RAF709|RAF-709|Raf kinase inhibitor

Cas No.:	1628838-42-5
Chemical Name:	N-(2-methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide
Synonyms:	RAF-709,RAF 709
SMILES:	O=C(NC1=CN=C(C)C(C2=CC(N3CCOCC3)=C(OC4CCOCC4)N=C2)=C1)C5=CC(C(F)(F)F)=CC=C5
Formula:	C₂₈H₂₉F₃N₄O₄
M.Wt:	542.55
Sotrage:	4°C for 1 year, -20°C for more than 2 years

Description:	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].
In Vitro:	RAF709 stabilizes BRAF-CRAF dimers with an EC50 of 0.8 μM. In cellular assays, the dose-response of pMEK and pERK are measured in Calu-6 cells with EC50=0.02 and 0.1 μM with minimal paradoxical activation and inhibition of proliferation with EC50=0.95 μM[1].

Cat. No.	Product name	Field of application
DC47985	GNE-9815	GNE-9815 is among the most highly kinase-selective RAF inhibitors targeting KRAS mutant cancers via combination treatment.
DC7719	ZM336372	ZM 336372 is a potent and selective c-Raf inhibitor with IC50 of 70 nM, 10-fold selectivity over B-RAF, no inhibition to PKA/B/C, AMPK, p70S6, etc.
DC7307	TAK-632	TAK-632 is a selective pan-RAF kinase inhibitor with IC50 values of 2.4/1.4 nM for BRAF V600E/c-RAF; > 60 fold selectivity over VEGFR.
DC8791	Sorafenib free base (BAY-43-9006)	Sorafenib(BAY 43-9006) is a potent inhibitor of Raf-1 with IC50 values of 6 nM, 22 nM and 90 nM for Raf-1, B-Raf, and VEGFR2 respectively, BAY 43-9006 suppresses both wild-type and V599E mutant BRAF activity in vitro.
DC2098	Sorafenib (BAY-43-9006)	Sorafenib Tosylate (Bay 43-9006, Nexavar) is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.
DC7279	SB-590885	SB590885 is a potent B-Raf inhibitor with Ki of 0.16 nM, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases.
DC9987	RAF709	RAF709 is a novel Raf kinase inhibitor extracted from patent WO2014151616A1, compound example 131, has an IC50 of 0.5 and 1.8 nM for c-Raf and b-Raf, respectively.
DC5049	RAF265 (CHIR-265)	RAF265 (CHIR-265) is a highly selective B-Raf and VEGFR2 inhibitor with IC50 of 3-60 nM and EC50 of 30 nM, including B-Raf, C-Raf and mutant B-Raf.
DC9814	PLX7904(PB04)	PLX7904(PB04) is a potent and selective paradox-breaker RAF inhibitor.
DC6301	PLX-4720	PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.