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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $47 | In Stock | |
5 mg | $97 | In Stock | |
10 mg | $163 | In Stock | |
25 mg | $297 | In Stock | |
50 mg | $490 | In Stock | |
100 mg | $715 | In Stock | |
1 mL x 10 mM (in DMSO) | $135 | In Stock |
Description | NSC781406 is a highly effective inhibitor of PI3K and mTOR (IC50: 2 nM for PI3Kα). |
Targets&IC50 | mTOR:5.4 nM, PI3Kδ:14 nM, PI3Kα:2 nM, PI3Kβ:9.4 nM, PI3Kγ:2.7 nM |
In vitro | NSC781406 shows reasonable liver microsome stability. NSC781406 displays effective PI3K inhibition (PI3Kα IC50=2.0 nM) that translates into BEL-7404 cells proliferation inhibition (IC50=20 nM) and it also demonstrates cytotoxic activities against leukemia, non-small cell, lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, and breast cancer. It is effective against 60 cancer cell lines with a mean GI50 value of 65 nM and with a GI50 value of less than 10 nM against four cancer cell lines. |
In vivo | NSC781406 is well tolerated at 30 mg/kg, with no observed mortality or significant reduction of body weight. NSC781406(30 mg/kg) treatment, causes statistically significant antitumor activity, in the xenograft models. It has a mean reduction in the relative tumor volume ratio of 52%. Sorafenib shows an inhibition ratio of 44% at 50 mg/kg . |
Molecular Weight | 627.68 |
Formula | C29H27F2N5O5S2 |
Cas No. | 1676893-24-5 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 150 mg/mL (238.98 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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