RAF709

CAS NO.：1628838-42-5
Empirical Formula: C28H29F3N4O4
Molecular Weight: 542.55
MDL number: MFCD30534393
Update Date: 2024-11-19 23:02:33

What is RAF709?

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.

Properties of RAF709

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

Safety information for RAF709

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07
GHS Hazard Statements	H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes	P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.