2-(4,4-二氟-1-哌啶基)-6-甲氧基-N-[1-异丙基-4-哌啶基]-7-[3-(1-吡咯烷基)丙氧基]-4-喹唑啉胺
- CAS号:1481677-78-4
- 英文名:UNC-0642
- 中文名:2-(4,4-二氟-1-哌啶基)-6-甲氧基-N-[1-异丙基-4-哌啶基]-7-[3-(1-吡咯烷基)丙氧基]-4-喹唑啉胺
- CBNumber:CB12668368
- 分子式:C29H44F2N6O2
- 分子量:546.7
- MOL File:1481677-78-4.mol
- 沸点 :679.2±65.0 °C(Predicted)
- 密度 :1.23±0.1 g/cm3(Predicted)
- 储存条件 :2-8°C
- 溶解度 :Soluble to 100 mM in DMSO and to 50 mM in 1eq. HCl
- 酸度系数(pKa) :10.06±0.20(Predicted)
- 形态 :powder
- 颜色 :white to beige
- WGK Germany :3
2-(4,4-二氟-1-哌啶基)-6-甲氧基-N-[1-异丙基-4-哌啶基]-7-[3-(1-吡咯烷基)丙氧基]-4-喹唑啉胺性质、用途与生产工艺
- 生物活性 UNC0642是有效,选择性的赖氨酸甲基转移酶 G9a 和 GLP 抑制剂, 抑制 G9a 的IC50 值小于2.5 nM。
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靶点
IC50: <2.5 nM (G9a)
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体外研究
UNC0642 displays high in vitro and cellular potency, low cell toxicity, and excellent selectivity. UNC0642 is competitive with the peptide substrate and non-competitive with the cofactor SAM. The K i of UNC0642 is determined to be 3.7±1 nM. UNC0642 displays high in vitro potency for GLP (IC 50 < 2.5 nM), similar to G9a. UNC0642 is more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels. UNC0642 exhibits high potency at reducing the H3K9me2 mark, low cell toxicity, and good separation of functional potency and cell toxicity in a number of cell lines. It reduces clonogenicity in PANC-1 cells, a pancreatic carcinoma cell line.
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体内研究
A single intraperitoneal (IP) injection (5 mg/kg) of UNC0642 results in a plasma C max (maximum concentration) of 947 ng/mL and an AUC (area under the curve) of 1265 hr*ng/mL.
- 更新日期:2024/11/08
- 产品编号:HY-13980
- 产品名称:UNC0642
- CAS编号:
- 包装:1 mg
- 价格:340元
- 更新日期:2024/11/08
- 产品编号:HY-13980
- 产品名称:2-(4,4-二氟-1-哌啶基)-6-甲氧基-N-[1-异丙基-4-哌啶基]-7-[3-(1-吡咯烷基)丙氧基]-4-喹唑啉胺 UNC0642
- CAS编号:1481677-78-4
- 包装:5mg
- 价格:750元
- 公司名称:CLEARSYNTH LABS LTD.
- 联系电话:--
- 电子邮件:sales@clearsynth.com
- 国家:印度
- 产品数:6257
- 优势度:58
- 公司名称:A.J Chemicals
- 联系电话:--
- 电子邮件:sales@ajchem.in
- 国家:印度
- 产品数:6100
- 优势度:58
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