Raf Inhibitor

B-Raf IN 17 (Compound 8e) is a potent and orally active type II multi-kinase inhibitor. B-Raf IN 17 exhibits potent cellular-level suppression of BRAF_WT, VEGFR-2, and FGFR-1 in A375 cell line, with IC₅₀ values of 0.02, 0.18 and 1.65 μM, respectively. B-Raf IN 17 can be used for the research of cancer.

Raf1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Raf1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

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

PHI-501 is a dual inhibitor targeting RAF/DDR. PHI-501 exhibits significant anti-proliferative effects in melanoma cell lines and significantly inhibits the colony formation of drug-resistant cells. PHI-501 strongly inhibits ERK and AKT phosphorylation. PHI-501 downregulates the gene sets in drug-resistant cells of TNFA-NFKB, IL6-JAK-STAT3, and KRAS signaling pathways as well as the epithelial-mesenchymal transition (EMT) signaling pathways. PHI-501 demonstrates significant anti-tumor effects in the SK-MEL3DR xenograft model. PHI-501 can be used for research on the problem of drug resistance in melanoma.

EGFR/BRAFV600E-IN-5 (Compound 7I) is a dual BRAFV600E/EGFR inhibitor with IC₅₀ of 0.048 μM and 0.037 μM, respectively. EGFR/BRAFV600E-IN-5 has significant anti-melanoma activity with IC₅₀ of 3.16 μM and 2.50 μM against MALME-3M and LOX-IMVI cell lines, respectively. EGFR/BRAFV600E-IN-5 exerts anti-tumor effects by inducing G1 arrest, inhibiting DNA synthesis, and activating the mitochondrial apoptosis pathway. EGFR/BRAFV600E-IN-5 can be used for melanoma research, especially for combined inhibition of BRAFV600E mutation and EGFR signaling pathway.

Pan-Raf/RTK inhibitor 1 (compound I-16) is a potent pan-Raf inhibitor with IC₅₀ values of 3.49 nM (BRaf^V600E), 8.86 nM (ARaf), 5.78 nM (BRaf^WT), and 1.65 nM (CRaf). Pan-Raf/RTK inhibitor 1 exhibits antiproliferative activities against various cancer cell lines and can be utilized in cancer research.

Ferroptosis inducer-3 (compound JB3) is an oral bioactive inhibitor of RAF1, with the IC₅₀ of 226.9 nM. Ferroptosis inducer-3 can induce ferroptosis and plays an important role in cancer research.

BRAFV600E-IN-1 (compound 9S) is a BRAF inhibitor. BRAFV600E-IN-1 has a significant apoptosis-inducing effect in cell lines expressing mutant KRAS and cancer cells expressing BRAFV600E.

MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both MEK and RAF. It shows potent inhibition with IC₅₀ values of 28 nM for MEK1, and 3 nM each for BRAF and BRAFV600E. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer.

ISIS 5132 is a 20-base phosphorothioate oligonucleotide that specifically down-regulates c-raf expression.

Vemurafenib-d₅ is the deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC₅₀s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively. Vemurafenib induces cell autophagy.

Regorafenib (monohydrate) (Standard) is the analytical standard of Regorafenib (monohydrate). This product is intended for research and analytical applications. Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC₅₀ values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity.

(Rac)-Zearalanone-d₆ is the d₆-labeled (Rac)-Zearalanone (HY-N6678A). (Rac)-Zearalanone is an ATP-competitive HSP90 inhibitor with an EC₅₀ of 2.3 μM. (Rac)-Zearalanone interferes with the binding of ATP to HSP90, impairs the chaperone function of HSP90, and promotes the degradation of client proteins. (Rac)-Zearalanone reduces intracellular accumulation of Raf-1, induces cleavage of caspase-3, and promotes Her2 degradation in a dose-dependent manner by disrupting the Her2-HSP90 interaction. (Rac)-Zearalanone can be used in the research of small cell lung cancer and breast cancer.

ML786 dihydrochloride is a potent and orally bioavailable Raf inhibitor, with IC₅₀s of 2.1, 4.2, and 2.5 nM for ^V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 dihydrochloride also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC₅₀=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 dihydrochloride can be used for the research of cancers.

ARQ-736 is a potent and selective B-RAF inhibitor that plays an important role in cancer study.

MEK1/C-Raf-IN-1 (Compound 14d) is a MEK1/C-Raf inhibitor with IC₅₀ values of 97 and 23 nM, respectively. MEK1/C-Raf-IN-1 has antitumor activity.

RAF-IN-2 is a RAF inhibitor. RAF-IN-2 can be used for proliferative diseases such as leukemia, psoriasis and fibrosis research.

Takeda-6D (compound 6d) is an orally active and potent BRAF/VEGFR2 inhibitor, with IC₅₀ values of 7.0 and 2.2 nM, respectively. Takeda-6D shows antiangiogenesis by suppressing the VEGFR2 pathway in 293/KDR and VEGF-stimulated HUVEC cells.Takeda-6D shows significant suppression of ERK1/2 phosphorylation. Takeda-6D shows antitumor activity.

EBI-907 is an orally active and highly potent B-Raf^V600E inhibitor. EBI-907 demonstrates excellent A375 and Colo-205 cellular antiproliferative activity with IC₅₀ values of 13 nM and 14 nM, respectively. EBI-907 can also cause tumor regression in a B-Raf^V600E-dependent Colo-205 tumor xenograft model of mice. EBI-907 is promising for research of melanoma and B-Raf^V600E associated cancers.

BRAF V600E/CRAF-IN-2 (Compound 9c) is a potent inhibitor of BRAF ^V600E/CRAF with IC₅₀s of 0.888 and 0.229 μM, respectively. BRAF V600E/CRAF-IN-2 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-2 has the potential for the research of cancer diseases.