OXA-01 |
| رقم الكتالوجGC15740 |
OXA-01 هو مثبط قوي لـ mTORC1 و mTORC2 ، بقيم IC50 تبلغ 29 نانومتر و 7 نانومتر ، على التوالي
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 936889-68-8
Sample solution is provided at 25 µL, 10mM.
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OXA-01 is an ATP-competitive and selective inhibitor of both mTORC1 and mTORC2 with IC50 values of 29 nM and 7 nM, respectively [1].
The mammalian target of rapamycin (mTOR) is a serine/threonine kinase and exists in two complexes, mTORC1 and mTORC2. MTORC1 activation through PI3K and Akt controls cell growth and mTORC2 phosphorylates Akt, SGK1, and PKC to control cell survival and cytoskeletal organization [1].
OXA-01 is a dual inhibitor of mTORC1 and mTORC2, and inhibited mTOR kinase with IC50 value of 11 nM. In cell-based assays, OXA-01 inhibited mTOR signaling of phospho-4E-BP1 with IC50 value of 1.1 μM [1].
In GEO colorectal xenograft model, the median plasma concentration of OXA-01 was 25.6 μM at 1 hour and 13.2 μM at 8 hours, and OXA-01 slowed tumor growth. In RIP-Tag2 pancreatic neuroendocrine tumors, OXA-01 reduced Akt, 4E-BP1 and S6K phosphorylation. OXA-01 also decreased cellular proliferation and increased apoptosis. OXA-01 reduced VEGF production, which was associated with decreased tumor angiogenesis [1].
Reference:
[1]. Falcon BL, Barr S, Gokhale PC, et al. Reduced VEGF production, angiogenesis, and vascular regrowth contribute to the antitumor properties of dual mTORC1/mTORC2 inhibitors. Cancer Res. 2011 Mar 1;71(5):1573-83.
| Cas No. | 936889-68-8 | SDF | |
| Chemical Name | trans-4-[8-amino-1-(7-chloro-1H-indol-2-yl)imidazo[1,5-a]pyrazin-3-yl]-cyclohexanecarboxylic acid | ||
| Canonical SMILES | OC([C@H]1CC[C@H](C2=NC(C3=CC4=C(C(Cl)=CC=C4)N3)=C5N2C=CN=C5N)CC1)=O | ||
| Formula | C21H20CIN5O2 | M.Wt | 409.9 |
| الذوبان | ≤3mg/ml in DMSO;1mg/ml in dimethyl formamide | 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 | 2.4396 mL | 12.1981 mL | 24.3962 mL |
| 5 mM | 487.9 μL | 2.4396 mL | 4.8792 mL |
| 10 mM | 244 μL | 1.2198 mL | 2.4396 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)
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