α,α,-Dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile
- Product Name
- α,α,-Dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile
- CAS No.
- 853910-02-8
- Chemical Name
- α,α,-Dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile
- 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;NVP BAG956,NVPBAG956,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
- CBNumber
- CB92518951
- Molecular Formula
- C28H21N5
- Formula Weight
- 427.51
- 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 Property
- 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
N-Bromosuccinimide Price
- Product number
- 528121
- Product name
- PI 3-K/PDK-1 Inhibitor, NVP-BAG956 - CAS 853910-02-8 - Calbiochem
- Packaging
- 5mg
- Price
- $251
- Updated
- 2023/01/07
- Product number
- 24195
- Product name
- NVP-BAG956
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $37
- Updated
- 2024/03/01
- Product number
- 24195
- Product name
- NVP-BAG956
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $151
- Updated
- 2024/03/01
- Product number
- 24195
- Product name
- NVP-BAG956
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $231
- Updated
- 2024/03/01
- Product number
- 3606
- Product name
- BAG956
- Purity
- ≥99%(HPLC)
- Packaging
- 10
- Price
- $263
- Updated
- 2021/12/16
α,α,-Dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile Chemical Properties,Usage,Production
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
Raw materials
Preparation Products
α,α,-Dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile Suppliers
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- Product
- NVP-BAG956 853910-02-8
- Price
- US $1.00/g
- Min. Order
- 1g
- Purity
- 99%
- Supply Ability
- 1ton
- Release date
- 2020-01-10