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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Raf-LY3009120
LY3009120

Chemical Structure : LY3009120

CAS No.: 1454682-72-4

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LY3009120 (DP-4978;LY-3009120)

货号: PC-43107Not For Human Use, Lab Use Only.

LY3009120 (DP-4978) is a potent pan-RAF and RAF dimer inhibitor with IC50 of 5.8, 9.1 and 15 nM for BRAF V600E, BRAF WT and CRAF WT, respectively.

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10 mg ￥1880 In stock
25 mg ￥3180 In stock
50 mg ￥5280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

LY3009120 (DP-4978) is a potent pan-RAF and RAF dimer inhibitor with IC50 of 5.8, 9.1 and 15 nM for BRAF V600E, BRAF WT and CRAF WT, respectively.
LY3009120 (DP-4978) inhibits ARAF, BRAF, and CRAF isoforms with similar affinity (4, 31-47 and 42 nM for ARAF, BRAF and CRAF), induces BRAF-CRAF dimerization but inhibits the phosphorylation of downstream MEK and ERK, also inhibits various forms of RAF dimers including BRAF or CRAF homodimers.
LY3009120 (DP-4978) exhibits anti-proliferative effects on cell lines harboring BRAF V600E, KRAS G13 and KRAS G12 mutations, inhibits cell growth of H2405, BxPC-3, and OV-90 cells (IC50=0.04, 0.087, and 0.007 uM).
LY3009120 (DP-4978) displays significant activity in in vivo BRAF mut and KRAS mut CRC xenograft models.

物理化学性质&存储条件

分子量 424.5144
分子式 C23H29FN6O
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

DMSO: ≥ 38 mg/mL
Chemical Name/SMILES

Urea, N-(3,3-dimethylbutyl)-N'-[2-fluoro-4-methyl-5-[7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl]phenyl]-

参考文献

1. Henry JR, et al. J Med Chem. 2015 May 28;58(10):4165-79.

2. Peng SB, et al. Cancer Cell. 2015 Sep 14;28(3):384-98.

3. Chen SH, et al. Cancer Discov. 2016 Mar;6(3):300-15.

4. Vakana E, et al. Oncotarget. 2017 Feb 7;8(6):9251-9266.

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