345987-15-7
345987-15-7 結(jié)構(gòu)式
基本信息
中文別名
AS601245.TFA鹽JNK抑制劑(AS601245)
ALPHA-[2-[[2-(3-吡啶基)乙基]氨基]-4-嘧啶基]-2-苯并噻唑乙腈
英文別名
CS-1619AS601245
AS601245.TFA
JNK Inhibitor V
2-Benzothiazoleacetonitrile, α-[2-[[2-(3-pyridinyl)ethyl]amino]-4-pyrimidinyl]-
alpha-[2-[[2-(3-Pyridinyl)ethyl]amino]-4-pyrimidinyl]-2-benzothiazoleacetonitrile
2-(1,3-benzothiazol-2-yl)-2-[2-(2-pyridin-3-ylethylamino)pyrimidin-4-yl]acetonitrile
所屬類別
生物化工：激動(dòng)劑抑制劑物理化學(xué)性質(zhì)
沸點(diǎn)635.6±65.0 °C(Predicted)
密度1.366±0.06 g/cm3(Predicted)
儲(chǔ)存條件Keep in dark place,Sealed in dry,Store in freezer, under -20°C
溶解度insoluble in H2O; insoluble in EtOH; ≥14.25 mg/mL in DMSO
酸度系數(shù)(pKa)5.32±0.10(Predicted)
形態(tài)白色至黃色固體
顏色Light yellow to yellow
常見問題列表
生物活性
AS601245 是一種口服活性、選擇性、ATP競(jìng)爭(zhēng)性的 JNK 抑制劑，IC50 分別為 150、220和 70 nM，對(duì)三種 JNK 人類亞型 (hJNK1、hJNK2和hJNK3)。AS601245 對(duì) c-src、CDK2 和 c-Raf 的選擇性為 10-20 倍，對(duì)一系列 Ser/Thr 和 Tyr 蛋白激酶的選擇性為 50-100 倍。具有神經(jīng)保護(hù)特性。靶點(diǎn)
|
hJNK1 150 nM (IC 50 ) |
hJNK2 220 nM (IC 50 ) |
hJNK3 70 nM (IC 50 ) |
體外研究
AS601245, an anti-Inflammatory JNK inhibitor, and Clofibrate have a synergistic effect in inducing cell responses and in affecting the gene expression profile in CaCo-2 colon cancer cells .
體內(nèi)研究
AS601245 (40, 60, and 80 mg/kg; i.p.) provides significant protection against the delayed loss of hippocampal CA1 neurons in a gerbil model of transient global ischemia.
AS601245 (0.3-10 mg/kg; p.o.) is a potent inhibitor of LPS-induced TNF-α release in mice.
| Animal Model: | C3H/HEN mice |
| Dosage: | 0.3, 1, 3, or 10 mg/kg |
| Administration: | P.o. |
| Result: | Decreased the TNF-α release in a dose-dependent manner. |