Raf

<p>MRTX0902 is an effective and high selective inhibitor of SOS1 with an IC50 of 46 nM and a Ki of 2 nM.</p>

<p>Sorafenib (Bay 43-9006) is a multikinase inhibitor that inhibits Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57</p>

<p>XL-281: potent oral RAF kinase inhibitor, effective on wild-type and mutants, reduces tumor growth and cell proliferation, increases apoptosis.</p>

<p>Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).</p>

<p>LXH254 is a B/C RAF inhibitor with IC50 values of 0.2 nM and 0.07 nM for inhibiting BRAF and CRAF.Cost-effective and quality-assured.</p>

<p>Regorafénib N-oxyde M2 is an active metabolite of Regorafenib.</p>

<p>LUT014 is a B-Raf inhibitor (IC50: 11.7 nM) and developed to decrease dose-limiting acneiform lesions associated with EGFR Inhibitors treatment.</p>

<p>B-Raf IN 2, compound Ia, is a highly effective and specific inhibitor of BRAF. It exhibits significant potential for cancer research.</p>

<p>14.3.3 protein antagonist, blocks binding to Raf-1/Bad/ASK1/exoenzyme S, competitive, no phosphorylation needed, KD ~80 nM.</p>

<p>SOS1-IN-17 (Compound 8d) is an orally active inhibitor targeting the SOS1-KRASG12C interaction, with an IC50 of 5.1 nM. It suppresses ERK phosphorylation in DLD-1 cells with an IC50 of 18 nM and demonstrates antiproliferative activity in KRASG12C-mutant Mia-Paca-2 cells, with an IC50 of 0.11 μM. In mouse models, SOS1-IN-17 shows antitumor efficacy against pancreatic cancer.</p>

<p>Cyclorasin 9A5 is a cell-permeable, 11-residue cyclic peptide that orthosterically disrupts the Ras-Raf protein interaction, demonstrating an inhibition</p>

<p>Cyclorasin 9A5 TFA is a cell-penetrating cyclic peptide consisting of 11 residues that inhibits the interaction between Ras and Raf proteins, with an IC50 of 120 nM.</p>

<p>Vem-L-Cy5 (compound 3), a Vemurafenib-based BRAF inhibitor conjugated with the near-infrared (NIR) fluorophore cyanine-5 (Cy5), selectively targets the BRAF</p>

<p>KG5 inhibits PDGFRβ, B-Raf, FLT3, KIT, c-Raf; has anticancer and antiangiogenic effects; Kd: 520 nM (PDGFRβ), 300 nM (PDGFRα).</p>

<p>PROTAC B-Raf degrader 1 is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf,PROTAC B-Raf degrader 1 With anti-cancer activity.</p>

<p>SOS1-IN-11 is an effective inhibitor of SOS1 (IC50 = 30 nM).</p>

<p>A unique collection of 365 compounds targeting MAPK signaling for drug discovery in MAPK related diseases;</p>

<p>Anti-Phospho-RAF1 (Ser259) Antibody (5X237) is an antibody targeting Phospho-RAF1 (Ser259). Anti-Phospho-RAF1 (Ser259) Antibody (5X237) can be used in ELISA, WB, IHC, IF.</p>

<p>Anti-Phospho-RAF1 (Ser621) Antibody (2K681) is an antibody targeting Phospho-RAF1 (Ser621). Anti-Phospho-RAF1 (Ser621) Antibody (2K681) can be used in ELISA, WB, IF.</p>

<p>RAS GTPase inhibitor 1 is a RAS GTPase inhibitor with potential antitumor activity.</p>

<p>Anti-Phospho-RAF1 (Ser43) Antibody (8R108) is an antibody targeting Phospho-RAF1 (Ser43). Anti-Phospho-RAF1 (Ser43) Antibody (8R108) can be used in ELISA, IF.</p>

<p>Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine</p>

<p>ZM 336372 is a potent and selective c-Raf inhibitor.</p>

<p>GW 5074 (Raf1 Kinase Inhibitor I)(IC50=9 nM) is an effective and specific c-Raf inhibitor.</p>

<p>Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ and is orally</p>

<p>Plixorafenib (PLX8394) is an orally active inhibitor of the serine/threonine protein kinase B-Raf (BRAF) protein.Cost-effective and quality-assured.</p>

<p>RO5126766 (CH5126766) is a dual RAF/MEK inhibitor with IC50 of 8.2 nM, 19 nM, 56 nM, and 160 nM for BRAF V600E, BRAF, CRAF, and MEK1, respectively. Phase 1.</p>

<p>Kobe 2602 is an inhibitor of Ras that exhibits anticancer chemotherapeutic activities.</p>

<p>Agerafenib (CEP32496) is a highly potent inhibitor of BRAF.</p>

<p>Takeda-6d is a novel, potent DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with IC50 of 7.0 nM and 2.2 nM, respectively.</p>

<p>AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits BRAF (WT), BRAF (V600E), and wild type CRAF (IC50s: 79/38/68 nM).</p>

<p>TAK-632 is a potent pan-Raf inhibitor.</p>

<p>RAF265 (CHIR-265) inhibits C-Raf/B-Raf/V600E (IC50: 3-60 nM), blocks VEGFR2 (EC50: 30 nM), in Phase 2 trials.</p>

<p>AD80, a multikinase inhibitor, inhibits RET, RAF, SRCand S6K, with greatly reduced mTOR activity.</p>

<p>Raf inhibitor 2 (CID 25014542) is novel inhibitor of Raf kinases.</p>

<p>Encorafenib (LGX818) is an orally available mutated BRaf V600E inhibitor(IC50=0.3 nM) with potential antineoplastic activity.</p>

<p>B-Raf IN 11 is a novel selective inhibitor.</p>

<p>BAY-293 is a potent, cell-active SOS1 inhibitor that disrupts the KRAS-SOS1 interaction (IC50: 21 nM).</p>

<p>NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and</p>

<p>RAF709 is a novel Raf kinase inhibitor with IC50s of 0.5 and 1.8 nM for c-Raf and b-Raf, respectively.</p>

<p>BI-882370 is a specific RAF kinase inhibitor.</p>

<p>K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).</p>

<p>SB590885 is an effective B-Raf inhibitor (Ki: 0.16 nM, in a cell-free assay).</p>

<p>Plx-4032 (Vemurafenib) is a small-molecule B-Raf inhibitor for the potential treatment of malignant melanoma.</p>

<p>Irreversible K-Ras(G12C) inhibitor 6 fully modifies the protein at 10 μM after 24h in vitro.</p>

<p>L-779450, an effective, ATP-competitive Raf kinase inhibitor (IC50: 10 nM) , displays &gt;7, &gt;30 and &gt;70-fold selectivity over p38α, GSK3β and Lck respectively.</p>

<p>PLX-4720 is a potent and selective B-Raf (V600E) inhibitor designed to block the ATP-binding site of oncogenic B-Raf.Cost-effective and quality-assured.</p>

<p>CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.</p>

<p>Belvarafenib (HM95573) is a potent pan-RAF inhibitor with antitumor activity and inhibits B-RAF, B-RAFv600E, and C-RAF.Cost-effective and quality-assured.</p>

<p>I-49 free base (Pyrido[4,3-d]pyrimidin-7(6H)-one, 2-methyl-4-[[(1R)-1-[2-methyl-3-(trifluoromethyl)phenyl]ethyl]amino]-6-(tetrahydro-2H-pyran-4-yl)-) is a novel</p>

<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>