澤布替尼作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetZanubrutinibCat. No.: HY-101474ACAS No.: 1691249-45-2分式: CHNO分量: 471.55作靶點(diǎn): Btk作通路: Protein Tyrosine Kinase/RTK儲(chǔ)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(shí)驗(yàn) DMSO : 56.75 mg/mL (120.35 mM)Ethanol : 1 mg/mL (insoluble)* means soluble, but saturation

2、unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)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(qǐng)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(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。BIOLOGICAL A

3、CTIVITY物活性 Zanubrutinib (BGB-3111)個(gè)選擇性的 Bruton tyrosine kinase (Btk) 抑制劑。IC & Target BTK1體外研究 Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (BTK) inhibitor. In both biochemical and cellular assays,Zanubrutinib demonstrates nanomolar BTK inhibition activity. In several MCL and DLBCL c

4、ell lines, Zanubrutinibinhibits BCR aggregation-triggered BTK autophosphorylation, blocks downstream PLC-2 signaling, and potentlyinhibits cell proliferation. In comparison with PCI-32765, Zanubrutinib shows much more restricted off-target activitiesagainst a panel of kinases, including ITK1.Page 1

5、of 2 www.MedChemE體內(nèi)研究 Zanubrutinib (BGB-3111) induces dose-dependent anti-tumor effects against REC-1 MCL xenografts engrafted eithersubcutaneously or systemically via tail vein injection in mice. In the subcutaneous xenografts, Zanubrutinib at 2.5 mg/kg BID shows similar activity as PCI-32765 at 50

6、 mg/kg QD. In the systemic model, the median survival ofZanubrutinib 25 mg/kg BID group is significantly longer than those of both PCI-32765 50 mg/kg QD and BID groups.In an ABC-subtype DLBCL (TMD-8) subcutaneous xenograft model, Zanubrutinib also demonstrates better anti-tumoractivity than PCI-3276

7、5. Preliminary 14-day toxicity study in rats shows that Zanubrutinib is very well tolerated andmaximal tolerate dose (MTD) is not reached when it is dosed up to 250 mg/kg/day1.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Thromb Haemost. 2019 Mar;119(3):397-406.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Na Li, et al. Abstract 2597: BGB-3111 is a novel and highly selective Brutons tyrosine kinase (BTK) inhibitor. Cancer Res 2015;75(15 Suppl):Abstract nr2597.McePdfHeightCaution: Product has not been fully validated for medical applications. For research use only.Tel