raf inhibitor 2

Raf inhibitor 2 (CID 25014542) is novel inhibitor of Raf kinases.

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 VEGFR3, PDGFR-β, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.

Regorafenib Hydrochloride (BAY73-4506 hydrochloride) is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity

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

LXH254 is a B C RAF inhibitor with IC50 values of 0.2 nM and 0.07 nM for inhibiting BRAF and CRAF.

TAK-632, a potent pan-Raf inhibitor (GenScript, 2020), is characterized by its molecular weight [M] for [C 22 H 19 FN 2 O 2] of 362.4 by LC-MS, with a purity of 99% (HPLC). The compound exhibits white to off-white solid form and has a melting point [M] ranging from 178°C to 182°C (GenScript, 2020). Its solubility profile includes DMSO, in which it is soluble to 100mM (GenScript, 2020).

OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel growth (angiogenesis) in tumors.

GW 5074 (Raf1 Kinase Inhibitor I)(IC50=9 nM) is an effective and specific c-Raf inhibitor. It has no effect on the activities of JNK1 2 3, MEK1, MKK6 7, CDK1 2, c-Src, p38 MAP, VEGFR2 or c-Fms.

Takeda-6d, a novel, potent DFG-out RAF vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor, inhibits B-RAF and VEGFR2 with IC50 of 7.0nM and 2.2nM.

Regorafénib N-oxyde M2 is an active metabolite of Regorafenib, a multi-target inhibitor for VEGFR1 2 3, PDGFRβ, RET, Kit, and Raf-1 (IC50s: 13 4.2 46, 1.5, 22, 7, and 2.5 nM).

5Z-7-Oxozeaenol (FR148083) is a potent, irreversible and selective inhibitor of transforming growth factor (TGF)-β-activated kinase 1 with IC50 of 8.1 nM for TAK1 and low activity against MEK1 with IC50 of 411 nM, it is also an inhibitor of VEGF-R2 with IC50 of 52 nM.

MEK RAF-IN-1 (Compound 16b) serves as an inhibitor targeting both MEK and RAF, demonstrating potent efficacy with IC 50 values reported at 28 nM for MEK1, and 3 nM for both BRAF and BRAFV600E. This compound exhibits significant antitumor capabilities, effectively curbing cell proliferation in vitro in MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Furthermore, MEK RAF-IN-1 significantly restricts tumor growth in xenograft mouse models employed in the study of colorectal cancer.

Phosphatidylserine is a naturally occurring phospholipid that comprises 2-10% of total phospholipids in mammals and is enriched in the central nervous system, particularly the retina. It is anionic and found mainly on the inner leaflet of the cell membrane. It is biosynthesized from phosphatidylcholine or phosphatidylethanolamine by phosphatidyl synthase 1 (PSS1) or PSS2, respectively, in the endoplasmic reticulum and can be reversibly converted back by the same enzymes. It can also be irreversibly converted to phosphatidylethanolamine by phosphatidylserine decarboxylase in the mitochondria. Phosphatidylserine binds to T cell immunoglobulin mucin type 1 (TIM-1) and TIM-4 receptors as well as brain-specific angiogenesis inhibitor 1 (BAI1), leading to anti-inflammatory and anti-atherosclerotic effects. It is also a cofactor involved in the activation of various signaling pathways through activation of protein kinase C, neutral sphingomyelinase, and c-Raf-1 protein kinase among others. Phosphatidylserine is externalized during apoptosis by scramblases in the plasma membrane as a signal for phagocytes to engulf the cell. Phosphatidylserines (bovine) is a mixture of bovine phosphatidylserines containing fatty acids with variable chain lengths at the sn-1 and sn-2 positions.

Rineterkib hydrochloride (compound B) is an orally active RAF and ERK1 2 inhibitor used in treating proliferative diseases characterized by activating mutations in the MAPK pathway, particularly KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC), and KRAS-mutant ovarian cancer[1].

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

B-Raf IN 8 (compound 7g) is a potent inhibitor of B-Raf (IC50 = 70.65 nM) with antitumor activity, demonstrating IC50 values of 9.78, 13.78, 18.52, and 29.85 μM against hepatocellular carcinoma (HEPG-2), colon carcinoma (HCT-116), mammary gland (MCF-7), and human prostate cancer (PC-3) cells [1].

B-Raf IN 7 (compound 6a) is a potent B-Raf inhibitor with an IC50 of 110.23 nM. It exhibits antitumor activity against colon carcinoma cells (HCT-116), mammary gland cells (MCF-7), hepatocellular carcinoma cells (HEPG-2), human cervical carcinoma cells (Hela), and human prostate cancer cells (PC-3), with IC50 values of 7.50, 9.87, 10.57, 11.63, and 12.83 μM, respectively [1].

RAF265 (CHIR-265) (CHIR-265) is a potent selective inhibitor of C-Raf B-Raf B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM. Phase 2.

Regorafenib (BAY 73-4506) mesylate is an orally active multi-target receptor tyrosine kinase inhibitor, inhibiting VEGFR1 2 3 (IC50=13 4.2 46 nM), PDGFRβ (IC50: 22 nM), Kit (IC50: 7 nM), RET (IC50: 1.5 nM), and Raf-1 (IC50: 2.5 nM), with potent anti-tumor and anti-angiogenic effects.

PLX7904 (PB04), also known as PB04, is a potent and selective paradox-breaker RAF inhibitor. It is able to efficiently inhibit activation of ERK1 2 in mutant BRAF melanoma cells but does not hyperactivate ERK1 2 in mutant RAS-expressing cells.

Pimasertib HCl is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1 2) with potential antineoplastic activity. Pimasertib selectively binds to and inhibits the activity of MEK1 2, preventing the activation of MEK1 2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK1 2 (MAP2K1 K2) are dual-specificity threonine tyrosine kinases that play key roles in the activation of the RAS RAF MEK ERK pathway and are often upregulated in a variety of tumor cell types.

MAPK-IN-2 (compound 3h) is an efficacious MAPK inhibitor with antineoplastic properties that significantly hinders proliferation across various cancer cell lines. It demonstrates robust suppression of the MAPK pathway (EGFR WT IC50 = 281 nM, c-MET IC50 = 205 nM, B-RAF WT IC50 = 112 nM, CDK4 6 IC50 = 95 and 184 nM, respectively) and exhibits pronounced activity against mutated forms of EGFR and B-RAF (EGFR T790M IC50 = 69 nM and B-RAF V600E IC50 = 83 nM) [1].

Protein kinase D (PKD), a serine threonine protein kinase activated by diacylglycerol downstream of PKC signaling, has three human isoforms that modulate cell proliferation, survival, invasion, and protein transport. CRT0066101 acts as an inhibitor of these three PKD isoforms, with IC50 values of 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively. It demonstrates selectivity for PKD over a range of more than 90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src, and c-Abl. This specificity allows CRT0066101 to inhibit cell proliferation, induce apoptosis, and notably reduce the viability of pancreatic cancer cells both in vitro and in vivo.

GNE-9815 (3-(2-cyanopropan-2-yl)-N-[2-fluoro-4-methyl-5-(7-methyl-8-oxo-7,8-dihydropyrido[2,3-d]pyridazin-3-yl)phenyl]benzamide) is a high kinase-selective inhibitor of RAF and targets KRAS-mutant cancers through combination therapy.