3α-Aminocholestane (Synonyms: 3AC) |
| カタログ番号GC33059 |
3α-アミノコレスタンは、IC50 が約 2.5 μM の選択的 SH2 ドメイン含有イノシトール-5'-ホスファターゼ 1 (SHIP1) 阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2206-20-4
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
3α-Aminocholestane is a selective SH2 domain-containing inositol-5′-phosphatase 1 (SHIP1) inhibitor with an IC50 of ~2.5 μM.
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].
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].
[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.
Cell experiment: | Cells are treated in triplicate or more with increasing concentrations of compounds (including 3α-Aminocholestane). Cell viability is determined with a Cell Counting Kit according to the manufacturer’s instructions. The odds density (OD) of compound (including 3α-Aminocholestane )-treated cells is divided by the OD of their vehicle control, and the viability is expressed as a percentage of untreated cells. Results are expressed as mean±standard error of the mean (SEM) of three individual experiments. For phosphatidyl inositol phosphates (PIP) add-back experiments, MCF-7 cells are treated for 2 h with 10 μM SHIP inhibitors (including 3α-Aminocholestane ), after which cells are washed and fresh medium is added. Cells are subsequently cultured in the absence (0 μM) or presence (10 or 20 μM) of either PtdIns(3,4)P2-diC16 (P-3416) or PtdIns(3,5)P2-diC16 (P-3516) for 36 h, after which cell viability is determined by the Cell Counting Kit[2]. |
Animal experiment: | NOD/SCID/γcIL2R (NSG) mice are injected intraperitoneally with 1×107 OPM2 cells and 6 h later receive an initial injection of 3α-Aminocholestane (3AC) or vehicle. 3α-Aminocholestane is suspended in a 0.3% Klucel/H2O solution at 11.46 mM and administered by intraperitoneal injection of 100 μL solution. Vehicle-treated mice receive 100 μL injection of 0.3% Klucel/H2O solution. The mice are then treated with 3α-Aminocholestane or vehicle daily for the next 6 d and then twice per week in the remaining 15 wks of the survival study[2]. |
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. | |
| Cas No. | 2206-20-4 | SDF | |
| 同義語 | 3AC | ||
| Canonical 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 | ||
| Formula | C27H49N | M.Wt | 387.68 |
| 溶解度 | Ethanol : 50 mg/mL (128.97 mM);DMSO : < 1 mg/mL (insoluble or slightly soluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *