|1-(4-(4-氨基-1-异丙基-1H-吡唑并[3,4-d]嘧啶-3-基)苯基)-3-(2-氟-5-(三氟甲基)苯基)脲|CsnPharm

CAS No.: 1384071-99-1

1-(4-(4-Amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)phenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea Catalog No. CSN22316

Synonyms: AD80

AD80 is a multikinase inhibitor with inhibitions on RET, RAF, SRC and S6K.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述AD80 is a multikinase inhibitor targeting on RET, RAF, SRC and S6K, eliminated its binding with TOR. Oral administration of AD80 resulted in a notable 70–90% of animals developing to adulthood in our Drosophila ptc>dRet^MEN2B model. It restored Src and Ras activities by the ectopic Src activation and thus strongly suppressed wing vein pattern phenotypes. AD80 inhibited proliferation of MZ-CRC-1 and TT thyroid cancer cells in culture, probably through the induction of apoptosis, with potent downregulation of phosphorylated Ret and several downstream biomarkers. AD80 also promoted enhanced tumour growth inhibition and reduced body-weight modulation relative to vandetanib in a mouse xenograft model. AD80 showed high activity in RET kinase gatekeeper mutant cells, Ba/F3 cells expressing KIF5B-RET^V804M or CCDC6-RET^V804M and inhibited phosphorylation of RET as well as of ERK, AKT, and S6K in these cells.
作用机制AD80 specifically targets RET and tightly binds to RET fusion kinase, effectively inhibiting RET kinase in DFG-out conformation.^[1]
动物研究
剂量
Mice: 20 mg/kg^[3] (i.p.); 30 mg/kg^[1] (p.o.)

给药途径
i.p., p.o.
参考文献

动物研究
剂量	Mice: 20 mg/kg^[3] (i.p.); 30 mg/kg^[1] (p.o.)
给药途径	i.p., p.o.

[1] Dar AC, Das TK, et al. Chemical genetic discovery of targets and anti-targets for cancer polypharmacology. Nature. 2012 Jun 6;486(7401):80-4.
[2] Plenker D, Riedel M, et al. Drugging the catalytically inactive state of RET kinase in RET-rearranged tumors. Sci Transl Med. 2017 Jun 14;9(394). pii: eaah6144.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1123 mL
- 10.5613 mL
- 21.1226 mL
- 5 mM
- 0.4225 mL
- 2.1123 mL
- 4.2245 mL
- 10 mM
- 0.2112 mL
- 1.0561 mL
- 2.1123 mL

技术信息

CAS号

1384071-99-1

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H19F4N7O

运输

蓝冰

分子量

473.43

别名

AD80

溶解度

DMSO	25.0 mg/mL (52.8 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	0.5 mg/mL	clear
PO	0.5% CMC-Na	45 mg/mL	suspension

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

1-(4-(4-Amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)phenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea Catalog No. CSN22316

靶点选择性

请登录您的专属账户

确认信息