BAY 61-3606 dihydrochloride 是一种口服有效的，ATP 竞争性的，可逆的选择性 Syk 抑制剂，Ki 为 7.5 nM，IC50 为 10 nM。BAY 61-3606 dihydrochloride 降低神经母细胞瘤细胞中的 ERK1/2 和 Akt 磷酸化。BAY 61-3606 dihydrochloride 降低 K-rn 细胞裂解物中 Syk 磷酸化。Bay 61-3606 dihydrochloride 作用于乳腺癌细胞，通过下调 Mcl-1 促进 TRAIL 诱导的细胞凋亡。 Information BAY-61-3606 BAY-61-3606 is a potent and selective inhibitor of Syk kinase (Ki = 7.5 nM). BAY-61-3606 induces cell cycle arrest and apoptosis . Targets Syk (Cell-free assay) 7.5 nM(Ki) In vitro BAY 61-3606 is a highly selective inhibitor of Syk kinase. Other selected tyrosine kinases, Lyn, Fyn, Src, Itk, and Btk, are not inhibited by BAY 61-3606 in concentrations up to 4.7 μM. BAY 61-3606 is also found to inhibit B cell receptor (BCR)-mediated signaling. Bay 61-3606 is a sensitizer of TRAIL-induced apoptosis. Mcl-1 downregulation by Bay 61-3606 are concentration- and time-dependent in MCF-7 cells. phosphorylation of Syk is reduced by Bay 61-3606 in MCF-7 and T47D cells. Downregulation of Mcl-1 by Bay 61-3606 is independent of Syk in breast cancer cells. Bay 61-3606 promotes the ubiquitin/proteasome-dependent degradation of the Mcl-1 protein in MCF-7 cells. Bay 61-3606 inhibits the phosphorylation of CDK9, RNA polymerase II, and Mcl-1 expression in MCF-7 cells. Bay 61-3606 inhibits CDK9 kinase activity with an in vitro IC50 of 37 nM. In vivo After 20 days of drug administration, the volume of the xenografted tumor was significantly (P Cell Research(from reference) Cell lines：MCF-7 cells Concentrations：2.5 μM or 5 μM Incubation Time：12 h or 24 h
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BAY-61-3606
CAS number：648903-57-5 molecular formula：C20H20Cl2N6O3
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| Chinese alias | - | ||
| English alias | MS-28520 | 2-(7-(3,4-Dimethoxyphenyl)imidazo(1,2-c)pyrimidin-5-ylamino)nicotinamide dihydrochloride | BAY 61-3606 (dihydrochloride) | YAB90357 | AKOS027276142 | HY-14985 | DTXSID20215179 | 2-[[7-(3,4-Dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]-3-p | ||
| CAS number | 648903-57-5 | molecular formula | C20H20Cl2N6O3 |
| molecular weight | 463.32 g/mol | Exact mass | 10mM in DMSO |
| PSA | 117.000 Ų | logp | 3.082 |
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