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-Ras-Raf-MAPK-ERK Pathway-Raf-LXH254
LXH254

Chemical Structure : LXH254

CAS No.: 1800398-38-2

加入收藏

LXH254 (Naporafenib, LXH-254)

货号: PC-35635Not For Human Use, Lab Use Only.

LXH254 (Naporafenib, LXH 254) is a highly potent, selective B/C RAF inhibitor with Kd of 1.3/3.6 nM respectively, shows less activity against ARAF.

规格 价格 库存 数量
5 mg ￥1180 In stock
10 mg ￥1980 In stock
25 mg ￥3280 In stock
50 mg ￥5280 In stock
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

LXH254 (Naporafenib, LXH 254) is a highly potent, selective B/C RAF inhibitor with Kd of 1.3/3.6 nM respectively, shows less activity against ARAF.
LXH254 (Naporafenib) inhibits pMEK and cell proliferation in Calu-6 cells with EC50 of 0.014 uM and 0.47 uM, respectively
LXH254 (Naporafenib) showed a high level of selectivity on a panel of 456 kinases, demonstrating greater than 98% on-target binding to BRAF, BRAFV600E, and CRAF at 1 uM and very few off-targets, with DDR1 (>99%), DDR2 (84%), and PDGFRb (>99%) the only kinases with binding >80% at 1 uM.
LXH254 (Naporafenib) was active in models harboring BRAF alterations, including atypical BRAF alterations coexpressed with mutant K/NRAS, and NRAS mutants, but had only modest activity in KRAS mutants. LXH254 caused paradoxical activation of MAPK signaling in a manner similar to dabrafenib in cells expressing only ARAF.
LXH254 (Naporafenib) demonstrated tumor regression in the Calu-6 xenograft nude rat model.

物理化学性质&存储条件

分子量 502.494
分子式 C25H25F3N4O4
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

N-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide

参考文献

1. Monaco KA, et al. Clin Cancer Res. 2021 Apr 1;27(7):2061-2073.
2. Ramurthy S, et al. J Med Chem. 2020 Mar 12;63(5):2013-2027.
3. Negrao MV, et al. J Thorac Oncol. 2020 Oct;15(10):1611-1623.

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: