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Isoforms Recommended:	B-Raf

Results for "

B-Raf V600E

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (13) Aurora Kinase (1) Autophagy (4) Bcl-2 Family (4) c-Fms (1) c-Met/HGFR (2) Caspase (3) CDK (1) EGFR (10) ERK (4) JNK (1) Ligands for E3 Ligase (1) MEK (5) Oxidative Phosphorylation (2) p38 MAPK (4) Parasite (2) Pim (1) PROTACs (4) Raf (62) Ras (1) Reference Standards (4) Src (1) Tie (1) VEGFR (4)
By Research Areas:	Cancer (67) Infection (2) Inflammation/Immunology (1)

Inhibitors & Agonists

Peptides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-14660

Dabrafenib 75+ Cited Publications GSK2118436A; GSK2118436	Raf	Cancer
Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC₅₀s of 5 nM and 0.6 nM for C-Raf and B-Raf ^V600E, respectively .

HY-12057

Vemurafenib Maximum Cited Publications 103 Publications Verification PLX4032; RG7204; RO5185426	Raf Autophagy	Cancer
Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of *B-RAF* kinase, with IC₅₀s of 31 and 48 nM for RAF ^V600E and c-RAF-1, respectively . Vemurafenib induces cell autophagy .

HY-15605

Encorafenib 40+ Cited Publications LGX818	Raf	Cancer
Encorafenib (LGX818) is a highly potent *BRAF* inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAF ^V600E (EC₅₀=4 nM).

HY-18652

Avutometinib 4 Publications Verification Ro 5126766; CH5126766	MEK Raf	Cancer
Avutometinib (Ro 5126766) is a first-in-class dual MEK/RAF inhibitor that allosterically inhibits BRAF ^V600E, CRAF, MEK, and *BRAF* (IC₅₀: 8.2, 56, 160 nM, and 190 nM, respectively).

HY-12558

LY3009120 10+ Cited Publications DP-4978	Raf Autophagy	Cancer
LY3009120 (DP-4978) is a pan RAF inhibitor which inhibits BRAF ^V600E, BRAF ^WT and CRAF ^WT with IC₅₀s of 5.8, 9.1 and 15 nM, respectively.

HY-51424

PLX-4720 15+ Cited Publications	Raf	Cancer
PLX-4720 is a potent and selective inhibitor of B-Raf ^V600E 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-Raf ^V600E than wild-type B-Raf.

HY-109080

Belvarafenib 5 Publications Verification HM95573; GDC-5573; RG6185	Raf	Cancer
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-RAF ^v600E and C-RAF respectively .

HY-15610

GDC-0623 5+ Cited Publications RG 7421; MEK inhibitor 1	MEK Apoptosis	Cancer
GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (K_i=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC₅₀=42 nM) versus A375 (BRAF ^V600E, EC₅₀=7 nM).

HY-132844

Tunlametinib HL-085	MEK	Cancer
Tunlametinib is a highly selective, orally active MEK1/2 inhibitor (IC₅₀=1.9 nM, MEK1). Tunlametinib blocks the RAS-RAF-MEK-ERK signaling pathway, arrests tumor cell cycle and promotes apoptosis. Tunlametinib potently inhibits the proliferation of RAS/RAF mutant cancer cells (such as BRAF V600E, KRAS G12C mutant cells). Tunlametinib shows synergistic anti-tumor effects with BRAF/KRASG12C/SHP2 inhibitors, Docetaxel (HY-B0011). Tunlametinib can be used to study targeted therapy for RAS/RAF mutation-driven malignancies (such as melanoma, colorectal cancer, and non-small cell lung cancer) .

HY-15200

Agerafenib 5+ Cited Publications CEP-32496; RXDX-105	Raf	Cancer
Agerafenib (CEP-32496; RXDX-105) is a highly potent and orally efficacious inhibitor of BRAF ^V600E with a K_d of 14 nM.

HY-153341

Tagarafdeg CFT1946	PROTACs Raf	Cancer
Tagarafdeg (CFT1946) is an orally active, CRBN-based and mutant-selective bifunctional degradation activating compound (BiDAC) degrader of BRAF ^V600E with a DC₅₀ of 14 nM in A375 cells. Tagarafdeg is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAF ^V600E splice variant. Tagarafdeg can be used in tumor research .

HY-18972

Plixorafenib 15+ Cited Publications PLX8394; FORE8394	Raf	Cancer
PLX8394 is a potent and selective *BRaf* inhibitor, with an IC₅₀ of appr 5 nM for BRAF ^V600E.

HY-18957

Lifirafenib 2 Publications Verification BGB-283	EGFR Raf	Cancer
Lifirafenib (BGB-283) 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.

HY-15767

TAK-632 4 Publications Verification	Raf Aurora Kinase	Cancer
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.

HY-137487

*PROTAC BRAF-V600E* degrader-1**	PROTACs Raf	Cancer
PROTAC BRAF-V600E degrader-1 (compound 23) is a potent PROTAC BRAF-V600E degrader whlie no degradation activity against BRAF-WT. PROTAC BRAF-V600E degrader-1 exhibits K_d values of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS) and inhibits the growth of melanoma cells . (In the molecular structure, target protein ligand: BI-882370 (HY-107779), red part; E3 ubiquitin enzyme ligand: Pomalidomide (HY-10984), blue part; PROTAC linker: G007-LK (HY-12438), black part.

