Raf

LY3009120 is a pan RAF inhibitor which inhibits BRAFV600E, BRAFWT and CRAFWT with IC50s of 5.8, 9.1 and 15 nM, respectively.

PLX8394 is a next-generation, orally available, small-molecule BRAF inhibitor with IC50 values of 3.8 nM, 14 nM and 23 nM for BRAF(V600E), WT BRAF and CRAF respectively. It has potential antineoplastic activity.

LXH254 is a type II ATP-competitive inhibitor that inhibits both B- and CRAF kinase activities at picomolar concentrations with a high degree of selectivity against a panel of 456 human kinases and in cell-based assays.

RAF709 is a potent inhibitor of B/C RAF kinase with almost equivalent IC50 values of 0.4 nM for B-RAF and C-RAF, showing a high level of selectivity, demonstrating greater than 99% on-target binding to BRAF, BRAFV600E, and CRAF at 1 μM and very few off-targets with DDR1 (>99%), DDR2 (86%), FRK (92%), and PDGFRb (96%), the only kinases with binding >80% at 1 μM.

Lifirafenib (BGB-283), also known as Beigene-283, potently inhibits RAF family kinases and EGFR activities in biochemical assays with IC50 values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant.

B-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-RafWT, B-RafV600E, and C-Raf, respectively.

MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 blocks the interaction of Ras with Raf. MCP110 disrupts this interaction might can be used for the research of human tumors.

CCT196969 is a pan-Raf inhibitor, which inhibits B-Raf, BRafV600E and CRAF with IC50s of 0.1, 0.04, and 0.01 μM, respectively.

Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively.

B-Raf IN 1 is a potent and selective B-Raf kinase inhibitor with an IC50 of 24 nM.

Sorafenib D3 (Bay 43-9006 D3) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.

Sorafenib D4 (Bay 43-9006 D4) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.

BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase.

RAF mutant-IN-1 is a RAF kinase inhibitor, extracted from patent WO2019107987A1, with IC50 values of 21 nM, 30 nM and 392 nM for C-RAF340D/Y341D, B-RAFV600E and B-RAFWT, respectively.

Rineterkib (ERK-IN-1) (compound B) is a RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway.

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

LUT014 is a B-Raf inhibitor with an IC50 of 11.7 nM, and developed to reduce dose-limiting acneiform lesions associated EGFR Inhibitors treatment. Extracted from patent WO 2019026065A2 .

CEP-32496 hydrochloride is a highly potent inhibitor of wild-type BRAF, V600E mutant BRAF and c-Raf with Kd values of 14 nM, 36 nM and 39 nM, respectively.

Dabrafenib Mesylate is a novel, potent, and selective Raf kinase inhibitor that is capableof inhibiting the kinase activity of wild-type B-Raf, B-RafV600Eand c-Raf with IC50 values of 3.2, 0.8, and 5.0 nM, respectively.

Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.

RRD-251 is a selective inhibitor of the retinoblastoma tumor suppressor protein (Rb)-Raf-1 interaction. This compound exhibits potent anti-proliferative, anti-angiogenic, and anti-tumor activities, making it valuable for research focused on cancer biology and therapeutic strategies targeting cell growth and tumor progression. Its ability to disrupt this critical protein interaction highlights its potential use in studies investigating the molecular mechanisms underlying various cancers.

2,4,3',4',6'-Penta-O-(3-methylbutanoyl)sucrose functions as a selective binder for Fibroblast Growth Factor Receptor 3 (FGFR3) and BRAF, playing a pivotal role in modulating pathways associated with cancer progression. Derived from Atractylodes japonica, this compound exhibits low cytotoxicity towards cancer cell lines, making it a suitable candidate for research applications focused on targeted cancer therapies and signaling pathway studies. Its unique structural characteristics enhance its potential for further exploration in drug development and therapeutic interventions.

CG 858-Neg is a negative control for Thalidomide-derived PROTAC degraders targeting BRAF and BRAFV600E, exhibiting Ki values of 9.5 nM and 14.4 nM, respectively. This compound effectively inhibits downstream phosphorylation of ERK and demonstrates suppression of BRAFV600E-driven tumorigenesis in melanoma (A375 cells, IC50 = 492 nM) and colorectal cancer (HT-29 cells, IC50 = 459 nM) models. CG 858-Neg is suitable for research applications focused on the mechanisms of melanoma and colorectal carcinoma.

Cefotetan is a selective inhibitor of the human Raf1 kinase inhibitor protein (hRKIP). By binding to hRKIP, Cefotetan reduces its interaction with Raf1 kinase, thereby alleviating the inhibition of the Ras/Raf1/MEK/ERK signaling pathway and facilitating enhanced ERK phosphorylation. This mechanism makes Cefotetan valuable for research on diseases linked to dysregulated signaling within this pathway. Additionally, Cefotetan functions as a broad-spectrum antibacterial agent by binding to bacterial penicillin-binding proteins (PBPs) and disrupting cell wall synthesis, making it useful for investigating bacterial infections, particularly in the contexts of bone, skin, urinary tract, and lower respiratory tract infections.

