4-氨基1-叔丁基-3-(1'-萘甲基)吡唑并[3,4-D]嘧啶
中文名称 | 4-氨基1-叔丁基-3-(1'-萘甲基)吡唑并[3,4-D]嘧啶 |
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中文同义词 | 4-氨基1-叔丁基-3-(1'-萘甲基)吡唑并[3,4-D]嘧啶;突变型CDK7抑制剂(1-NM-PP1);1-(叔丁基)-3-(萘-1-基甲基)-1H-吡唑并[3,4-D]嘧啶-4-胺;4-氨基1-叔丁基-3-(1'-萘甲基)吡唑并[3,4-D]嘧啶 |
英文名称 | 1 NM-PP1 |
英文同义词 | 4-AMINO-1-TERT-BUTYL-3-(1'-NAPHTHYLMETHYL)PYRAZOLO[3,4-D]PYRIMIDINE;4-AMINO-1-TERT-BUYTL-3-(1-NAPHTHYLMETHYL)PYRAZOLO[3,4-D]PYRIMIDINE;1 NM-PP1;MUTANT KINASES INHIBITOR II;PP1 ANALOG II;1-(1,1-Dimethylethyl)-3-(1-naphthalenylmethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine;1-tert-Butyl-3-(naphthalen-1-ylmethyl)-1H-pyrazolo[3,4-D]pyrimidin-4-amine;Chebi:52309 |
CAS号 | 221244-14-0 |
分子式 | C20H21N5 |
分子量 | 331.41 |
EINECS号 | |
相关类别 | 小分子抑制剂,天然产物;小分子抑制剂;细胞生物学试剂;Inhibitors;Bases & Related Reagents;Intermediates & Fine Chemicals;Nucleotides;Pharmaceuticals;Tyrosine Kinase Inhibitors;API |
Mol文件 | 221244-14-0.mol |
结构式 |
4-氨基1-叔丁基-3-(1'-萘甲基)吡唑并[3,4-D]嘧啶 性质
熔点 | 175-176°C |
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沸点 | 545.7±45.0 °C(Predicted) |
密度 | 1.25±0.1 g/cm3(Predicted) |
储存条件 | Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
溶解度 | 氯仿(微溶)、甲醇(微溶、加热) |
酸度系数(pKa) | 4.50±0.30(Predicted) |
形态 | 白色固体 |
颜色 | 白色至米色 |
IC50: 4.3 nM (v-Src-as1), 3.2 nM (c-Fyn-as1), 28 μM (v-Src), 1 μM (c-Fyn), 3.4 μM (c-Abl), 29 μM (CDK2), 24 μM (CAMKII), 120 nM (cAbl-as2), 5 nM (CDK2-as1), 8 nM (CAMKII-as1)
Cdk7 from Cdk7 as/as or Cdk7 +/+ cells is immunoprecipitated and tested its kinase activity towards both a Pol II CTD-containing fusion protein (GST-CTD) and human Cdk2. Cdk7 recovered from the mutant, but not the wild-type, cells is inhibited by 1-NM-PP1 (1-NMPP1), with an IC 50 of ~50 nM with either substrate. Replacement of wild-type Cdk7 with Cdk7 as/as also rendered growth of HCT116 cells sensitive to 1-NM-PP1. In the absence of 1-NM-PP1, the wild-type and Cdk7 as/as cells had population doubling times of ~17.9 and ~20.2 h, respectively, with similar cell-cycle distributions in asynchronous culture, indicating minimal impairment of Cdk7 function by the F91G mutation per se. The homozygous Cdk7 as/as cells are sensitive to 1-NM-PP1, however, with an IC 50 ~100 nM measured by cell viability (MTT) assays performed after 96 h of 1-NM-PP1 exposure. In contrast, wild-type HCT116 cells are resistant to 10 μM 1-NM-PP1. Addition of 10 μM 1-NM-PP1 retards G1/S progression by the mutant but not the wild-type cells. When added simultaneously with serum to the Cdk7 as/as cells, 1-NM-PP1 prevents any progression into S phase in the next 15 h. After 24 h, there is evidence of progression into S-phase by a fraction of Cdk7 as/as cells released from serum starvation directly into medium containing 1-NM-PP1, while a fraction remained in G1. The addition of 1-NM-PP1 3 h or 6 h after serum addition delays S-phase entry by ~7 h or by ~3 h, respectively.
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-13942 | 1-NM-PP1 | 1 mg | 401元 | |
2024/08/19 | HY-13942 | 4-氨基1-叔丁基-3-(1'-萘甲基)吡唑并[3,4-D]嘧啶 1-NM-PP1 | 221244-14-0 | 5mg | 884元 |