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

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).

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.

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.

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).

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.

B-Raf IN 17 (Compound 8e) is an effective, orally active type II multi-kinase inhibitor. It shows potent cellular inhibition against BRAFWT, VEGFR-2, and FGFR-1 in the A375 cell line, with IC50 values of 0.02, 0.18, and 1.65 μM, respectively. B-Raf IN 17 is applicable for cancer research.

RAF-IN-2 is a RAF inhibitor. This compound can be utilized in research related to proliferative diseases such as leukemia, psoriasis, and fibrosis.

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.

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.

Phosphatidylserine is a phospholipid naturally present in mammals, exhibiting anti-inflammatory and anti-atherosclerotic effects. It activates PKC, neutral sphingolipidase, C-raf-1 protein kinase, and other cofactors involved in multiple signaling pathway activations.

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.

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.

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].