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AT406(Xevinapant,SM406,ARRY334543)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AT406(Xevinapant,SM406,ARRY334543)图片
CAS NO:1071992-99-8
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)561.71
FormulaC32H43N5O4
CAS No.1071992-99-8
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (178.0 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: N/A
Solubility (In vivo)30% Propylene glycol, 5% Tween 80, 65% D5W: 30mg/mL
Chemical Name/SynonymAT-406; AT 406; AT406; SM-406, ARRY-334543; SM 406, ARRY 334543; SM406, ARRY334543; D 1143; Debio 1143; N65WC8PXDD; SM 406; (5S,8S,10aR)-N-benzhydryl-5-((S)-2-(methylamino)propanamido)-3-(3-methylbutanoyl)-6-oxo-decahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide;
实验参考方法
In VitroAT-406 is a Smac mimetic and appears to mimic closely the AVPI peptide in both hydrogen bonding and hydrophobic interactions with XIAP, with additional hydrophobic contacts with W323 of XIAP. AT-406 is more sensitive to these IAPs than Smac AVPI peptide with 50-100 fold binding affinities. AT-406 (at 1 μM) completely restores the activity of caspase-9, which is suppressed by 500 nM XIAP BIR3 in a cell-free system.
In VivoAT-406 has good pharmacokinetic (PK) properties and oral bioavailability in mice, rats, non-human primates, and dogs. In the MDA-MB-231 xenograft, AT-406 effectively induces cIAP1 degradation and processing of procaspase-8, cleavage of PARP in tumor tissues at 100 mg/kg with well toleration even at 200 mg/kg. AT-406 induces significant tumor growth inhibition with p of 0.0012 at 100 mg/kg.
Animal modelMDA-MB-231 xenograft tumors in severe combined immune deficiency (SCID) mice
Formulation & DosageHCl salt form of AT-406 in water; 10, 30, 100 mg/kg; Oral
References[1] Cai Q, et al. J Med Chem, 2011, 54(8), 2714-2726.
生物活性

[1] Cai Q, et al. J Med Chem, 2011, 54(8), 2714-2726.

[1] Cai Q, et al. J Med Chem, 2011, 54(8), 2714-2726.