Raf Inhibitor

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.

Rineterkib (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF.

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.

TBAP-001 (Synthesis 13), extracted from patent WO2015075483A1, is a pan-RAF kinase inhibitor, with an IC₅₀ of 62 nM in BRAF V600E kinase assay.

MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 blocks the interaction of Ras with Raf. MCP110 disrupts this interaction might can be used for the research of human tumors.

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.

Flezurafenibum (Flezurafenib) is a rapidly accelerated fibrosarcoma (Raf) kinase inhibitor, with antineoplastic effect.

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.

RRD-251 is an inhibitor of retinoblastoma tumor suppressor protein (Rb)-Raf-1 interaction, with potent anti-proliferative, anti-angiogenic and anti-tumor activities.

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).

TAT-Braftide is a peptide inhibitor designed to block the dimerization of BRAF, thereby inhibiting its kinase activity. The destruction of BRAF dimer by TAT-Braftide makes BRAF protein more susceptible to proteasome degradation, directly inhibits the activity of BRAF kinase, and reduces the activation of MAPK signaling pathway. Tat-braftide can be used for the role of RAF kinase in MAPK signaling pathway and for the study of BRAF mutant cancers.

PLX7922, a RAF inhibitor, can bind with BRAF^V600E. PLX7922 inhibits pERK in BRAF^V600E cell lines, and activates pERK in mutant NRAS cell lines.

Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAF^G469A with IC₅₀ of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells (EC₅₀ is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence. Braftide can be used for cancer research.

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

BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC₅₀ of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile.