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

产品咨询: sales@probechem.com
订购: order@probechem.com

首页-小分子抑制剂&激动剂-Tyrosine Kinase-RET Tyrosine Kinase (c-RET)-TPX-0046
TPX-0046

Chemical Structure : TPX-0046

CAS No.: 2359649-81-1

加入收藏

TPX-0046 (Enbezotinib, TPX0046)

货号: PC-73416Not For Human Use, Lab Use Only.

TPX-0046 (Enbezotinib) is a potent, selective next-generation RET/SRC inhibitor, demonstrates low nanomolar potency against WT and 18 RET mutations/fusions, as well as SRC, and is VEGFR2/KDR-sparing.

规格 价格 库存 数量
5 mg ￥2980 In stock
10 mg ￥4880 In stock
25 mg Get quote
100 mg Get quote
获取报价单
* 请选择数量再加入购物车
 or Bulk Inquiry

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

TPX-0046 (Enbezotinib) is a potent, selective next-generation RET/SRC inhibitor, demonstrates low nanomolar potency against WT and 18 RET mutations/fusions, as well as SRC, and is VEGFR2/KDR-sparing.
TPX-0046 inhibited RET phosphorylation (IC50 < 10 nM) in tumor cell lines (LC2/ad, CCDC6-RET; TT, RET C634W) and Ba/F3 engineered RET models (WT, G810R).
TPX-0046 inhibited KIF5B-RET Ba/F3, LC2/ad, and TT cells with IC50 values of 1 nM in cell proliferation assays.
TPX-0046 potently inhibited Ba/F3 RET engineered cells with SFMs (e.g. G810C/R/S) with mean proliferation IC50 of 1-17 nM.
TPX-0046 demonstrated marked in vivo anti-tumor efficacy in RET-driven cell-derived and patient-derived xenograft tumor models, a single dose of 5 mg/kg TPX-0046 inhibited >80% of RET phosphorylation.
TPX-0046 is a unique next-generation RET inhibitor that possesses potent in vitro and in vivo activity against a diverse range of RET alterations, including SFM-mediated resistance.

物理化学性质&存储条件

分子量 424.43
分子式 C21H21FN6O3
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

(13E,14E,15aS,18aR,5R)-35-fluoro-5-methyl-15,15a,16,17,18,18a-hexahydro-4-oxa-7-aza-1(5,3)-cyclopenta[b]pyrazolo[1',5':1,2]pyrimido[4,5-e][1,4]oxazina-3(3,2)-pyridinacyclooctaphan-8-one

参考文献

1. A.Drilon, et al. Annals of Oncology Volume 30, Supplement 5, October 2019, Pages v190-v191

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: