欢迎访问ProbeChem中文网站,英文网站请访问www.probechem.com

首页-小分子抑制剂&激动剂-Tyrosine Kinase-Bcr-Abl-Olverembatinib
Olverembatinib

Chemical Structure : Olverembatinib

CAS No.: 1257628-77-5

Olverembatinib (HQP1351, GZD824, HQP-1351, GZD-824)

货号: PC-38306Not For Human Use, Lab Use Only.

Olverembatinib (HQP1351, GZD824) is an orally bioavailable multikinase inhibitor targeting a broad spectrum of mutant KIT kinases (KIT-V559D IC50=1.4 nM).

规格 价格 库存 数量
10 mg ¥1180 In stock
25 mg ¥1980 In stock
50 mg ¥3280 In stock
100 mg Get quote

大包装,大折扣!

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Olverembatinib (HQP1351, GZD824) is an orally bioavailable multikinase inhibitor targeting a broad spectrum of mutant KIT kinases (KIT-V559D IC50=1.4 nM).
Olverembatinib (HQP1351, GZD824) also inhibits Bcr-Abl (WT) and Bcr-Abl (T315I) with IC50 of 0.34 nM and 0.68 nM, respectively.
Olverembatinib (HQP1351, GZD824) strongly inhibited wild-type KIT kinase and KIT kinases with primary mutations within exon 11 (L576P and V559D), with an inhibition rate of over 90% at 10 nM.
Olverembatinib (HQP1351, GZD824) showed strong inhibitory effect on KIT kinase with secondary mutations in the ATP-binding pocket (V559D/T670I and V559D/V654A).
The inhibition rates on KIT with A-loop mutations (A829P, D816H and D816 V) were relatively weaker at 10 nM (20–40%).
Olverembatinib (HQP1351, GZD824) exhibited potent binding affinities to additional kinases at 10 nM, including BRAF (V600E), DDR1, FLT3, PDGFRB, RET (M918T), TAK1 and TIE2.
Olverembatinib (HQP1351, GZD824) shows antiproliferative activity in GIST cells with KIT mutations (GIST T1 cells IC50=27 nM), inhibits colony formation, cell migration and invasion, induces cell cycle arrest and cell apoptosis, regulates KIT oncogenic signaling proteins in vitro.
Olverembatinib (HQP1351, GZD824) exhibits antitumor activity in GIST xenograft models in vivo. Olverembatinib (HQP1351) also is a potent Omicron NTD-mediated cytokine release inhibitor.

物理化学性质&存储条件

分子量 532.22
分子式 C29H27F3N6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-Methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]benzamide

参考文献

1. Liu X, et al. Cell Biosci. 2019 Oct 26;9:88.

2. Fang DD, et al. Transl Oncol. 2022 Jan;15(1):101244.

备案号:沪ICP备16042516号-1 Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright

联系我们 sales@probechem.com

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • *Additional Information:

询单

  • *产品名称:
  • *姓名:
  • *邮箱:
  • *公司名称:
  • *询单数量:
  • *国籍:
  • 询单信息: