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Raf inhibitor
Sorafenib Tosylate (Nexavar) is a novel, small molecular inhibitor of several tyrosine protein kinases (VEGFR and PDGFR) and RAF/MEK/ERK cascade inhibitor with an IC50 of 6, 22, 38 nM for Raf-1, wt BRAF and V599E mutant BRAF.- Arda Kipcak, .et al. , Mol Biol Rep, 2024, Jul 13;51(1):799 PMID: 39001931
- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Paula Sagmeister, .et al. , J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. , J Transl Sci, 2020, 7: 1-10
- Mariko Fujisawa, .et al. , Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298 PMID: 32593665
- Fangyuan Lai, .et al. , Stem Cell Res Ther, 2018, 9: 107 PMID: 29661222
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
- Arum Park, .et al. , J Cancer, 2017, 8(12): 2303-2311 PMID: 28819434
- Cong Li, .et al. , Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Zhihong Li, .et al. , J Med Chem, 2014, Apr 24;57(8):3430-49 PMID: 24641103
- Hideki Yamaguchi, .et al. , Cancer Sci, 2014, 105(5): 528-536 PMID: 24612061
- Yaping Zhang, .et al. , J Pharmacokinet Pharmacodyn., 2014, 41(6): 675-691 PMID: 25326874
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Raf inhibitor
PLX-4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf.- Jiang Zhou, .et al. , Neoplasia, 2025, Oct:68:101223 PMID: 40850308
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VEGFR inhibitor
Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature.- Lila Louadj, .et al. , Sci Rep, 2026, Apr 4;16(1):16233 PMID: 41935207
- Uzma Hasan, .et al. , Drug Deliv Transl Res, 2024, Feb;14(2):342-359 PMID: 37587289
- Hasan U, .et al. , Research Square, 2023, 13 Apr
- Paula Sagmeister, .et al. , J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. , J Transl Sci, 2020, 7: 1-10
- Makoto Koyama, .et al. , Int J Oncol, 2020, Sep 2 PMID: 32901840
- Mariko Fujisawa, .et al. , Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298 PMID: 32593665
- Sunil Kumar Yadava, .et al. , Colloids Surf B Biointerfaces, 2020, Mar 2;190:110927 PMID: 32169777
- Takeshi Uenaka, .et al. , Hum Mol Genet, 2018, Nov 15; 27(22): 3974-3985 PMID: 30137437
- Yi Xu, .et al. , Free Radic Biol Med, 2016, Jul; 96: 67-77 PMID: 27101738
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B-Raf inhibitor
GDC-0879 is a specific inhibitor of B-Raf kinase enzyme,targeting B-Raf (V600E) (IC50: 0.13 nM).- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
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EphB4 inhibitor
NVP-BHG712 is a selective inhibitor of EphB4 kinase that exhibits selectivity for EphB4 over more than 40 other kinases in vitro, including FGFR3.- Ryuzaburo Yuki, .et al. , Eur J Pharmacol, 2024, Jan 15:963:176229 PMID: 38072041
- Y Kaibori, .et al. , the FASEB Journal, 2019, Jan 22:fj201801519RR PMID: 30668924
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Selective B-RAF Inhibitor
LGX818 is an orally available Raf kinase inhibitor with potential antineoplastic activity.- Seidel D, .et al. , Biosens Bioelectron, 2019, Jan 1;123:185-194 PMID: 30201332
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Raf inhibitor
Dabrafenib is a potent and selective inhibitor of B-RAF protein kinase carrying V600E mutation, currently in clinical trial.- Shamima Azma Ansari, .et al. , Br J Cancer, 2025, Sep 9 PMID: 40926063
- Rana Can Baygin, .et al. , Sci Rep, 2024, Jan 2;14(1):286 PMID: 38167959
- Ali Talebi, .et al. , J Exp Clin Cancer Res, 2023, Apr 19;42(1):92 PMID: 37072838
- Yuki Shimizu, .et al. , Cancer Lett, 2022, Sep 1;543 PMID: 35724767
- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Chenyang He, .et al. , Clinical and Translational Biophotonics, 2020, TTh3B.2
- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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RKIP/Raf1 inhibitor
Locostatin is a cell permeable, potent inhibitor of Raf kinase inhibitor protein (RKIP)/Raf1 kinase interaction and an inhibitor of cell migration.- Wei Sun, .et al. , J Orthop Translat, 2024, Jan; 44: 114-124 PMID: 38304614
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Raf inhibitor
PLX4032 (Vemurafenib) also known as RG7204, Vemurafenib, R7204; RO5185426. PLX4032 is a B-raf inhibitor with an IC50 of 44 nM.- Yoon Jin Lee, .et al. , Ann Dermatol, 2023, Dec;35(6):439-450 PMID: 38086358
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Lee YJ, .et al. , Research Square, 2022, April 27th
- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Guixin Zhu, .et al. , Nat Cell Biol, 2021, Sep;23(9):978-991 PMID: 34497368
- Makoto Koyama, .et al. , Int J Oncol, 2020, Sep 2 PMID: 32901840
- Kudo K, .et al. , FASEB J, 2018, Dec 3:fj201800664RR PMID: 30508500
- Min Ho Choe, .et al. , Cell Death Dis, 2018, Jun; 9(6): 640 PMID: 29844307
- Jan Dorrie, .et al. , Int J Mol Sci, 2018, Jan; 19(1): 289 PMID: 29346301
- Aishwarya Kundu, .et al. , Mol Carcinog, 2017, Jan; 56(1): 49-61 PMID: 26878440
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Toshinori Sueda, .et al. , Sci Rep, 2016, 6: 18949 PMID: 26750638
- Yanling Li, .et al. , Onco Targets Ther, 2015, 8: 1043-1051 PMID: 25999739
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pan-RAF inhibitor
TAK-632 is a potent pan-RAF inhibitor with favorable in vitro activity (BRAF(V600E) IC50, 2.4 nM; BRAF(wt), 8.3 nM; CRAF, 1.4 nM; pMEK (A375) IC50, 12 nM; pMEK (HMVII), 49 nM; V/B ratio.- Yosi Shamay, .et al. , Nat Mater, 2018, Apr; 17(4): 361-368 PMID: 29403054
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Raf/MEK dual inhibitor
Avutometinib (RO5126766, CH5126766), is a protein kinase inhibitor specific for the Raf and MEK mitogen-activated protein kinases (MAPKs) with potential anti-neoplastic activity.
- Yuki Shimizu, .et al. , Cancer Lett, 2022, Sep 1;543 PMID: 35724767
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RAF/VEGFR Inhibitor
RAF265 (CHIR-265) is an oral, highly selective RAF and VEGFR kinase inhibitor, which is to control or normalize VEGFR-2 along with the inhibition of B-raf and c-Raf mutation to prevent cancers. -
RAF/VEGFR Inhibitor
Raf265 derivative is a derivative of Raf265 that is an oral, highly selective RAF and VEGFR kinase inhibitor with IC50 of of 5 to 10 μM. -
Raf kinase inhibitor
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. -
Raf/EGFR inhibitor
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 kinase inhibitor
B-Raf IN 1 is a potent and selective B-Raf kinase inhibitor with an IC50 of 24 nM. -
Raf/VEGFR3 inhibitor
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. -
Raf/VEGFR3 inhibitor
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. -
raf kinase inhibitor
Raf inhibitor 2 is a potent raf kinase (IC50<1.0 μM) inhibitor, compound 32, extracted from patent EP1003721B1. Raf inhibitor 2 can be used for cancer research. -
Tyrosinase Inhibitor
Norartocarpetin is a potent tyrosinase inhibitor, demonstrating significant inhibition with an IC50 value of 0.47 μM. This compound serves as an effective antibrowning agent for food systems research and exhibits notable anticancer activity against lung carcinoma cells (NCI-H460) with an IC50 of 22 μM. Its antiproliferative effects are mediated through targeting the Ras/Raf/MAPK signaling pathway, inducing mitochondrial-mediated apoptosis, causing S-phase cell cycle arrest, and inhibiting cell migration and invasion in human lung carcinoma cells. -
RAF-1/HIF-1α Inhibitor
MO-2097 is a selective RAF-1 and HIF-1α inhibitor that induces the destabilization of RAF-1, resulting in decreased levels of epithelial-mesenchymal transition (EMT) transcription factors and mesenchymal markers. Additionally, MO-2097 effectively inhibits HIF-1α protein expression mediated by hnRNPA2B1 in hypoxic conditions. This compound promotes the generation of mitochondrial reactive oxygen species (ROS), contributing to apoptosis in malignant cells. MO-2097 demonstrates significant potential in suppressing colorectal cancer metastasis by targeting the RAF/MEK/ERK signaling pathway and has shown efficacy in reducing tumor growth in HCT116 cell xenograft mouse models, thus serving as a valuable tool for colorectal cancer research. -
PI3K/Akt/Ras/Raf/MAPK Inhibitor
Erufosine is a potent inhibitor of the PI3K/Akt and Ras/Raf/MAPK signaling pathways. It demonstrates significant cytotoxic activity against breast cancer cell lines, specifically MCF-7 and MDA-MB-231, with IC50 values of 40.95 μM and 40.8 μM, respectively. By reducing the phosphorylation levels of PI3K (p85), Akt (PKB), and cRaf, Erufosine serves as a valuable tool in the research of breast cancer and myeloid leukemia. -
RAF/DDR Inhibitor
PHI-501 is a dual inhibitor targeting RAF and DDR pathways. It demonstrates potent anti-proliferative effects in melanoma cell lines, effectively inhibiting colony formation in drug-resistant cells. PHI-501 disrupts ERK and AKT phosphorylation and downregulates key gene sets associated with TNFA-NFKB, IL6-JAK-STAT3, and KRAS signaling pathways, as well as pathways involved in epithelial-mesenchymal transition. In vivo studies show significant anti-tumor efficacy in the SK-MEL3DR xenograft model, making PHI-501 valuable for research on drug resistance in melanoma. -
Raf/EGFR Inhibitor
Lifirafenib maleate is a potent inhibitor of Raf kinase and EGFR, exhibiting IC50 values of 23 nM and 29 nM for recombinant BRafV600E and EGFR, respectively. This compound effectively disrupts critical signaling pathways involved in cancer cell proliferation and survival. Lifirafenib maleate is relevant for research applications in cancer biology, particularly in studies focusing on targeted therapies for tumors with BRAF mutations or EGFR dysregulation. -
EGFR/BRAF Inhibitor
EGFR/BRAF-IN-1 is a selective inhibitor targeting both EGFR and BRAFV600E with an IC50 of 45 nM. This compound, a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, effectively inhibits cancer cell proliferation with a GI50 of 35 nM. Additionally, EGFR/BRAF-IN-1 exhibits notable antioxidant properties, making it a valuable reagent for research in cancer biology and therapeutic development. -
RAF inhibitor
PF-04880594 is an inhibitor of RAF with IC50 values of 0.19 nM/0.13 nM and 0.39 nM for BRAF/BRAFV599E and c-RAF, respectively. -
RAS/RAF/MAPK inhibitor
Diazepinomicin, also known as TLN-4601, is a small-molecule inhibitor of the RAS/RAF/MAPK signaling pathway with potential antineoplastic activity. -
Ras/Raf/MEK inhibitor
Balamapimod, also known as MKI-822, is a Ras/Raf/MEK inhibitor. -
pan RAF inhibitor
Belvarafenib (HM95573) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively. -
B-Raf inhibitor
B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor with cell IC50s of 0.31 uM and 2 nM for A375 proliferation and A375 p-ERK respectively -
dual BRAF inhibitor
AZ304 is a potent dual BRAF inhibitor targeting the kinase domains of wild type BRAF, V600E mutant BRAF. AZ304 exerted potent inhibitory effects on both wild type and V600E mutant forms of the serine/threonine-protein kinase BRAF, with IC50 values of 79?nM and 38?nM, respectively. -
Raf nhibitor
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. -
RAF/ERK1/2 inhibitor
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.
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Raf Inhibitor
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. -
Raf inhibitor
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. -
Tyrosine kinase inhibitor
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. -
Raf inhibitor
ML 786 dihydrochloride is a potent Raf kinase inhibitor (IC50 values are 2.1, 2.5 and 4.2 nM for B-RafV600E, C-Raf and wild-type B-Raf respectively). -
pan-Raf inhibitor
MLN 2480 is an oral, selective pan-Raf kinase inhibitor in chinical trials.

