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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; 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;Urea, N-(3,3-dimethylbutyl)-N'-[2-fluoro-4-methyl-5-[7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl]phenyl]-
CBNumber:
CB72725629
Molecular Formula:
C23H29FN6O
Molecular Weight:
424.51
MDL Number:
MFCD28411374
MOL File:
1454682-72-4.mol
Last updated:2023-06-30 15:45:59

LY-3009120 Properties

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)
FDA UNII 1GDT36RARO

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P264-P270-P271-P280-P301+P312-P302+P352-P304+P340-P305+P351+P338-P330-P332+P313-P337+P313-P362-P403+P233-P405-P501
HS Code  2933998090

LY-3009120 price More Price(24)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 21504 LY3009120 ≥98% 1454682-72-4 5mg $141 2024-03-01 Buy
Cayman Chemical 21504 LY3009120 ≥98% 1454682-72-4 10mg $253 2024-03-01 Buy
Cayman Chemical 21504 LY3009120 ≥98% 1454682-72-4 25mg $558 2024-03-01 Buy
Cayman Chemical 21504 LY3009120 ≥98% 1454682-72-4 50mg $979 2024-03-01 Buy
Tocris 6854 LY3009120 ≥98%(HPLC) 1454682-72-4 10 $101 2021-12-16 Buy
Product number Packaging Price Buy
21504 5mg $141 Buy
21504 10mg $253 Buy
21504 25mg $558 Buy
21504 50mg $979 Buy
6854 10 $101 Buy

LY-3009120 Chemical Properties,Uses,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]

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

Global( 84)Suppliers
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ATK CHEMICAL COMPANY LIMITED
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Aladdin Scientific
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LY-3009120 Spectrum

LY-3009120 Urea, 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]- DP 4978 N-(3,3-Dimethylbutyl)-N'-[2-fluoro-4-methyl-5-[7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl]phenyl]urea LY3009120; LY-3009120; LY 3009120; DP-4978; DP 4978; DP4978 CS-1616 LY-3009120(DP-4978) LY03009120(DP-4978) Raf kinases,DP 4978,inhibit,LY-3009120,DP4978,Autophagy,LY3009120,Raf,LY 3009120,Inhibitor 1454682-72-4 C23H29FN6O