ChemicalBook > CAS DataBase List > RAF709

RAF709

Product Name: RAF709
CAS No.: 1628838-42-5
Chemical Name: RAF709
Synonyms: RAF709;CS-2505;RAF-709;RAF 709;RAF709, 10 mM in DMSO;Inhibitor,inhibit,Raf,Raf kinases,RAF709,RAF-709,RAF 709;N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide;N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide;N-[2-Methyl-5'-(4-morpholinyl)-6'-[(tetrahydro-2H-pyran-4-yl)oxy][3,3'-bipyridin]-5-yl]-3-(trifluoromethyl)benzamide;Benzamide, N-[2-methyl-5'-(4-morpholinyl)-6'-[(tetrahydro-2H-pyran-4-yl)oxy][3,3'-bipyridin]-5-yl]-3-(trifluoromethyl)-
CBNumber: CB63155071
Molecular Formula: C28H29F3N4O4
Formula Weight: 542.55
MOL File: 1628838-42-5.mol

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RAF709 Property

Boiling point:: 622.7±55.0 °C(Predicted)
Density: 1.321±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO:100.0(Max Conc. mg/mL);184.31(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:2):0.33(Max Conc. mg/mL);0.61(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);55.29(Max Conc. mM)
Ethanol:100.0(Max Conc. mg/mL);184.31(Max Conc. mM)
form: A crystalline solid
pka: 11.87±0.70(Predicted)
color: White to off-white

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Safety

HS Code: 2934999090

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

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.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 23820
Product name: RAF709
Purity: ≥98%
Packaging: 1mg
Price: $44
Updated: 2024/03/01

Cayman Chemical

Product number: 23820
Product name: RAF709
Purity: ≥98%
Packaging: 5mg
Price: $172
Updated: 2024/03/01

Cayman Chemical

Product number: 23820
Product name: RAF709
Purity: ≥98%
Packaging: 10mg
Price: $321
Updated: 2024/03/01

AK Scientific

Product number: 3613EB
Product name: N-[6-Methyl-5-[5-morpholin-4-yl-6-(oxan-4-yloxy)pyridin-3-yl]pyridin-3-yl]-3-(trifluoromethyl)benzamide
Packaging: 10mg
Price: $455
Updated: 2021/12/16

Axon Medchem

Product number: Axon2817
Product name: RAF709
Purity: 99%
Packaging: 50mg
Price: $462
Updated: 2021/12/16

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RAF709 Chemical Properties,Usage,Production

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-RAF^V600E, 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.

Uses

RAF709 is a potent, selective, and efficacious RAF inhibitor with IC50s of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively[1]. Antitumor efficacy[1].

in vivo

RAF709 proves to be soluble, kinase selective, and efficacious in a KRAS mutant xenograft model. RAF709 shows dose-proportional increases in plasma exposure and a corresponding dosedependent inhibition of pERK in Calu-6 tumors. Treatment with RAF709 results in dose-dependent antitumor activity with 10 mg/kg being subefficacious (%T/C=92%), 30 mg/kg results in measurable antitumor activity (%T/C=46%), and 200 mg/kg results in mean tumor regression of 92%, while the same high dose is not efficacious in the PC3, KRAS WT model^[1].

IC 50

CRAF: 0.5 nM (IC₅₀); Braf: 0.4 nM (IC₅₀)

References

[1] Nishiguchi GA, et al. Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers. J Med Chem. 2017 Jun 22;60(12):4869-4881. DOI:10.1021/acs.jmedchem.6b01862

RAF709 Preparation Products And Raw materials

Raw materials

Preparation Products

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1628838-42-5, RAF709Related Search:

RAD140 XMD16-5 GNE-3511 BAY-876 Acebilustat BETA-LAPACHONE TAK 599

CS-2505

RAF-709;RAF 709

RAF709

Benzamide, N-[2-methyl-5'-(4-morpholinyl)-6'-[(tetrahydro-2H-pyran-4-yl)oxy][3,3'-bipyridin]-5-yl]-3-(trifluoromethyl)-

N-[2-Methyl-5'-(4-morpholinyl)-6'-[(tetrahydro-2H-pyran-4-yl)oxy][3,3'-bipyridin]-5-yl]-3-(trifluoromethyl)benzamide

Inhibitor,inhibit,Raf,Raf kinases,RAF709,RAF-709,RAF 709

N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide

RAF709, 10 mM in DMSO

N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide

1628838-42-5

C28H29F3N4O4