Raf

<p>B-Raf IN 1 is a B-Raf (IC50: 24 nM) and c-Raf (IC50: 25 nM) inhibitor.</p>

<p>SGX-523 is a selective Met inhibitor (IC50: 4 nM), no inhibitory to Abl, BRAFV599E, p38α, and c-Raf.</p>

<p>Vemurafenib (RG7204) is a B-RAF inhibitor that inhibits RAFV600E and c-RAF-1 (IC50=31/48 nM) selectively and potently.</p>

<p>LY3009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. Phase 1.</p>

<p>PROTAC BRAF-V600E degrader-1 (Compound 23) selectively induces degradation of BRAF-V600E but not wildtype BRAF.</p>

<p>Dabrafenib (GSK2118436A) is a Raf inhibitor that inhibits C-Raf and B-RafV600E (IC50=5/0.6 nM) and is ATP-competitive.</p>

<p>Dabrafenib Mesylate (GSK2118436 Mesylate) is a B-Raf inhibitor(IC50s of 0.6 and 5.0 nM for RafV600E and c-Raf, respectively).</p>

Doramapimod (BIRB 796) is a highly potent inhibitor of p38 MAPK (Kd: 0.1 nM), but weakly inhibits c-RAF, Fyn, Lck, ERK-1, SYK, IKK2, and ZAP-70.

<p>TAK-580 (MLN2480) is an oral, selective pan-Raf kinase inhibitor in Clinicalal trials.</p>

<p>Regorafenib HCl (BAY73-4506) is an oral inhibitor targeting angiogenic, stromal, and cancer kinases with strong antitumor effects.</p>

<p>AZ628 is a new pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc.</p>

<p>Raf inhibitor 1 dihydrochloride (B-Raf inhibitor 1 dihydrochloride) is a potent and selective B-Raf inhibitor.</p>

<p>B-Raf inhibitor 1 (B-Raf inhibitor 1) is a potent and selective B-Raf inhibitor.</p>

TBAP-001 is a RAF kinase inhibitor, with an IC50 of 62 nM in BRAF V600E kinase assay and an IC50 of 18 nM in Cell-Based Phosho-ERK Assay.

<p>PLX7904 (PB04), a selective RAF inhibitor, blocks ERK1/2 in mutant BRAF melanoma without activating it in RAS mutants.</p>

<p>B-Raf IN 13 is a potent B-Raf inhibitor with anticancer activity.B-Raf IN 13 has an IC50 of 3.55 nM in the BRAF V600E enzyme assay.</p>

<p>GDC-0879 (AR-00341677) is a novel, potent and selective B-Raf inhibitor with IC50 of 0.13 nM with activity against c-Raf as well.</p>

<p>MCP110 is an inhibitor of the interaction of Ras with Raf-1 and can be used in studies about the treatment of human tumors.</p>

<p>BRAF inhibitor is an inhibitor of B-Raf.</p>

<p>SOS1-IN-15 is an orally active and potent SOS1 inhibitor with potential antitumor activity.SOS1-IN-15 is used in the study of colon cancer.</p>

<p>GSK2008607 is a potent B-RafV600E inhibitor with anticancer activity and can be used to study breast, colorectal, melanoma, thyroid, and ovarian cancers.</p>

<p>Raf inhibitor 3 (Example 30), a potent inhibitor of both B-Raf and C-Raf, exhibits IC50 values below 15 nM. It is applicable in cancer research studies [1].</p>

<p>Uplarafenib (B-Raf IN 10), a potent BRAF inhibitor (IC50: 50-100 nM), exhibits antitumor effects on solid cancers.</p>

<p>Lifirafenib (Beigene-283) is a potent inhibitor of RAF family kinases and EGFR in biochemical assays with IC50 of 23, 29 and 495 nM for the recombinant</p>

<p>B-Raf IN 15 is a BRAF inhibitor that inhibits BRAFWT and BRAFV600E and can be used to study melanoma and cancer.</p>

<p>B-Raf IN 16, a BRAF inhibitor, belongs to cyclic iminopyrimidine derivatives and can be used for cancer or tumour research.</p>

<p>Exarafenib (RAF/KIN_2787) is an oral pan-RAF inhibitor with antitumor properties, targeting MAPK signaling in cancer research.</p>

<p>HG6-64-1 (HMSL 10017-101-1, compound 9 (XI-1)) is a potent and selective B-Raf inhibitor with an IC50 = 0.09 μM in B-raf V600E-transformed Ba/F3 cells.</p>

<p>Pan-Raf/RTK inhibitor 1 (compound I-16) is a potent pan-Raf inhibitor with IC50 values of 3.49 nM (BRafV600E), 8.86 nM (ARaf), 5.78 nM (BRafWT), and 1.65 nM (CRaf). It exhibits antiproliferative activity against various cancer cell lines and can be utilized in cancer research.</p>

<p>Brimarafenib is a selective RAF dimerization inhibitor, which can inhibit BRAF and CRAF, and exhibits inhibitory effects on a variety of RAF mutations.</p>

<p>Rineterkib (ERK-IN-1) is an inhibitor of RAF and ERK1/2 activating mutations in the MAPK pathway.</p>

<p>SKLB646 is an orally active multitarget kinase inhibitor that exhibits potent suppression of several kinases. It demonstrates significant inhibitory effects on SRC and VEGFR2, with IC50 values of 0.002 μmol/L and 0.012 μmol/L, respectively. Additionally, SKLB646 shows notable inhibition of B-Raf and C-Raf, with IC50 values of 0.022 μmol/L and 0.019 μmol/L, respectively. The compound inhibits the activation of the SRC signaling pathway and blocks the MAPK signaling pathway by inhibiting Raf kinases. Furthermore, SKLB646 inhibits the proliferation, migration, and invasion of human umbilical vein endothelial cells (HUVEC), thereby suppressing tumor-induced angiogenesis. SKLB646 also displays significant anti-proliferative and anti-survival effects on triple-negative breast cancer (TNBC) cell lines.</p>

<p>IHMT-RAF-128 is a potent pan-RAF inhibitor that demonstrates robust antitumor activity in xenograft mouse tumor models without causing significant toxicity.</p>