PTC299 ( PTC-299 | PTC 299 )

产品货号. M11050 CAS No. 1256565-36-2

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

PTC299
注意事项

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
产品简述

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。
产品描述

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.
体外实验

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.
体内实验

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同义词

PTC-299 | PTC 299
通路

Others
靶点

Other Targets
受体

Other Targets
研究领域

Cancer
适应症

Breast Cancer

CAS Number

1256565-36-2
分子量

467.346
分子式

C25H20Cl2N2O3
纯度

>98% (HPLC)
溶解度

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

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

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

1. Cao L, et al. Mol Cancer Ther. 2018 Oct 23. pii: molcanther.0863.2018.

计算器

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