small Molecules 您邊的抑制劑師www.MedC

4、hemESolubility: 2.5 mg/mL (5.30 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.30 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 ()-Zanubrutinib種有效的選擇性 Brutons 酪氨酸激酶 (Btk) 抑制劑。體外研究 In both biochemical and cellular assays, ()-Zanubrutinib demonstrates nanomolar Btk inhibiti

5、on activity. Inseveral MCL and DLBCL cell lines, ()-Zanubrutinib inhibits BCR aggregation-triggered Btkautophosphorylation, blocks downstream PLC-2 signaling, and potently inhibits cell proliferation. Incomparison with ibrutinib, ()-Zanubrutinib shows much more restricted off-target activities again

6、st a panel ofkinases, including ITK. ()-Zanubrutinib is at least 10-fold weaker than ibrutinib in inhibiting rituximab inducedADCC, consistent with its weak ITK inhibition activity 1.體內(nèi)研究 ()-Zanubrutinib induces dose-dependent anti-tumor effects against REC-1 MCL xenografts engrafted eithersubcutane

7、ously 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.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Dr. Wang from Chinese Aca

8、demy of Sciences.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Na L, et al. BGB-3111 is a novel and highly selective Brutons tyrosine kinase (BTK) inhibitor. abstract. In: Proceedings of the 106thAnnual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res2015;75(15 Suppl):Abstract nr 2597. doi:10.1158/1538-7445.AM2015-2597McePdfHeightCaution: Product has not been fully validated for medical applic