RAF709

Base Information

Chemical Name:RAF709
CAS No.:1628838-42-5
Molecular Formula:C28H29F3N4O4
Molecular Weight:542.55
Hs Code.:2934999090
Mol file:1628838-42-5.mol

Synonyms:RAF709

Suppliers and Price of RAF709

Supply Marketing:

Business phase:: The product has achieved commercial mass production^*data from LookChem market partment

Manufacturers and distributors:

Manufacture/Brand
Chemicals and raw materials
Packaging
price

DC Chemicals
RAF709 >98%
1 g
$ 1800.00

DC Chemicals
RAF709 >98%
100 mg
$ 500.00

ChemScene
RAF709 99.91%
50mg
$ 490.00

ChemScene
RAF709 99.91%
5mg
$ 90.00

ChemScene
RAF709 99.91%
10mg
$ 150.00

ChemScene
RAF709 99.91%
100mg
$ 790.00

ChemScene
RAF709 99.91%
25mg
$ 300.00

Cayman Chemical
RAF709 ≥98%
10mg
$ 263.00

Cayman Chemical
RAF709 ≥98%
5mg
$ 140.00

Cayman Chemical
RAF709 ≥98%
1mg
$ 35.00

Total 16 raw suppliers

Chemical Property of RAF709

Chemical Property:

Boiling Point:622.7±55.0 °C(Predicted)
PKA:11.87±0.70(Predicted)
PSA：85.81000
Density:1.321±0.06 g/cm3(Predicted)
LogP:5.25550

Purity/Quality:

99%, ^*data from raw suppliers

RAF709 >98% ^*data from reagent suppliers

Safty Information:

Pictogram(s):
Hazard Codes:

MSDS Files:

Useful:

Description RAF709 is a potent inhibitor of B-RAF and C-RAF (IC50s = 0.4 and 0.5 nM, respectively). It is selective for RAF kinases exhibiting >99% inhibition of only B-RAF, B-RAFV600E, and C-RAF in a panel of 456 kinases. However, DDR1, DDR2, FRK, and PDGFRβ are also inhibited by >80% at a concentration of 1 μM. RAF709 inhibits phosphorylation of MEK and ERK (EC50s = 0.02 and 0.1 μM, respectively) with minimal paradoxical activation, stabilizes BRAF-CRAF dimers (EC50 = 0.8 μM), and reduces proliferation of Calu-6 RAS mutant cells (EC50 = 0.95 μM). In a Calu-6 mouse non-small cell lung cancer (NSCLC) xenograft model, RAF709 (10-200 mg/kg) reduces ERK phosphorylation and decreases tumor volume in a dose-dependent manner without affecting total body weight.

Technology Process of RAF709

There total 8 articles about RAF709 which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:

synthetic route:

Reference yield: 66.0%

: 2081-44-9
Tetrahydro-pyran-4-ol

: N-(6′-fluoro-2-methyl-5′-morpholino-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide

: 1628838-42-5
N-(2-methyl-5′-morpholino-6′-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide

Guidance literature:: Tetrahydro-pyran-4-ol; With sodium hydride; In mineral oil; at 20 ℃;

N-(6′-fluoro-2-methyl-5′-morpholino-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide; In mineral oil;
DOI:10.1021/acs.jmedchem.6b01862

Reference yield:

: 884495-22-1
3-amino-5-bromo-2-fluoropyridine

: 1628838-42-5
N-(2-methyl-5′-morpholino-6′-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide

Guidance literature:: Multi-step reaction with 3 steps

1.1: sodium hydride / N,N-dimethyl-formamide / 0.25 h / 0 - 20 °C

1.2: 3 h / 80 °C

2.1: dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH₂Cl₂; sodium carbonate / water; 1,2-dimethoxyethane / 1.5 h / 100 °C / Inert atmosphere

3.1: sodium hydride / mineral oil / 20 °C

With dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH₂Cl₂; sodium hydride; sodium carbonate; In 1,2-dimethoxyethane; water; N,N-dimethyl-formamide; mineral oil; 2.1: |Suzuki-Miyaura Coupling;
DOI:10.1021/acs.jmedchem.6b01862

Reference yield:

: 4-(5-bromo-2-fluoropyridin-3-yl)morpholine

: 1628838-42-5
N-(2-methyl-5′-morpholino-6′-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide

Guidance literature:: Multi-step reaction with 2 steps

1: dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH₂Cl₂; sodium carbonate / water; 1,2-dimethoxyethane / 1.5 h / 100 °C / Inert atmosphere

2: sodium hydride / mineral oil / 20 °C

With dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH₂Cl₂; sodium hydride; sodium carbonate; In 1,2-dimethoxyethane; water; mineral oil; 1: |Suzuki-Miyaura Coupling;
DOI:10.1021/acs.jmedchem.6b01862