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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Raf-PLX8394
PLX8394

Chemical Structure : PLX8394

CAS No.: 1393466-87-9

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PLX8394 (Plixorafenib, PLX-8394)

货号: PC-72242Not For Human Use, Lab Use Only.

PLX8394 (Plixorafenib, PLX-8394) is a next-generation, orally available, small-molecule BRAF inhibitor with IC50 values of 3.8 nM, 14 nM and 23 nM for BRAF (V600E), WT BRAF and CRAF, respectively.

规格 价格 库存 数量
5 mg ￥780 In stock
10 mg ￥1180 In stock
25 mg ￥2180 In stock
50 mg ￥3580 In stock
100 mg ￥5580 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PLX8394 (Plixorafenib, PLX-8394) is a next-generation, orally available, small-molecule BRAF inhibitor with IC50 values of 3.8 nM, 14 nM and 23 nM for BRAF (V600E), WT BRAF and CRAF, respectively.
PLX8394 suppresses mutant BRAF cells without activating the MAPK pathway in cells bearing upstream activation, overcame several known mechanisms of resistance to first-generation RAF inhibitors.
PLX8394 inhibits ERK signaling by specifically disrupting BRAF-containing dimers, including BRAF homodimers and BRAF-CRAF heterodimers, but not CRAF homodimers or ARAF-containing dimers.
As a BRAF-specific dimer breaker, PLX8394 selectively inhibits ERK signaling in tumors driven by dimeric BRAF mutants, including BRAF fusions and splice variants as well as BRAF V600 monomers, but spares RAF function in normal cells in which CRAF homodimers can drive signaling.

物理化学性质&存储条件

分子量 542.54
分子式 C25H21F3N6O3S
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

(R)-N-(3-(5-(2-cyclopropylpyrimidin-5-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)-3-fluoropyrrolidine-1-sulfonamide

参考文献

1. Marimuthu A, et al. Nature. 2015 Oct 22;526(7574):583-6.

2. Tutuka CSA, et al. Mol Cancer. 2017 Jun 28;16(1):112.

3. Hartsough EJ, et al. Mol Cancer Ther. 2018 Jan;17(1):84-95.

4. Yao Z, et al. Nat Med. 2019 Feb;25(2):284-291.

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