AT-406 HCl

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

AT-406，一种口服活性的多重凋亡蛋白抑制剂 (IAP) 拮抗剂。

AT-406, an orally active antagonist of multiple inhibitor of apoptosis proteins(IAP), inhibits progression of human ovarian Y binding to XIAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 66.4 nM, 1.9 nM, and 5.1 nM, 50- to 100-fold higher affinities than the Smac AVPI peptide.

Xevinapant (AT-406) hydrochloride potently inhibits cell growth in the MDA-MB-231 breast and SK-OV-3 ovarian cancer cell lines with IC50=144 nM and 142 nM, respectively.Xevinapant (0-3 μM; 0-48 horus) hydrochloride effectively induces cell death in a time- and dose-dependent manner.

Xevinapant (AT-406) hydrochloride is very effective in inhibition of tumor growth in the MDA-MB-231 xenograft model, and has minimal toxicity to animals. Xevinapant hydrochloride evaluated for its pharmacokinetic (PK) properties in mice, rats, non-human primates and dogs. Animal Model:SCID mice bearing MDA-MB-231 xenograft tumors Dosage:30 and 100 mg/kg Administration:p.o.; 5 days a week for 2 weeks Result:Strongly inhibits tumor growth at 30 and 100 mg/kg and completely inhibits tumor growth during the treatment with 100 mg/kg.

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Others

Other Targets

Apoptosis protein

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1071992-57-8

598.19

C32H44ClN5O4

>98% (HPLC)

In Vitro:?DMSO : 175 mg/mL (292.55 mM)

N12[C@@H](CCN(C[C@@H](C1=O)NC(=O)[C@H](C)NC)C(=O)CC(C)C)CC[C@H]2C(=O)NC(c1ccccc1)c1ccccc1

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(-20℃)

With Ice Pack

≥ 2 years