AMG232featured
WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#:206149
CAS#:1352066-68-2
Description:AMG232 is an extremely potent MDM2 inhibitor (SPR KD = 0.045 nM, SJSA-1 EdU IC50 = 9.1 nM), with remarkable pharmacokinetic properties and in vivo antitumor activity in the SJSA-1 osteosarcoma xenograft model (ED50 = 9.1 mg/kg). AMG232 is currently under clinical development.
Price and Availability
AMG232, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.
Chemical Structure
Theoretical Analysis
MedKoo Cat#: 206149Name: AMG232CAS#: 1352066-68-2Chemical Formula: C28H35Cl2NO5SExact Mass: 567.1613Molecular Weight: 568.55Elemental Analysis: C, 59.15; H, 6.20; Cl, 12.47; N, 2.46; O, 14.07; S, 5.64
Synonym:AMG232; AMG-232; AMG 232.
IUPAC/Chemical Name:2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid
InChi Key:DRLCSJFKKILATL-YWCVFVGNSA-N
InChi Code:InChI=1S/C28H35Cl2NO5S/c1-17(2)24(16-37(35,36)18(3)4)31-26(19-9-11-21(29)12-10-19)23(20-7-6-8-22(30)13-20)14-28(5,27(31)34)15-25(32)33/h6-13,17-18,23-24,26H,14-16H2,1-5H3,(H,32,33)/t23-,24-,26-,28-/m1/s1
SMILES Code:CC(C)S(C[C@H](C(C)C)N(C1=O)[C@@H]([C@H](C[C@@]1(CC(O)=O)C)C2=CC=CC(Cl)=C2)C3=CC=C(C=C3)Cl)(=O)=O
Technical Data
Additional Information
References
1: Wang Y, Zhu J, Liu JJ, Chen X, Mihalic J, DeignanJ, Yu M, Sun D, Kayser F, McGee LR, Lo MC, Chen A, Zhou J, Ye Q, HuangX, Long AM, Yakowec P, Oliner JD, Olson SH, Medina JC. Optimizationbeyond AMG 232: discovery and SAR of sulfonamides on a piperidinonescaffold as potent inhibitors of the MDM2-p53 protein-proteininteraction. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3782-5. doi:10.1016/j.bmcl.2014.06.073. Epub 2014 Jul 1. PubMed PMID: 25042256.
2: Rew Y, Sun D. Discovery of a small molecule MDM2 inhibitor (AMG 232)for treating cancer. J Med Chem. 2014 Aug 14;57(15):6332-41. doi:10.1021/jm500627s. Epub 2014 Jul 9. PubMed PMID: 24967612.
3: Gonzalez AZ, Eksterowicz J, Bartberger MD, Beck HP, Canon J, Chen A,Chow D, Duquette J, Fox BM, Fu J, Huang X, Houze JB, Jin L, Li Y, Li Z,Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, McMinn DL, Oliner JD,Osgood T, Rew Y, Saiki AY, Shaffer P, Wortman S, Yakowec P, Yan X, Ye Q,Yu D, Zhao X, Zhou J, Olson SH, Medina JC, Sun D. Selective and potentmorpholinone inhibitors of the MDM2-p53 protein-protein interaction. JMed Chem. 2014 Mar 27;57(6):2472-88. doi: 10.1021/jm401767k. Epub 2014Mar 4. PubMed PMID: 24548297.
4: Sun D, Li Z, Rew Y, Gribble M, Bartberger MD, Beck HP, Canon J, ChenA, Chen X, Chow D, Deignan J, Duquette J, Eksterowicz J, Fisher B, FoxBM, Fu J, Gonzalez AZ, Gonzalez-Lopez De Turiso F, Houze JB, Huang X,Jiang M, Jin L, Kayser F, Liu JJ, Lo MC, Long AM, Lucas B, McGee LR,McIntosh J, Mihalic J, Oliner JD, Osgood T, Peterson ML, Roveto P, SaikiAY, Shaffer P, Toteva M, Wang Y, Wang YC, Wortman S, Yakowec P, Yan X,Ye Q, Yu D, Yu M, Zhao X, Zhou J, Zhu J, Olson SH, Medina JC. Discoveryof AMG 232, a potent, selective, and orally bioavailable MDM2-p53inhibitor in clinical development. J Med Chem. 2014 Feb27;57(4):1454-72. doi: 10.1021/jm401753e. Epub 2014 Feb 5. PubMed PMID:24456472.
