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853910-02-8

853910-02-8 Structure

853910-02-8 Structure
IdentificationBack Directory
[Name]

α,α,-Dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile
[CAS]

853910-02-8
[Synonyms]

CS-437
BAG 956
NVP-BAG 956
NVP-BAG956, >=98%
BAG956(NVP-BAG956)
NVP-BAG 956 BAG 956
NVP-BAG956;BAG 956;NVP-BAG 956
PI 3-K/PDK-1 Inhibitor, NVP-BAG956 - CAS 853910-02-8 - Calbiochem
2-Methyl-2-[4-[2-methyl-8-[(pyridin-3-yl)ethynyl]imidazo[4,5-c]quinolin-1-yl]phenyl]propionitrile
2-methyl-2-[4-[2-methyl-8-(2-pyridin-3-ylethynyl)imidazo[4,5-c]quinolin-1-yl]phenyl]propanenitrile
2-Methyl-2-(4-(2-Methyl-8-(pyridin-3-ylethynyl)-1H-iMidazo[4,5-c]quinolin-1-yl)phenyl)propanenitrile
2-Methyl-2-[4-(2-methyl-8-pyridin-3-ylethynyl-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile,NVP-BAG
α,α,-Dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile
Benzeneacetonitrile, α,α-dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-
[EINECS(EC#)]

200-258-5
[Molecular Formula]

C28H21N5
[MDL Number]

MFCD16618394
[MOL File]

853910-02-8.mol
[Molecular Weight]

427.51
Chemical PropertiesBack Directory
[Melting point ]

>224oC (dec.)
[Boiling point ]

694.8±65.0 °C(Predicted)
[density ]

1.17
[storage temp. ]

Store at RT
[solubility ]

DMSO (Slightly, Heated), Methanol (Slightly)
[form ]

Orange powder
[pka]

4.99±0.30(Predicted)
[color ]

White
Hazard InformationBack Directory
[Uses]

NVP-BAG956 acts as a rapamycin inhibitor used in the treatment of various melanomas through cell-induced apoptosis. Also used in antileukemic therapies as a dual PI3K/PDK-1 inhibitor.
[General Description]

A cell-permeable imidazoquinoline compound that acts as a potent, reversible, and ATP-competitive PI 3-K/PDK1 dual kinase inhibitor (IC50 = 56, 446, 35, 117, and 245 nM against p110α, p110β, p110δ, p110γ, and PDK1, respectively), displaying much reduced potency against VEGFR1 (IC50 = 2.56 μM) and little or no activity toward a panel of 15 other kinases (IC50 >10 μM). Shown to effectively inhibit the constitutive phosphorylation of PKB (T308 & S473; IC50 ≤45 nM) as well as PKB downstream effectors GSK3β (S9), FKHRL1 (T32), and p70S6K (T389) in human glioma U87MG and adeonocarcinoma PC3M cultures with PTEN deletion in vitro and retard PC3M-derived tumor growth in mice (by 50%; 75 mg/kg; twice per day p.o.) in vivo. Also reported to exhibit antiproliferative activities against BCRF-ABL- and mutant FLT3-expressing cells either alone or in combination with other PI3K/AKT, mTOR, and tyrosine kinase inhibitors, LY294002 (Cat. Nos. 440202 & 440204), Rapamycin (Cat. No. 553210), and PKC412 (Cat. No. 539648).
[storage]

Store at -20°C
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