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AT406 (Xevinapant, SM406, ARRY334543)

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InvivoChem Cat #: V0053

CAS #: 1071992-99-8Purity ≥98%

Description: Xevinapant (formerly Debio1143; AT-406; SM-406, ARRY-334543) is a first-in-class and orally bioavailable peptidomimetic of SMAC (second mitochondrial-derived activator of caspases)/DIABLO with potential antitumor activity, also an antagonist of IAP (inhibitor of apoptosis protein via E3 ubiquitin ligase) proteins. It acts by binding to XIAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Kis of 66.4 nM, 1.9 nM, and 5.1 nM, respectively.

References: Cancer Res. 2004 Oct 15;64(20):7183-90.

Related CAS: 1071992-57-8 (HCl salt) 1071992-99-8 (free base)

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Molecular Weight (MW)	561.71
Formula	C32H43N5O4
CAS No.	1071992-99-8
Storage	-20℃ for 3 years in powder form
Storage	-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/Synonym	AT-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;

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In Vitro	AT-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 Vivo	AT-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 model	MDA-MB-231 xenograft tumors in severe combined immune deficiency (SCID) mice
Formulation & Dosage	HCl 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.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Purity ≥98%
COA
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NMR

[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.

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