[CAS NO. 2206-20-4] 3α-Aminocholestane
PRODUCTS SPECIFICATIONS [2206-20-4]
DESCRIPTION [2206-20-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 387.68 |
| Molecular Formula | C27H49N |
| SMILES | CC(C)CCC[C@@H](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 |
4 Publications Citing Use of MCE
Summary
3α-Aminocholestane is a selective SH2 domain-containing inositol-5′-phosphatase 1 ( SHIP1 ) inhibitor with an IC 50 of ~2.5 μM.
IC50 & Target
IC50: 2.5 μM (SHIP1) [1]
In Vitro
OPM2 cell viability is effectively reduced by 3α-Aminocholestane (3AC) treatment. RPMI8226 and U266 cells show significantly less sensitivity to 3α-Aminocholestane treatment when compare with OPM2 cells, although viability is decreased significantly at concentrations of ≥12.5 μM. Treatment with 3α-Aminocholestane for 36 h severely reduces the percentage of cells in the S phase, which is accompanied by an increase of cells in the G2/M phase. In contrast, in the less proliferative RPMI8226 and U266 cells, cell cycle progression is blocked in the G0/G1 phase upon 3α-Aminocholestane treatment, in conjunction with a reduced percentage of cells undergoing the S phase [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
It is found that 3α-Aminocholestane (3AC) results in reduced multiple myeloma (MM) growth in vivo , as determined by quantitation of free human Igλ light chain in the plasma after OPM2 challenge. In addition, reduced numbers of circulating OPM2 cells, as determined by human HLA-ABC staining, is observed in peripheral blood from 3α-Aminocholestane-treated mice compare with vehicle controls. Most importantly, 3α-Aminocholestane treatment results in significantly enhanced survival of mice after tumor challenge. In 3α-Aminocholestane-treated mice that resist treatment, it is found that MM tumors exhibit an upregulation of SHIP2, reminiscent of in vitro treatment of OPM2 cells and suggesting that SHIP1 inhibition may select for tumor cells with increased SHIP2 expression [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
Ethanol : 50 mg/mL ( 128.97 mM ; Need ultrasonic)
DMSO : < 1 mg/mL (insoluble or slightly soluble)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5794 mL | 12.8972 mL | 25.7945 mL |
| 5 mM | 0.5159 mL | 2.5794 mL | 5.1589 mL |
| 10 mM | 0.2579 mL | 1.2897 mL | 2.5794 mL |
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Add each solvent one by one: 10% EtOH >> 90% corn oil
Solubility: ≥ 3.25 mg/mL (8.38 mM); Clear solution
References
- [1] Chen Z, et al. Signalling thresholds and negative B-cell selection in acute lymphoblastic leukaemia. Nature. 2015 May 21;521(7552):357-61.
- [2] Gwenny M Fuhler, et al. Therapeutic Potential of SH2 Domain-Containing Inositol-5′-Phosphatase 1 (SHIP1) and SHIP2 Inhibition in Cancer. Mol Med. 2012 Feb 10;18:65-75.
