LY-3009120
- Product Name
- LY-3009120
- CAS No.
- 1454682-72-4
- Chemical Name
- LY-3009120
- Synonyms
- DP 4978;CS-1616;LY-3009120;LY03009120(DP-4978);LY-3009120（DP-4978）;LY3009120, 10 mM in DMSO;LY3009120; LY-3009120; LY 3009120; DP-4978; DP 4978; DP4978;Raf kinases,DP 4978,inhibit,LY-3009120,DP4978,Autophagy,LY3009120,Raf,LY 3009120,Inhibitor;N-(3,3-dimethylbutyl)-N'-[2-fluoro-4-methyl-5-[7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl]phenyl]-;N-(3,3-Dimethylbutyl)-N'-[2-fluoro-4-methyl-5-[7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl]phenyl]urea
- CBNumber
- CB72725629
- Molecular Formula
- C23H29FN6O
- Formula Weight
- 424.51
- MOL File
- 1454682-72-4.mol
LY-3009120 Property
- Density
- 1?+-.0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- insoluble in H2O; insoluble in EtOH; ≥4.25 mg/mL in DMSO with gentle warming and ultrasonic
- form
- solid
- pka
- 13.52±0.70(Predicted)
- color
- Light yellow to khaki
- InChIKey
- HHCBMISMPSAZBF-UHFFFAOYSA-N
- SMILES
- N(CCC(C)(C)C)C(NC1=CC(C2C(C)=NC3C(C=2)=CN=C(NC)N=3)=C(C)C=C1F)=O
Safety
- HS Code
- 2933998090
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P330Rinse mouth.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- SML3055
- Product name
- LY3009120
- Purity
- ≥98% (HPLC)
- Packaging
- 10mg
- Price
- $121
- Updated
- 2025/07/31
- Product number
- SML3055
- Product name
- LY3009120
- Purity
- ≥98% (HPLC)
- Packaging
- 50mg
- Price
- $391
- Updated
- 2025/07/31
- Product number
- 21504
- Product name
- LY3009120
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $141
- Updated
- 2024/03/01
- Product number
- 21504
- Product name
- LY3009120
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $253
- Updated
- 2024/03/01
- Product number
- 21504
- Product name
- LY3009120
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $558
- Updated
- 2024/03/01
LY-3009120 Chemical Properties,Usage,Production
Uses
LY 3009120 is a potent pan-Rad inhibitor used in the inhibition of tumors. Dose-dependant inhibition.
Definition
ChEBI: LY3009120 is a member of the class of pyridopyrimidines that is pyrido[2,3-d]pyrimidine substituted by methylamino, 5-{[(3,3-dimethylbutyl)carbamoyl]amino}-4-fluoro-2-methylphenyl, and methyl groups at positions 2, 6 and 7, respectively. It is a potent pan RAF inhibitor which inhibits BRAF(V600E), BRAF(WT) and CRAF(WT) (IC50 = 5.8, 9.1 and 15 nM, respectively). It also inhibits RAF homo- and heterodimers and exhibits anti-cancer properties. It has a role as a necroptosis inhibitor, an apoptosis inducer, an antineoplastic agent, a B-Raf inhibitor and an autophagy inducer. It is a pyridopyrimidine, a biaryl, an aromatic amine, a member of phenylureas, a member of monofluorobenzenes, an aminotoluene and a secondary amino compound.
Biological Activity
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]
Synthesis
1454682-74-6
1454682-77-9
1454682-72-4
GENERAL PROCEDURE: 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)urea (25.9 g, 68.5 mmol), 7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl trifluoromethanesulfonate (22.09 g 68.5 mmol) and sodium bicarbonate (17.28 g, 206 mmol) were dissolved in a solvent mixture of 1,4-dioxane (500 mL) and water (125 mL) and bubbled under argon protection for 20 min. Tetrakis(triphenylphosphine)palladium (3.96 g, 3.43 mmol) was added and the reaction was heated at 50 °C under argon atmosphere. Subsequently 7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl trifluoromethanesulfonate (300 mg, 0.55 mmol) was added by supplementation and heating was continued at 50 °C overnight. After completion of the reaction, the mixture was cooled to room temperature, the solid was collected by filtration and washed sequentially with water and ether. The resulting solid was treated with acetonitrile (50 mL) and stirred at 80 °C for 30 min, the solid was again collected by filtration, washed with acetonitrile and dried in vacuum at 80 °C to give a light yellow solid. The solid was further treated with methanol (50 mL), heated at 80 °C for 1 h. After cooling to room temperature, the solid was filtered, washed with methanol (20 mL) and dried under vacuum to afford the target product 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (22.5 g, yield 77%), as a light yellow solid. Mass spectrum (m/z): 425.2 (M + 1).
in vivo
LY3009120 (20 mg/kg bid) displays significant activity in in vivo BRAFmut and KRASmut CRC xenograft models. In Colo 205 xenografts (BRAFmut), LY3009120 results in statistically significant tumor regression, while treatment of HCT 116 xenografts (KRASmut) results in statistically significant inhibition of tumor growth. LY3009120 treatment reduces pMEK1/2 in all HT-29 xenografts and reduces pERK1/2 in the majority of HT-29 xenografts[1]. LY3009120 (15 or 30 mg/kg) achieves almost complete tumor growth regression, and inhibits downstream phospho-MEK and ERK by approximately 70% and 60%, respectively, in the H2405 model[2].
IC 50
BRafV600E: 5.8 nM (IC50); Braf: 9.1 nM (IC50); CRAF: 15 nM (IC50)
storage
Store at -20°C
References
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.
LY-3009120 Preparation Products And Raw materials
Raw materials
Preparation Products
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