An inhibitor of SHP-1 (IC50 = ~2.5 µM); selective for SHP-1 over SHP-2 and PTEN (IC50s = >20 µM); induces hyperactivation of SYK in patient-derived Ph+ ALL cells; reduces leukemia burden and increases survival in a tyrosine kinase inhibitor-resistant patient-derived Ph+ ALL mouse xenograft model at 50 mg/kg; reduces cell viability of OPM2 cells in a concentration-dependent manner and of RPMI8226 cells at ≥12.5 µM; halts the cell cycle at the G0/G1 or G2/M stages in the highly proliferative OPM2 or less proliferative RPMI8226 cell lines

3α-Aminocholestane – 5 mg

Brand:
Cayman
CAS:
2206-20-4
Storage:
-20
UN-No:
Non-Hazardous - /

3α-Aminocholestane is an inhibitor of SH2 domain-containing inositol-5’-phosphatase 1 (SHP-1; IC50 = ~2.5 µM).{35841} It is selective for SHP-1 over SHP-2 and phosphatase and tensin homolog (PTEN; IC50s = >20 µM). 3α-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. 3α-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.{35843} 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. 3α-Aminocholestane reduces tumor burden and increases survival in an OPM2 mouse xenograft model.  

 

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Description

An inhibitor of SHP-1 (IC50 = ~2.5 µM); selective for SHP-1 over SHP-2 and PTEN (IC50s = >20 µM); induces hyperactivation of SYK in patient-derived Ph+ ALL cells; reduces leukemia burden and increases survival in a tyrosine kinase inhibitor-resistant patient-derived Ph+ ALL mouse xenograft model at 50 mg/kg; reduces cell viability of OPM2 cells in a concentration-dependent manner and of RPMI8226 cells at ≥12.5 µM; halts the cell cycle at the G0/G1 or G2/M stages in the highly proliferative OPM2 or less proliferative RPMI8226 cell lines, respectively; induces apoptosis via activation of caspase-3, caspase-9, and PARP in OPM2 cells but not in RPMI8226 cells

Formal name: (3α,5α)-cholestan-3-amine

Synonyms:  3AC

Molecular weight: 387.7

CAS: 2206-20-4

Purity: ≥95%

Formulation: A solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phosphatases||Research Area|Cancer|Cell Cycle|G1||Research Area|Cancer|Cell Cycle|G2/M||Research Area|Cancer|Cell Death|Apoptosis

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