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Chemical Structure : LY3009120
CAS No.: 1454682-72-4
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $188 | In stock | |
| 25 mg | $318 | In stock | |
| 50 mg | $528 | In stock | |
| 100 mg | Get quote | ||
| 200 mg | Get quote | ||
| 1 g | Get quote |
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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.
| M.Wt | 424.5144 | |
| Formula | C23H29FN6O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: ≥ 38 mg/mL |
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| 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]- |
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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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