中文名 | BP-1-102 |
英文名 | BP-1-102 |
别名 | BP-1-102游离态 化合物BP-1-102 转录因子STAT3小分子抑制剂(BP-1-102) |
英文别名 | BP1-102 BP1-102 BP 1-102 BP-1-102 BP 1-102. STAT3 Inhibitor XVIII STAT3 INHIBITOR XVIII STAT3 Inhibitor XVIII, BP-1-102 4-(N-(4-Cyclohexylbenzyl)-2-(2,3,4,5,6-pentafluoro-N-methylphenylsulfonamido)acetamido)-2-hydr 4-(N-(4-cyclohexylbenzyl)-2-(2,3,4,5,6-pentafluoro-N-methylphenylsulfonamido)acetamido)-2-hydroxybenzoic acid Benzoic acid, 4-[[(4-cyclohexylphenyl)methyl][2-[methyl[(2,3,4,5,6-pentafluorophenyl)sulfonyl]amino]acetyl]amino]-2-hydroxy- |
CAS | 1334493-07-0 |
化学式 | C29H27F5N2O6S |
分子量 | 626.59 |
密度 | 1.474±0.06 g/cm3(Predicted) |
沸点 | 749.2±70.0 °C(Predicted) |
溶解度 | DMSO: ≥ 33 mg/mL |
酸度系数 | 3.15±0.10(Predicted) |
存储条件 | Inert atmosphere,Store in freezer, under -20°C |
体外研究 | BP-1-102 binds Stat3 with an affinity K D of 504 nM. BP-1-102 inhibits Stat3 DNA-binding activity in vitro , with an IC 50 value of 6.8±0.8 μM. It blocks Stat3-phospho-tyrosine peptide interactions and Stat3 activation at 4-6.8 μM, and selectively inhibits growth, survival, migration, and invasion of Stat3-dependent tumor cells. BP-1-102-mediated inhibition of aberrantly active Stat3 in tumor cells suppresses the expression of c-Myc, Cyclin D1, Bcl-xL, Survivin, VEGF, and Krüppel-like factor 8. |
体内研究 | Mice therapeutically given BP-1-102, an orally bioavailable compound targeting STAT3/NF-kB activation and cross-talk, exhibit reduced colon tumorigenesis and diminished expression of STAT3/NF-kB-activating cytokines in the neoplastic areas. BP-1-102 is orally bioavailable and that the agent accumulates in tumor tissues at levels sufficient to inhibit aberrantly active Stat3 functions and inhibit tumor growth. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.596 ml | 7.98 ml | 15.959 ml |
5 mM | 0.319 ml | 1.596 ml | 3.192 ml |
10 mM | 0.16 ml | 0.798 ml | 1.596 ml |
5 mM | 0.032 ml | 0.16 ml | 0.319 ml |
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