Raf Inhibitor

Belvarafenib (Standard) is the analytical standard of Belvarafenib (HY-109080). This product is intended for research and analytical applications. 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.

BRAF inhibitor (Standard) is the analytical standard of BRAF inhibitor (HY-10247). This product is intended for research and analytical applications. BRAF inhibitor (Compound P-0850) is a B-Raf inhibitor with anti-tumor activity.

XL-281 (BMS-908662) is an orally active inhibitor for RAF kinase, with IC₅₀s of 2.6, 4.5 and 6 nM, for CRAF, B-RAF, and B-RAFV600E, respectively. XL-281 exhibits antitumor activity.

RAF-IN-4 (Compound 120) is a Raf Kinase inhibitor. RAF-IN-4 shows IC₅₀ values of 134.3, 118.6 and 276.7 nM for B-Raf, B-Raf (V600E) and C-Raf. RAF-IN-4 can inhibit the proliferation of cancer cells by blocking the Raf signaling pathway. RAF-IN-4 can be used for research of cancer, such as lung cancer and breast cancer.

IHMT-RAF-128, a highly potent pan-RAF inhibitor. IHMT-RAF-128 shows potent antitumor efficacy in xenograft mouse tumor models without causing any apparent toxicities.

DPQZ is an anti-tubulin agent that inhibits cell separation and induces cell cycle arrest at the G2/M phase. In addition, DPQZ induces caspase-dependent apoptosis of HSC-3 cells by inhibiting Ras/Raf and activating MAP kinase. DPQZ can be used in the study of oral cancer.

Encorafenib (Standard) is the analytical standard of Encorafenib. This product is intended for research and analytical applications. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAF^V600E (EC₅₀=4 nM).

SKLB646 is an orally active multi-target kinase inhibitor. SKLB646 shows significant inhibitory effects on SRC and VEGFR2 with IC₅₀ values ??of 0.002 μmol/L and 0.012 μmol/L, respectively. SKLB646 also shows significant inhibitory effects on B-Raf and C-Raf with IC₅₀ values ??of 0.022 μmol/L and 0.019 μmol/L, respectively. SKLB646 inhibits the activation of the SRC signaling pathway and blocks the MAPK signaling pathway by inhibiting Raf kinase. In addition, SKLB646 can inhibit the proliferation, migration and invasion of human umbilical vein endothelial cells (HUVEC) to inhibit tumor-induced angiopoietic formation. SKLB646 shows significant anti-proliferative and anti-survival activities against triple-negative breast cancer (TNBC) cell lines.

Sorafenib (tosylate) (Standard) (Bay 43-9006 (tosylate) (Standard)) is the analytical standard of Sorafenib (tosylate) (HY-10201A). This product is intended for research and analytical applications. Sorafenib (Bay 43-9006) tosylate is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib tosylate induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib tosylate inhibits tumor growth and metastasis in mouse and rat models. Sorafenib tosylate can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.

CP-724714 succinate is an orally active and selective HER2 tyrosine kinase inhibitor with an IC₅₀ of 10 nM. CP-724714 succinate inhibits HER2 receptor autophosphorylation and blocks the downstream Ras-Raf-Mek-Erk signaling pathway, thereby inducing cell cycle arrest and apoptosis in tumor cells. CP-724714 succinate exhibits antiviral activity and inhibits various porcine diarrheal coronaviruses, including SADS-CoV (IC₅₀ of 0.91 μM). CP-724714 succinate is an inhibitor of the hepatic transport receptors OATP1B1/MDR1/BSEP, and can enter hepatocytes via active uptake and trigger the accumulation of drugs and bile acids within hepatocytes. CP-724714 succinate can be used in research related to HER2-overexpressing breast cancer and porcine diarrheal coronavirus infection.

Dabrafenib (Mesylate) (Standard) is the analytical standard of Dabrafenib (Mesylate). This product is intended for research and analytical applications. Dabrafenib Mesylate is a potent and selective Raf kinase inhibitor with IC50s of 0.6 and 5.0 nM for RafV600E and c-Raf, respectively.

B-Raf-IN-21 is a B-Raf kinase inhibitor with a K_d of 4.8 nM and an IC₅₀ of 6 nM. B-Raf-IN-21 can be used for the research of stroke.

PLX-4720-d₇ is the deuterium labeled PLX-4720. PLX-4720 is a potent and selective inhibitor of?B-RafV600E?with?an 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.

RAF265 (Standard) is the analytical standard of RAF265 (HY-10248). This product is intended for research and analytical applications. RAF265 is a potent and orally active RAF/VEGFR2 inhibitor.

BI-882370 (Standard) is the analytical standard of BI-882370 (HY-107779). This product is intended for research and analytical applications. BI-882370 is a potent and selective RAF K_inase inhibitor that binds to the ATP binding site of the K_inase positioned in the DFG-out (inactive) conformation of the BRAF K_inase. BI-882370 (BI 882370) inhibits the oncogenic BRAFV600E-mutant, the WT BRAF and CRAF K_inases with IC₅₀s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family K_inases.

Regorafenib (Hydrochloride) (Standard) is the analytical standard of Regorafenib (Hydrochloride). This product is intended for research and analytical applications. Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.

B-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with K_is of 1 nM, 1 nM, and 0.3 nM for B-Raf^WT, B-Raf^V600E, and C-Raf, respectively.

AFG210 is a potent multi-target kinase inhibitor that primarily inhibits Abl kinase (IC₅₀=330 nM), and also has inhibitory effects on other kinases such as B-Raf, C-Raf, FGFR-1, RET and VEGF receptors. AFG210 can be used to study chronic myeloid leukemia and other diseases with abnormal activation of Abl kinase.

AZ 628 (Standard) is the analytical standard of AZ 628 (HY-11004). This product is intended for research and analytical applications. AZ 628 is a pan-Raf K_inase inhibitor with IC₅₀s of 105, 34 and 29 nM for B-Raf, B-RafV600E, and c-Raf-1, respectively.

PLX-4720 (Standard) is the analytical standard of PLX-4720. This product is intended for research and analytical applications. 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.