| Identification | Back 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 Properties | Back 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 | [InChI]
1S/C28H21N5/c1-19-32-26-17-31-25-13-8-20(6-7-21-5-4-14-30-16-21)15-24(25)27(26)33(19)23-11-9-22(10-12-23)28(2,3)18-29/h4-5,8-17H,1-3H3 | [InChIKey]
GVPAGJWVBUZHNQ-UHFFFAOYSA-N |
| Hazard Information | Back 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). | [IC 50]
PI3Kδ: 35 nM (IC50); PI3Kα: 56 nM (IC50); PI3Kγ: 117 nM (IC50); PI3Kβ: 446 nM (IC50); PDK1: 240 nM (IC50); VEGFR1: 2.56 μM (IC50) | [storage]
Store at -20°C |
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