2-[(1S)-1-[(2-氨基-9H-嘌呤-6-基)氨基]乙基]-5-甲基-3-(2-甲基苯基)-4(3H)-喹唑啉酮盐酸盐
中文名称 | 2-[(1S)-1-[(2-氨基-9H-嘌呤-6-基)氨基]乙基]-5-甲基-3-(2-甲基苯基)-4(3H)-喹唑啉酮盐酸盐 |
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中文同义词 | 2-[(1S)-1-[(2-氨基-9H-嘌呤-6-基)氨基]乙基]-5-甲基-3-(2-甲基苯基)-4(3H)-喹唑啉酮盐酸盐;PI3K抑制剂(CAL-130 HYDROCHLORIDE);化合物 T10660L |
英文名称 | (S)-2-(1-((2-aMino-9H-purin-6-yl)aMino)ethyl)-5-Methyl-3-(o-tolyl)quinazolin-4(3H)-one hydrochloride |
英文同义词 | (S)-2-(1-((2-aMino-9H-purin-6-yl)aMino)ethyl)-5-Methyl-3-(o-tolyl)quinazolin-4(3H)-one hydrochloride;CAL-130 (Hydrochloride);2-[(1S)-1-[(2-Amino-9H-purin-6-yl)amino]ethyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone hydrochloride (1:1);CAL-130 HCl;CAL130 Hydrochloride,CAL 130 Hydrochloride |
CAS号 | 1431697-78-7 |
分子式 | C23H23ClN8O |
分子量 | 462.94 |
EINECS号 | |
相关类别 | 细胞生物学试剂 |
Mol文件 | 1431697-78-7.mol |
结构式 |
2-[(1S)-1-[(2-氨基-9H-嘌呤-6-基)氨基]乙基]-5-甲基-3-(2-甲基苯基)-4(3H)-喹唑啉酮盐酸盐 性质
储存条件 | Store at -20°C |
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溶解度 | 溶于二甲基亚砜 |
形态 | 粉末 |
颜色 | 浅黄至黄色 |
p110δ 1.3 nM (IC 50 ) |
p110γ 6.1 nM (IC 50 ) |
p110β 56 nM (IC 50 ) |
p110α 115 nM (IC 50 ) |
CAL-130 preferentially inhibits the function of both p110γ and p110δ catalytic domains. IC 50 values of CAL-130 are 1.3 and 6.1 nM for p110δ and p110γ, respectively, as compared to 115 and 56 nM for p110α and p110β. CAL-130 does not inhibit additional intracellular signaling pathways (i.e., p38 MAPK or insulin receptor tyrosine kinase) that are critical for general cell function and survival.
The clinical significance of interfering with the combined activities of PI3Kγ and PI3Kδ is determined by administering CAL-130 to Lck/Pten fl/fl mice with established T cell acute lymphoblastic leukemia (T-ALL). Candidate animals for survival studies are ill appearing, have a white blood cell (WBC) count above 45,000 μL -1 , evidence of blasts on peripheral smear, and a majority of circulation cells (>75%) staining double positive for Thy1.2 and Ki-67. Mice receive an oral dose (10 mg/kg) of CAL-130 every 8 hr for a period of 7 days and are then followed until moribund. Despite the limited duration of therapy, CAL-130 is highly effective in extending the median survival for treated animals to 45 days as compared 7.5 days for the control group.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-16122B | 2-[(1S)-1-[(2-氨基-9H-嘌呤-6-基)氨基]乙基]-5-甲基-3-(2-甲基苯基)-4(3H)-喹唑啉酮盐酸盐 CAL-130 Hydrochloride | 1431697-78-7 | 2mg | 1773元 |
2024/08/19 | HY-16122B | 2-[(1S)-1-[(2-氨基-9H-嘌呤-6-基)氨基]乙基]-5-甲基-3-(2-甲基苯基)-4(3H)-喹唑啉酮盐酸盐 CAL-130 Hydrochloride | 1431697-78-7 | 5mg | 2660元 |