PTC299

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

PTC299 (PTC-299) 是一种新型有效的二氢乳清酸脱氢酶 (DHODH) 抑制剂，可抑制 HeLa 细胞中缺氧诱导的 VEGFA 蛋白产生，IC50 为 1.64 nM。

PTC299 (PTC-299) is a novel potent inhibitor of dihydroorotate dehydrogenase (DHODH), inhibits hypoxia-induced VEGFA protein production in HeLa cells with IC50 of 1.64 nM; inhibited DHODH activity more potently than teriflunomide and with potency similar to that of brequinar, demonstrates broad and potent activity against hematological cancer cells in preclinical models, inhibits AML patient-derived cells with IC50 of 2-60 nM; demonstrates advantages over previously reported DHODH inhibitors, including greater potency, good oral bioavailability and lack of off-target kinase inhibition and myelosuppression.Breast Cancer Phase 1 Clinical.

PTC299 inhibits hypoxia-induced VEGFA protein production in HeLa cells with an EC50 of 1.64 ± 0.83 nM.PTC299 is the most potent inhibitor with an IC50 of about 1 nM, over 10 to 1000-fold more potent than Brequinar, Vidofludimus or A 77-1726 in leukemia cells.

——

PTC-299 | PTC 299

Others

Other Targets

Other Targets

Cancer

Breast Cancer

1256565-36-2

467.346

C25H20Cl2N2O3

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (106.99 mM)

COC1=CC=C(C=C1)C2C3=C(CCN2C(=O)OC4=CC=C(C=C4)Cl)C5=C(N3)C=CC(=C5)Cl

4-chlorophenyl (S)-6-chloro-1-(4-methoxyphenyl)-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indole-2-carboxylate

(-20℃)

With Ice Pack

≥ 2 years