Tinlorafenib is a potent inhibitor of BRAF and CRAF kinases, exhibiting IC50 values of 5.8 nM and 4.1 nM, respectively. It specifically targets V600E and V600K mutations in BRAF with IC50s of 4.25 nM and 2.7 nM, making it valuable for studying BRAF-driven tumors. Notably, Tinlorafenib demonstrates effective penetration of the blood-brain barrier, facilitating research into both central nervous system tumors and extracranial malignancies associated with BRAF mutations.

ML786 is a potent Raf inhibitor with oral bioavailability, demonstrating IC50 values of 2.1 nM for V600EΔB-Raf, 4.2 nM for wild-type B-Raf, and 2.5 nM for C-Raf. Additionally, ML786 exhibits inhibitory effects on Abl-1, DDR2, EPHA2, KDR, and RET, with IC50 values under 0.5 nM, 7.0 nM, 11 nM, 6.2 nM, and 0.8 nM, respectively. This compound is suitable for research applications focused on cancer biology, helping to advance understanding of therapeutic targets within malignancies.

KG5 is an orally active dual inhibitor targeting PDGFRβ and B-Raf through allosteric mechanisms. It also exhibits inhibitory effects on Flt3, KIT, and c-Raf. KG5 demonstrates significant anticancer and antiangiogenic activities, making it a valuable reagent for research in cancer therapy and angiogenesis studies.

INU-152 is a potent and selective inhibitor of B-Raf, a key kinase in the MAPK signaling pathway. This compound effectively reduces tumor cell proliferation, enhances autophagy, and induces apoptosis through the inhibition of B-Raf activity. INU-152 demonstrates significant cytotoxicity against cancer cells transformed with v-Ha-ras (Ras-NIH 3T3), making it a valuable tool for cancer research applications.

B-Raf IN 9 is a potent B-Raf inhibitor with an IC50 of 24.79 nM, targeting the B-Raf signaling pathway. This compound induces apoptosis and causes cell cycle arrest at the G2/M phase. B-Raf IN 9 demonstrates significant antitumor activity against the human prostate cancer PC-3 cell line, with an IC50 of 7.83 µM, making it a valuable tool for cancer research and therapeutic investigations.

EGFR/BRAFV600E-IN-1 is a potent dual inhibitor targeting EGFR and the BRAFV600E mutation, with IC50 values of 0.08 µM and 0.15 µM, respectively. This compound effectively induces apoptosis and induces cell cycle arrest in the pre-G1 and G2/M phases. Additionally, it demonstrates significant antiproliferative activity against A-549, MCF-7, Panc-1, and HT-29 cell lines, with IC50 values of 1.2 µM, 0.79 µM, 1.3 µM, and 1.23 µM, respectively, making it valuable for cancer research focused on these targets.

SJ-C1044 is a pan-RAF inhibitor that demonstrates both immunomodulatory and anti-tumor properties. This compound effectively targets wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values of 331, 257, and 187 nM, respectively, leading to inhibition of Kras activation and MEK-ERK phosphorylation, which reduces tumor cell proliferation. Additionally, SJ-C1044 exhibits inhibitory effects on VEGFR2, TIE2, and CSF1R, with IC50 values of 100, 23, and 235 nM, respectively, contributing to the improvement of the tumor immune microenvironment via the inhibition of angiogenesis and modulation of macrophage function. SJ-C1044 is suitable for research applications in colorectal cancer studies.

Takeda-6D is a potent and orally active inhibitor targeting BRAF and VEGFR2, displaying IC50 values of 7.0 nM and 2.2 nM, respectively. This compound effectively suppresses angiogenesis by inhibiting the VEGFR2 signaling pathway in 293/KDR and VEGF-stimulated HUVEC cells. Additionally, Takeda-6D demonstrates significant inhibition of ERK1/2 phosphorylation, indicating its potential for antitumor activity in various cancer research applications.

SKLB646 is a multi-target kinase inhibitor with a focus on SRC, Raf, and VEGFR2. It exhibits potent inhibitory activity against SRC and VEGFR2, with IC50 values of 0.002 μmol/L and 0.012 μmol/L, respectively, as well as significant effects on B-Raf and C-Raf. SKLB646 disrupts SRC signaling and inhibits the MAPK pathway by targeting Raf kinases, leading to decreased proliferation, migration, and invasion in human umbilical vein endothelial cells (HUVEC), thereby impeding tumor-induced angiogenesis. It also demonstrates significant anti-proliferative and anti-survival effects on triple-negative breast cancer (TNBC) cell lines, making it a valuable tool for cancer research.

AD57 is an orally active multikinase inhibitor that targets RET, BRAF, S6K, and Src, effectively reducing mTOR activity. This compound demonstrates significant biological activity by interfering with critical signaling pathways involved in cancer proliferation and survival. AD57 is suitable for research applications focused on cancer biology and therapeutic development against malignancies driven by these kinases.

AD57 hydrochloride is a multikinase inhibitor that targets RET, BRAF, S6K, and Src pathways. This orally active compound demonstrates significant biological activity in modulating aberrant signaling pathways associated with various cancers. Research applications include studying the effects of combined inhibition on tumor growth and resistance mechanisms in cancer cell lines and animal models.