location： Home > Products > Signaling Pathways > Apoptosis > IAP

AT406 (Xevinapant, SM406, ARRY334543)

Price：

Market Price：

This product is for research use only, not for human use. We do not sell to patients.

Number： - + Pieces（InventoryPieces）

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)

Customer Validation

Official Supplier of

Related Products

Publications Citing InvivoChem Products

Physicochemical and Storage Information
Protocol
Quality Control Documentation
Related Biological Data
Customer Review

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;

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
- Mass
- Concentration
- Volume
- Molecular Weight *
- =
- ×
- ×
The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂
- Concentration _(start)
- ×
- Volume _(start)
- =
- Concentration _(final)
- ×
- Volume _(final)
- ×
- =
- ×
- C1
- V1
- C2
- V2

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
MSDS

[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.

Home Prev Next Last page / pices

发评论

Your information is safe with us. * Required Fields.

Product name

Cat

Applicant name

Email address

Phone number

Organization name

Country

Requested quantity

Remarks