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LY3009120pan-RAF and RAF dimer inhibitor

LY3009120

Catalog No. A8716
Size Price Stock Qty
5mg $103.00 In stock
25mg $335.00 In stock
100mg $699.00 In stock

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Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

LY3009120

Protocol

Cell experiment [1]:

Cell lines

A375 cells and HCT116 cells

Preparation method

This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.5 μM, 24, 72 h

Applications

LY3009120 suppresses the proliferation of melanoma cells with either BRAF or NRAS mutation. It also induces cell cycle G0/G1 arrest and apoptosis in tumor cells with RAS or BRAF mutation.

Animal experiment [1]:

Animal models

Female NIH nude rats bearing xenograft tumors

Dosage form

Oral administration, 5, 10, or 15 mg/kg, twice daily

Application

Treatment of rat bearing melanoma BRAF V600E A375 xenograft tumors by 5, 10, or 15 mg/kg, twice daily of LY3009120, induced tumor growth inhibition and regression in a dose-dependent manner.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Peng S B, Henry J R, Kaufman M D, et al. Inhibition of RAF isoforms and active dimers by LY3009120 leads to anti-tumor activities in RAS or BRAF mutant cancers[J]. Cancer Cell, 2015, 28(3): 384-398.

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Chemical Properties

Cas No. 1454682-72-4 SDF Download SDF
Chemical Name 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(2-methyl-7-(methylamino)pyrido[2,3-d]pyrimidin-3-yl)phenyl)urea
Canonical SMILES CC1=NC2=NC(NC)=NC=C2C=C1C3=CC(NC(NCCC(C)(C)C)=O)=C(F)C=C3C
Formula C23H29FN6O M.Wt 424.51
Solubility Soluble in DMSO Storage Store at -20°C
General tips N/A
Shipping Condition N/A

Background

LY3009120 is a pan-RAF and RAF dimer inhibitor. It inhibits BRAF WT, CRAF, WT, BRAFV600E, and BRAFV600E+G468A with the IC50 values of 9.1, 15, 5.8, and 17 nM, respectively. [1]

RAF is family of serine/threonine-protein kinase mediates Ras GTPases and the MAPK/ERK cascade. It involves in proliferation, differentiation, apoptosis, survival and oncogenic transformation. [1]

In NRAS mutant SK-Mel2 cells or KRAS mutant HCT116 cells, LY3009120 inhibits the kinase activity of CRAF in a dose-dependent manner and induces BRAF/CRAF heterodimerization. It also blocks Phospho-MEK and -ERK and induces minimal paradoxical activation in RAS mutant Cells. Moreover, treatment of BRAF V600E A375 melanoma cells by LY3009120 for 24 hr predominantly induces a G0/G1 arrest with more than 95% cells in G0/G1 phase. [1]

In nude rats bearing A375 xenograft tumors, oral LY3001920 treatment exerts a dose-dependent inhibition of phospho-MEK and –ERK. 15 or 30 mg/kg LY3009120 shows near complete tumor regression in nude rats bearing PDX tumors. [1]

Reference:
1.  Peng SB, Henry JR, Kaufman MD et al. Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers. Cancer Cell. 2015 Sep 14;28(3):384-98.