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NSC781406

Catalog No. T16355Cas No. 1676893-24-5

NSC781406 is a highly effective inhibitor of PI3K and mTOR (IC50: 2 nM for PI3Kα).

NSC781406

NSC781406

Purity: 99.58%
Catalog No. T16355Cas No. 1676893-24-5
NSC781406 is a highly effective inhibitor of PI3K and mTOR (IC50: 2 nM for PI3Kα).
Pack SizePriceAvailabilityQuantity
2 mg$35In Stock
5 mg$58In Stock
10 mg$94In Stock
25 mg$171In Stock
50 mg$257In Stock
100 mg$395In Stock
200 mg$562In Stock
1 mL x 10 mM (in DMSO)$81In Stock
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Purity:99.58%
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Product Introduction

Bioactivity
Description
NSC781406 is a highly effective inhibitor of PI3K and mTOR (IC50: 2 nM for PI3Kα).
Targets&IC50
PI3Kγ:2.7 nM, mTOR:5.4 nM, PI3Kα:2 nM, PI3Kδ:14 nM, PI3Kβ:9.4 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 .
Chemical Properties
Molecular Weight627.68
FormulaC29H27F2N5O5S2
Cas No.1676893-24-5
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM1.5932 mL7.9658 mL15.9317 mL79.6584 mL
5 mM0.3186 mL1.5932 mL3.1863 mL15.9317 mL
10 mM0.1593 mL0.7966 mL1.5932 mL7.9658 mL
20 mM0.0797 mL0.3983 mL0.7966 mL3.9829 mL
50 mM0.0319 mL0.1593 mL0.3186 mL1.5932 mL
100 mM0.0159 mL0.0797 mL0.1593 mL0.7966 mL

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