- NVP-BAG956
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- $1.00 / 1g
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2020-01-13
- CAS:853910-02-8
- Min. Order: 1g
- Purity: 99%
- Supply Ability: 1ton
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| α,α,-Dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile Basic information |
Product Name: | α,α,-Dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile | Synonyms: | BAG 956;α,α,-Dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile;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-pyridin-3-ylethynyl-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile,NVP-BAG;NVP-BAG 956
BAG 956;NVP-BAG956, >=98%;BAG956(NVP-BAG956);NVP-BAG956;BAG 956;NVP-BAG 956 | CAS: | 853910-02-8 | MF: | C28H21N5 | MW: | 427.51 | EINECS: | 200-258-5 | Product Categories: | Akt;mTOR;PI3K | Mol File: | 853910-02-8.mol | |
| α,α,-Dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile Chemical Properties |
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 |
| α,α,-Dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile Usage And Synthesis |
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 |
| α,α,-Dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile Preparation Products And Raw materials |
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