NCT-505 free base

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

NCT-505 游离碱 (NCT505) 是一种有效的、选择性的、口服的 ALDH1A1 抑制剂，IC50 为 7 nM (hALDH1A1)。

NCT-505 free base (NCT505) is a potent, selective, orally available ALDH1A1 inhibitor with IC50 of 7 nM (hALDH1A1), exhibits high specificity over other ALDH isozymes and unrelated dehydrogenases; also exhibits IC50 of 30 nM in MIA PaCa-2 Aldefluor cell-based assays; demonstrates target engagement in CETSA asssay (EC50=3.4 uM), inhibits the formation of 3D spheroid cultures of OV-90 cancer cells, and potentiates the cytotoxicity of Paclitaxel in SKOV-3-TR, a Paclitaxel resistant ovarian cancer cell line.

NCT-505 (Compound 86) is a potent and selective aldehyde dehydrogenase (ALDH1A1) inhibitor, with an IC50 of 7 nM, and weakly inhibits hALDH1A2, hALDH1A3, hALDH2, hALDH3A1 (IC50s, >57, 22.8, 20.1, >57 μM). NCT-505 has no obvious inhibitory effec on 5-hydroxyprostaglandin dehydrogenase (HPGD) and type-4 hydroxysteroid dehydrogenase (HSD17β4) (IC50, >57 μM). Moreover, NCT-505 shows potent cellular activities, reducing the viability of OV-90 cells with an EC50 of 2.10-3.92 μM. NCT-505 is also cytotoxic to SKOV-3-TR cells, with IC50s of 1, 3, 10, 20, 30 μM, respectively, in the titration assay.

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NCT505 | NCT 505

Metabolic Enzyme/Protease

ALDH

ALDH

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2231079-74-4

521.611

C27H28FN5O3S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (191.71 mM)

CS(=O)(=O)N1CCN(CC1)C(=O)C2=CN=C3C=CC(=CC3=C2N4CCC(CC4)(C#N)C5=CC=CC=C5)F

1-(6-Fluoro-3-(4-(methylsulfonyl)piperazine-1-carbonyl)quinolin-4-yl)-4-phenylpiperidine-4-carbonitrile

(-20℃)

With Ice Pack

≥ 2 years