Raf Inhibitor

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

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.

B-Raf IN 6 (compound 2c) is a potent inhibitor of protein kinase B-Raf with an IC₅₀ of 1.7 nM. B-Raf IN 6 is devoid of binding to the secondary target PXR and resists rapid metabolism. B-Raf IN 6 has the potential for the research of cancer disease.

KRAS-IN-55 is a pan-KRAS inhibitor with IC₅₀ values of 4.3, 9.6 and 1.6 nM against KRAS^G12C, KRAS^G12D and KRAS^G12V, respectively. KRAS-IN-55 induces the formation of a new binding pocket on KRAS, thereby forming a high-affinity ternary complex with cyclophilin A (CYPA), inhibiting the interactions of KRAS with downstream effectors RAF and PI3K, and blocking oncogenic MAPK and PI3K signaling pathways. KRAS-IN-55 is applicable to cancer research such as colorectal cancer and non-small cell lung cancer.

BRAF V600E/CRAF-IN-1 (Compound 8b) is a potent inhibitor of BRAF ^V600E/CRAF. BRAF V600E/CRAF-IN-1 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-1 has the potential for the research of cancer diseases.

Erufosine is an inhibitor of PI3K/Akt and Ras/Raf/MAPK signaling pathways. Erufosine inhibits the activity of breast cancer cell lines MCF-7 and MDA-MB 231 (IC₅₀: 40.95/40.8 μM). Erufosine reduces the phosphorylation of PI3K (p85), Akt (PKB), and cRaf. Erufosine can be used in the study of breast cancer and myeloid leukemia.

EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAF^V600E dual inhibitor with IC₅₀s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC₅₀s of 1.2, 0.79, 1.3, and 1.23 µM, respectively.

CCT239065 is an orally available, effective inhibitor of the mutant protein kinase ^V600EBRAF (RAF) with anti-tumor activity. CCT239065 inhibits downstream signaling of ^V600EBRAF in cancer cells, blocking DNA synthesis and suppressing proliferation.

B-Raf IN 14 (Comp 25) is a BRAF inhibitor with IC₅₀ value of 11.08 μM, which can be used in cancer-related research.

MO-2097 is a RAF-1/HIF-1α inhibitor. MO-2097 induces RAF-1 destabilization, leading to a reduction in EMT-associated transcription factors and mesenchymal markers. MO-2097 inhibits HIF-1a protein expression mediated by hnRNPA2B1 under hypoxic and mimetic hypoxia. MO-2097 induces mitochondrial ROS, which leads to apoptosis in cells. MO-2097 effectively suppresses colorectal cancer metastasis by inhibiting the RAF/MEK/ERK signaling pathway. MO-2097 attenuates tumor growth in a xenograft HCT116 cell mouse model. MO-2097 can be used for the study of colorectal cancer.

ISIS 5132 sodium scrambled negative control is the sequence scrambled negative control of ISIS 5132 sodium.

AD57 hydrochloride is an orally active multikinase inhibitor, inhibits RET, BRAF, S6K and Src.

Antiproliferative agent-54 (Compound 6z) is the inhibitor for multiple kinases, such as ABL WT, B-RAF, EGFR, HCK, LYN A and SRC with IC₅₀ of 6-50 nM. Antiproliferative agent-54 inhibits proliferation of several cancer cell, inhibits HUVEC and HepG2, with EC₅₀ of 34 and 38 nM. Antiproliferative agent-54 exhibits good pharmacokinetic characteristics in rats.

ML786 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 also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC₅₀=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 can be used for the research of cancers.

INU-152 is a potent and selective B-Raf inhibitor. INU-152 reduces tumor cell proliferation, enhances autophagy, and induces apoptosis by inhibiting B-Raf activity. INU-152 exhibits significant cytotoxicity against cancer cells transformed with v-Ha-ras (Ras-NIH 3T3). INU-152 can be utilized in cancer research.

BJ-2302 is a Src kinase inhibitor with an IC₅₀ of 3.23 μM, and inhibits cathepsin S (CTSS) activity.BJ-2302 binds to Src, suppresses PI3K/AKT and Ras/Raf/ERK pathways, and reduces CTSS and MMP-9 expression.BJ-2302 inhibits cancer cell invasion, metastasis, proliferation, and tumor growth.BJ-2302 does not induce cytotoxicity in normal breast epithelial cells.BJ-2302 can be used for the research of breast cancer and triple-negative breast cancer.

Lifirafenib (BGB-283) maleate is a novel and potent Raf Kinase and EGFR inhibitor with IC₅₀ values of 23 and 29 nM for recombinant BRaf^V600E and EGFR, respectively.

ATWLPPRAANLLMAAS is a chimeric peptide with anti-angiogenic and potent anti-tumor effects. ATWLPPRAANLLMAAS can inhibit the proliferation, viability, migration, and invasion of human hepatocellular carcinoma cells, and induce apoptosis..

Raf inhibitor 3 (Example 30) is a Raf inhibitor. Raf inhibitor 3 inhibits B-Raf and C-Raf with IC₅₀ values less than 15 nM. Raf inhibitor 3 can be used for research of cancers.