AT-406
- Product Name
- AT-406
- CAS No.
- 1071992-57-8
- Chemical Name
- AT-406
- Synonyms
- AT-406;AT-406(HCl);AT-406 (hydrochloride);Xevinapant hydrochloride;(5S,8S,10aR)-N-(Diphenylmethyl)decahydro-5-[[(2S)-2-(methylamino)-1-oxopropyl]amino]-3-(3-methyl-1-oxobutyl)-6-oxo-pyrrolo[1,2-a][1,5]diazocine-8-carboxamide hydrochloride (1:1)
- CBNumber
- CB32516001
- Molecular Formula
- C32H44ClN5O4
- Formula Weight
- 598.19
- MOL File
- 1071992-57-8.mol
AT-406 Property
- storage temp.
- Store at -20°C, sealed storage, away from moisture and light
- solubility
- DMSO : 175 mg/mL (292.55 mM; Need ultrasonic)
- form
- Solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- API0013793
- Product name
- AT-406
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $301.4
- Updated
- 2021/12/16
- Product number
- orb181200
- Product name
- AT-406
- Purity
- >98%
- Packaging
- 100mg
- Price
- $838.1
- Updated
- 2021/12/16
- Product number
- orb181200
- Product name
- AT-406
- Purity
- >98%
- Packaging
- 250mg
- Price
- $1504.5
- Updated
- 2021/12/16
- Product number
- orb181200
- Product name
- AT-406
- Purity
- >98%
- Packaging
- 1000mg
- Price
- $3136.5
- Updated
- 2021/12/16
AT-406 Chemical Properties,Usage,Production
Uses
Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors[1][2].
in vivo
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[1].
Xevinapant hydrochloride evaluated for its pharmacokinetic (PK) properties in mice, rats, non-human primates and dogs[1].
| Animal Model: | SCID mice bearing MDA-MB-231 xenograft tumors[1] |
| 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. |
IC 50
cIAP1: 1.9 nM (Ki); cIAP2: 5.1 nM (Ki); XIAP: 66.4 nM (Ki)
References
[1] Cai Q, Sun H, Peng Y, et al. A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment. J Med Chem. 2011;54(8):2714-2726. DOI:10.1021/jm101505d
[2] Brunckhorst MK, et al. AT-406, an orally active antagonist of multiple inhibitor of apoptosis proteins, inhibits progression of human ovarian cancer. Cancer Biol Ther. 2012;13(9):804-811. DOI:10.4161/cbt.20563
AT-406 Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from AT-406 manufacturers
- Product
- AT-406 1071992-57-8
- Price
- US $7.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 100kg
- Release date
- 2019-08-04