B-Raf Inhibitor

TAK-632 is a potent pan-RAF inhibitor with IC₅₀ of 1.4, 2.4 and 8.3 nM for CRAF, BRAF^V600E, BRAF^WT, respectively.

Raf inhibitor 1 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.

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.

Sorafenib (Standard) (Bay 43-9006 (Standard)) is the analytical standard of Sorafenib (HY-10201). This product is intended for research and analytical applications. Sorafenib (Bay 43-9006) 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 induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.

BRAF inhibitor. RG6344 can be used for the study of BRAF V600-mutant solid tumors, such as colorectal cancer (CRC).

CCT196969 is a pan-Raf inhibitor, which inhibits B-Raf, BRaf^V600E and CRAF with IC₅₀s of 0.1, 0.04, and 0.01 μM, respectively.

Tinlorafenib (PF-07284890) is the orally active inhibitor for BRAF and CRAF with IC₅₀s of 5.8 nM and 4.1 nM. Tinlorafenib (Compound 10) inhibits V600E mutated BRAF and V600K mutanted BRAF with IC₅₀s of 4.25 nM and 2.7 nM. Tinlorafenib can cross the blood brain barrier. Tinlorafenib demonstrates CNS penetration and can be used in the research of BRAF-associated malignant and benign tumors of the CNS as well as extracranial malignancies.

RAF709 is a potent, selective, and efficacious RAF inhibitor with IC₅₀s of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively. Antitumor efficacy.

N-trans-feruloyloctopamine is a natural hydroxycinnamic acid amide compound derived from garlic outer skin, possessing tyrosinase inhibition, FGF2 inhibition, anti-melanogenic, and anti-tumor activities. N-trans-feruloyloctopamine inhibits tyrosinase activity and downregulates tyrosinase mRNA and protein expression (IC₅₀ = 5.3 μM), and inhibits melanogenesis in α-MSH-stimulated B16F10 cells. N-trans-feruloyloctopamine inhibits Akt and p38 MAPK phosphorylation, binds to E-cadherin to block EMT, reduces Slug, inhibits hepatocellular carcinoma invasion, and induces hepatocellular carcinoma cell apoptosis. N-trans-feruloyloctopamine can be used in research related to hepatocellular carcinoma, pigmentation disorders, and UVB-induced skin damage.

PLX7904 is a potent and selective BRAF inhibitor, with IC₅₀ of appr 5 nM against BRAF^V600E in mutant RAS expressing cells.

Omzirafenib (LUT014) is a topical inhibitor targeting BRAF that cannot pass through the blood-brain barrier. Omzirafenib inhibits BRAF kinase and abnormally activates the MAPK/ERK signaling pathway, promoting the proliferation of epidermal keratinocytes, repairing skin barrier damage caused by radiation damage, and alleviating inflammatory responses. Omzirafenib is independent of RAS signaling and accelerates the repair and regeneration of damaged skin cells. Omzirafenib can be used to study radiation dermatitis, especially skin damage caused by breast cancer radiotherapy.

BRAF inhibitor (Compound P-0850) is a B-Raf inhibitor with anti-tumor activity.

L-779450 is a potent and selective B-Raf kinase inhibitor with a K_d of 2.4 nM.

BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAF^V600E-mutant, the WT BRAF and CRAF kinases with IC₅₀s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases.

B-Raf IN 11 is a B-Raf^V600E mutant kinase inhibitor with an IC₅₀ of 76 nM, and exhibits an IC₅₀ of 238 nM against wild-type B-Raf kinase. B-Raf IN 11 inhibits the kinase activities of B-Raf^V600E mutant and wild-type B-Raf kinase. B-Raf IN 11 is applicable to relevant research on colorectal cancer.

HG6-64-1 (HMSL 10017-101-1) is a B-raf kinase modulator.HG6-64-1 modulates B-raf kinase activity, including the V600E mutant form and the drug-resistant gatekeeper mutation T529I. HG6-64-1 is a germinal center kinase inhibitor. HG6-64-1 induces cell cycle arrest and apoptosis. HG6-64-1 can be used for the research of diffuse large B-cell lymphoma (DLBCL).

Uplarafenib (B-Raf IN 10) (Compound C09) is a BRAF inhibitor with an IC₅₀ between 50 and 100 nM. Uplarafenib shows antitumor activity.

AD57 is an orally active multikinase inhibitor, inhibits RET, BRAF, S6K and Src, with greatly reduces mTOR activity.

B-Raf IN 1 is a potent and selective B-Raf kinase inhibitor with an IC₅₀ of 24 nM.

Sorafenib-¹³C,d₃ (Bay 43-9006-¹³C,d₃) is the ¹³C, deuterated-labeled Sorafenib (HY-10201). Sorafenib (Bay 43-9006) 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 induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.