SAR245409 (XL765) (Synonyms: PI3K-IN-1;XL-147 derivative 1) |
Catalog No.GC14884
One-Click Copy Product Info
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SAR245409(XL765)(XL-147 유도체 1)는 PI3K의 강력한 억제제입니다. SAR245409(XL765)(25 μM)는 PI3K/Akt 신호 전달 경로를 차단합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1349796-36-6
Sample solution is provided at 25 µL, 10mM.
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SAR245409 (XL765) is a selective dual inhibitor of PI3K and mTOR (IC50= 9 nM for PI3Kγ).
PI3K (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. It plays a key role in PI3K/Akt/mTOR pathway.
In PA cell lines, combination of XL765 and TMZ blocked the cell growth and led to apoptosis [1]. In a variety of tumor cell lines that mutated on PI3K signaling, XL765 inhibited PIP3 formation in the membrane and AKT/p70S6K/S6 phosphorylation [2].
In GH3 xenograft tumor mouse models, combination use of XL765 and TMZ inhibited tumor growth, reduced serum GH and prolactin levels with no increased systemic side effects [1]. In severe combined immunodeficient mice, XL765 abolished MPNST local and metastatic growth. [3]. In multiple human xenograft models in nude mice, repeat dose administration showed significant tumor growth inhibition that related to antiproliferative and antiangiogenic response etc. [2]
References:
1. Dai C, Zhang B, Liu X et al. Inhibition of PI3K/AKT/mTOR pathway enhances temozolomide-induced cytotoxicity in pituitary adenoma cell lines in vitro and xenografted pituitary adenoma in female nude mice. Endocrinology. 2013 Mar;154(3):1247-59.
2. Yu P, Laird AD, Du X et al. Characterization of the activity of the PI3K/mTOR inhibitor XL765 (SAR245409) in tumor models with diverse genetic alterations affecting the PI3K pathway. Mol
Cancer Ther. 2014 May;13(5):1078-91.
3. Ghadimi MP, Lopez G, Torres KE et al. Targeting the PI3K/mTOR axis, alone and in combination with autophagy blockade, for the treatment of malignant peripheral nerve sheath tumors. Mol Cancer Ther. 2012 Aug;11(8):1758-69.
| Cas No. | 1349796-36-6 | SDF | |
| Synonyms | PI3K-IN-1;XL-147 derivative 1 | ||
| Chemical Name | N-[4-[[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl]-3-methoxy-4-methylbenzamide | ||
| Canonical SMILES | CC1=C(C=C(C=C1)C(=O)NC2=CC=C(C=C2)S(=O)(=O)NC3=NC4=CC=CC=C4N=C3NC5=CC(=CC(=C5)OC)OC)OC | ||
| Formula | C31H29N5O6S | M.Wt | 599.66 |
| Solubility | ≥ 15mg/mL in DMSO | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6676 mL | 8.3381 mL | 16.6761 mL |
| 5 mM | 333.5 μL | 1.6676 mL | 3.3352 mL |
| 10 mM | 166.8 μL | 833.8 μL | 1.6676 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 saline, 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)