ChemicalBook > CAS DataBase List > NSC781406

NSC781406

Product Name: NSC781406
CAS No.: 1676893-24-5
Chemical Name: NSC781406
Synonyms: NSC781406;NSC-781406;NSC 781406;NSC781406, 10 mM in DMSO;NSC781406;NSC-781406;NSC 781406;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;Benzenesulfonamide, 2,4-difluoro-N-[2-methoxy-5-[4-[3-[4-(methylsulfonyl)-1-piperazinyl]-1-propyn-1-yl]-6-quinolinyl]-3-pyridinyl]-
CBNumber: CB43334188
Molecular Formula: C29H27F2N5O5S2
Formula Weight: 627.68
MOL File: 1676893-24-5.mol

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NSC781406 Property

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

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 29226
Product name: NSC 781406
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 29226
Product name: NSC 781406
Packaging: 10mg
Price: $261
Updated: 2024/03/01

Cayman Chemical

Product number: 29226
Product name: NSC 781406
Packaging: 5mg
Price: $139
Updated: 2024/03/01

ChemScene

Product number: CS-6958
Product name: NSC781406
Purity: 99.91%
Packaging: 1mg
Price: $60
Updated: 2021/12/16

ChemScene

Product number: CS-6958
Product name: NSC781406
Purity: 99.91%
Packaging: 5mg
Price: $120
Updated: 2021/12/16

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NSC781406 Chemical Properties,Usage,Production

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

NSC781406 Preparation Products And Raw materials

Raw materials

Preparation Products

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NSC781406 Suppliers

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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

1676893-24-5

C29H27F2N5O5S2