NSC781406
NSC781406 Basic information
- Product Name:
- NSC781406
- Synonyms:
-
- NSC781406
- NSC781406;NSC-781406;NSC 781406
- NSC-781406;NSC 781406
- Benzenesulfonamide, 2,4-difluoro-N-[2-methoxy-5-[4-[3-[4-(methylsulfonyl)-1-piperazinyl]-1-propyn-1-yl]-6-quinolinyl]-3-pyridinyl]-
- NSC781406,Phosphoinositide 3-kinase,NSC 781406,NSC-781406,PI3K,Mammalian target of Rapamycin,Inhibitor,inhibit,mTOR
- 2,4-difluoro-N-[2-methoxy-5-[4-[3-[4-(methylsulfonyl)-1-piperazinyl]-1-propyn-1-yl]-6-quinolinyl]-3-pyridinyl]-benzenesulfonamide
- NSC781406, 10 mM in DMSO
- CAS:
- 1676893-24-5
- MF:
- C29H27F2N5O5S2
- MW:
- 627.68
- Mol File:
- 1676893-24-5.mol
NSC781406 Chemical Properties
- Boiling point:
- 775.1±70.0 °C(Predicted)
- Density
- 1.52±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMF: 10mg/mL; DMSO: 20mg/mL; DMSO:PBS (pH 7.2) (1:4): 0.2mg/mL
- form
- A solid
- pka
- 6.23±0.40(Predicted)
- color
- White to off-white
NSC781406 Usage And Synthesis
Description
NSC 781406 is a dual inhibitor of PI3K and mammalian target of rapamycin (mTOR; IC50s = 2.0, 9.4, 2.7, 14, and 5.4 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, and mTOR, respectively). It inhibits cell growth in the NCI-60 panel of cancer cell lines (mean GI50 = 65 nM). NSC 781406 (30 mg/kg) reduces tumor volume in a BEL-7404 hepatic cancer mouse xenograft model.
Uses
NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.
in vivo
In the xenograft models, treatment with 30 mg/kg of NSC781406 results in statistically significant antitumor activity, with a mean reduction in relative tumor volume ratio of 52%. Sorafenib displays an inhibition ratio of 44% at 50 mg/kg. NSC781406 is well tolerated at 30 mg/kg, with no observed mortality or significant reduction of body weight[1].
IC 50
PI3Kα: 2 nM (IC50); PI3Kγ: 2.7 nM (IC50); PI3Kβ: 9.4 nM (IC50); PI3Kδ: 14 nM (IC50); mTOR: 5.4 nM (IC50)
References
[1] Chen Y, et al. Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma. Bioorg Med Chem. 2016 Mar 1;24(5):957-66. DOI:10.1016/j.bmc.2016.01.008
NSC781406Supplier
- Tel
- sales@boylechem.com
- Tel
- 021-58955995
- sales@medchemexpress.cn
- Tel
- 021-52996696，15000506266 15000506266
- Tel
- 18800159827
- youcochem@163.com
- Tel
- 13816613772
- huahero21@sina.com
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