Description
AM-8735 is a potent and selective MDM2 inhibitor with an IC50 of 25 nM.
Product information
CAS Number: 1429386-01-5
Molecular Weight: 568.51
Formula: C27H31Cl2NO6S
Chemical Name: 2-[(2R,5R,6R)-6-(3-chlorophenyl)-5-(4-chlorophenyl)-4-[(1S)-1-cyclopropyl-2-(2-methylpropane-2-sulfonyl)ethyl]-3-oxomorpholin-2-yl]acetic acid
Smiles: CC(C)(C)S(=O)(=O)C[C@H](C1CC1)N1[C@@H]([C@H](O[C@H](CC(O)=O)C1=O)C1C=C(Cl)C=CC=1)C1C=CC(Cl)=CC=1
InChiKey: ZTMSSDQFJNEUNG-WMMXXEOUSA-N
InChi: InChI=1S/C27H31Cl2NO6S/c1-27(2,3)37(34,35)15-21(16-7-8-16)30-24(17-9-11-19(28)12-10-17)25(18-5-4-6-20(29)13-18)36-22(26(30)33)14-23(31)32/h4-6,9-13,16,21-22,24-25H,7-8,14-15H2,1-3H3,(H,31,32)/t21-,22-,24-,25-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
AM-8735 displays substantial growth inhibition of wild-type p53 cells (IC50=63 nM) and no growth inhibition of p53-deficient cells (IC50>25 μM). AM-8735exhibits a dose-dependent increase of p21 mRNA, a direct transcriptional readout of p53 activity, in HCT116 p53wt cells (IC50=160 nM).
In Vivo:
AM-8735 also demonstrates significant time and concentration dependent p21 mRNA induction in vivo in a pharmacodynamic assay in SJSA-1 osteosarcoma tumors. AM-8735 shows excellent antitumor activity in the SJSA-1 osteosarcoma xenograft model with an ED50 of 41 mg/kg.
Products are for research use only. Not for human use.
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