3alpha-Aminocholestane

3alpha-Aminocholestane is an inhibitor of SH2 domain-containing inositol-5'-phosphatase 1 (SHP-1, IC50 = ~2.5 µM). It is selective for SHP-1 over SHP-2 and phosphatase and tensin homolog (PTEN, IC50s = >20 µM). 3alpha-Aminocholestane induces hyperactivation of the tyrosine kinase SYK in patient-derived Ph+ acute lymphoblastic leukemia (ALL) cells and selectively induces cytotoxicity in these cells over mature B cell lymphoma cells. It reduces leukemia burden and increases survival in a tyrosine kinase inhibitor-resistant patient-derived Ph+ ALL mouse xenograft model when administered at a dose of 50 mg/kg. 3alpha-Aminocholestane reduces cell viability of OPM2 multiple myeloma (MM) cells in a concentration-dependent manner and of RPMI8226 MM cells when used at concentrations greater than or equal to 12.5 µM. It halts the cell cycle at the G0/G1 or G2/M stages in the highly proliferative OPM2 or less proliferative RPMI8226 cell lines, respectively. It induces apoptosis via activation of caspase-3, caspase-9, and poly(ADP-ribose) polymerase (PARP) in OPM2 cells but not in RPMI8226 cells. 3alpha-Aminocholestane reduces tumor burden and increases survival in an OPM2 mouse xenograft model.Formal Name: (3alpha,5alpha)-cholestan-3-amine. CAS Number: 2206-20-4. Synonyms: 3AC. Molecular Formula: C27H49N. Formula Weight: 387.7. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: Chloroform: 30 mg/ml. SMILES: C[C@H](CCCC(C)C)[C@@]1([H])CC[C@@]2([H])[C@]3([H])CC[C@@]4([H])C[C@H](N)CC[C@]4(C)[C@@]3([H])CC[C@@]21C. InChi Code: InChI=1S/C27H49N/c1-18(2)7-6-8-19(3)23-11-12-24-22-10-9-20-17-21(28)13-15-26(20,4)25(22)14-16-27(23,24)5/h18-25H,6-17,28H2,1-5H3/t19-,20+,21-,22+,23-,24+,25+,26+,27-/m1/s1. InChi Key: RJNGJYWAIUJHOJ-FBVYSKEZSA-N.