BAY-069

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BAY-069 是一种有效的支链氨基酸转氨酶 1 和 2 (BCAT1, BCAT2) 抑制剂，IC50 分别为 31 nM 和 153 nM。BAY-069 也可以用作化学探针。BAY-069 可用于抗癌研究。

BAY-069 is a potent branched-chain amino acid transaminases 1 (BCAT1) and BCAT2 inhibitor with IC50 values of 31 nM and 153 nM, respectively. BAY-069 also can be used as a chemical probe. BAY-069 can be used tor research anticancer.

BAY-069 (compound 36a) (70 nM-50 μM; 72 h) inhibits cell proliferation of U-87 and MDA-MB-231.Cell Proliferation Assay Cell Line:U-87 and MDA-MB-231 Concentration:70 nM-50 μM Incubation Time:72 h Result:Inhibited cell proliferation of U-87 and MDA-MB-231 with IC50s of 358 nM and 874 nM, respectively.

BAY-069 exhibits high metabolic stability after incubation with human liver microsomes (CLblood = 0.11 L/h/kg) and moderate metabolic stability after incubation with rat hepatocytes (CLblood = 1.8 L/h/kg); shows high permeability through Caco-2 cell monolayers with no hint of efflux.BAY-069 (0.3 mg/kg for i.v.; 0.6 mg/kg for p.o.; single dosage) exhibits a favorable pharmacokinetic profile after i.v. dosing with low blood clearance (CLblood), moderate volume of distribution at steady state (Vss), and intermediate terminal half-life (t1/2).Animal Model:Male Wistar rats Dosage:0.3 mg/kg for i.v.; 0.6 mg/kg for p.o.Administration:i.v. or p.o.; single dosage Result:Pharmacokinetic Parameters of BAY-069 in male Wistar rats.

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Others

Other Targets

Reactive Oxygen Species

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2639638-66-5

446.81

C22H14ClF3N2O3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 200 mg/mL (447.62 mM; 超声助溶 )

O=C1N(C=2C3=C(C(Cl)=C(OC4=C(C)C=CC=C4)C2)C=CC=C3)C(=O)NC(C(F)(F)F)=C1

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(-20℃)

With Ice Pack

≥ 2 years