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

α,α,-Dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile 구조식 이미지
카스 번호:
853910-02-8
상품명:
α,α,-Dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile
동의어(영문):
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
분자식:
C28H21N5
포뮬러 무게:
427.51
MOL 파일:
853910-02-8.mol
MSDS 파일:
SDS

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

녹는점
>224oC (dec.)
끓는 점
694.8±65.0 °C(Predicted)
밀도
1.17
저장 조건
Store at RT
용해도
DMSO(약간 용해됨, 가열), 메탄올(약간 용해됨)
물리적 상태
오렌지 파우더
산도 계수 (pKa)
4.99±0.30(Predicted)
색상
하얀색

안전

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

용도

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.

일반 설명

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).

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

원자재

준비 용품


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

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