HY-14177

Raf inhibitor 1 3 Publications Verification	Raf	Cancer
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.

HY-17598

Rafoxanide 5+ Cited Publications	Oxidative Phosphorylation Parasite p38 MAPK Raf Apoptosis	Infection Cancer
Rafoxanide is a poent, orally active halogenated salicylaniline agent with antiparasitic activity. Rafoxanide interferes with energy metabolism in trematodes by uncoupling oxidative phosphorylation. Rafoxanide is also found to be a potent inhibitor of the BRAF V600E mutant protein, which is important in colorectal cancer. Rafoxanide can be used for the control of infestation with Hemonchus species or Fasciola species in sheep and cattle as well as Oestrus ovis in sheep. Rafoxanide can also be used for cancer research .

HY-18997

PLX7904 3 Publications Verification PB04	Raf	Cancer
PLX7904 is a potent and selective *BRAF* inhibitor, with IC₅₀ of appr 5 nM against BRAF ^V600E in mutant RAS expressing cells.

HY-107779

BI-882370	Raf	Cancer
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 .

HY-12846

CCT196969	Raf	Cancer
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.

HY-12291

HG6-64-1 HMSL 10017-101-1	Raf Apoptosis	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) .

HY-147405

Tinlorafenib PF-07284890; ARRY-461	Raf ERK	Cancer
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 .

HY-77113

B-Raf IN 11	Raf	Cancer
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 .

HY-12847

CCT241161	Raf Src Apoptosis	Cancer
CCT241161 is an orally active pan-RAF inhibitor with IC₅₀s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, *V600E-BRAF* and *BRAF, respectively. CCT241161 shows good activity to in BRAF* and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity .

HY-117273

AZ304	Raf Autophagy	Cancer
AZ304 is an ATP-competitive dual *BRAF* kinase inhibitor, potently inhibits wild type BRAF, V600E mutant BRAF and wild type CRAF, with IC₅₀s of 79 nM, 38 nM and 68 nM, respectively. AZ304 also has significant effect on other kinases, such as p38 (IC₅₀, 6 nM), CSF1R (IC₅₀, 35 nM). Anti-tumor activity .

HY-E70649

BRAF V600E Recombinant Human Active Protein Kinase	Raf	Cancer
BRAF is a member of the Raf kinase family of growth signal transduction protein kinases. BRAF has multiple mutants. BRAF V600E is commonly found in melanoma. BRAF V600E Recombinant Human Active Protein Kinase is a recombinant BRAF V600E protein that can be used to study BRAF V600E-related functions .

HY-136567

TBAP-001	Raf	Cancer
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 .

HY-149380

Vem-L-Cy5	Raf	Cancer
Vem-L-Cy5 (compound 3)，modified with the NIR fluorophore cyanine-5 (Cy5)，is a Vemurafenib (HY-12057)-based inhibitor of *BRAF. Vem-L-Cy5 targets to BRAF* ^V600E，and also inhibits MEK phosphorylation. Vem-L-Cy5 has cell permeability，and inhibits cell growth of many types of cancer .

HY-137488

*PROTAC BRAF-V600E* degrader-2**	PROTACs Raf	Cancer
PROTAC BRAF-V600E degrader-2 (compound 12) is a potent *BRAF-V600E* degrader with K_ds of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-2 selectively degraded the kinase domain of BRAF-V600E but not the wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits melanoma cell growth .

HY-175831

BRAFV600E-IN-2	Raf	Cancer
BRAFV600E-IN-2 is a **BRAF V600E inhibitor with IC₅₀** ≤10 nM. BRAFV600E-IN-2 has anti-tumor activity .

HY-155736

MAPK-IN-2	p38 MAPK EGFR Raf CDK c-Met/HGFR	Cancer
MAPK-IN-2 (compound 3h) is a potent MAPK inhibitor with antineoplastic activity. MAPK-IN-2 inhibits cancer cell proliferation among serval cancer cell lines, and suppresses MAPK pathway with potant efficacy (EGFR ^WT IC₅₀=281 nM, c-MET IC₅₀=205 nM, B-RAF ^WT IC₅₀=112 nM, and CDK4/6 IC₅₀=95 and 184 nM, respectively). MAPK-IN-2 even shows a remarkable potency against mutated EGFR and B-RAF (EGFR ^T790M IC₅₀=69 nM and B-RAF ^V600E IC₅₀=83 nM) .

HY-144269

SHR902275	Raf	Cancer
SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC₅₀s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAF ^wt, and bRAF ^V600E, respectively. SHR902275 shows cell growth inhibition with GI₅₀s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively .

HY-126298

RAF mutant-IN-1	Raf	Cancer
RAF mutant-IN-1 is a RAF kinase inhibitor, extracted from patent WO2019107987A1, with IC₅₀ values of 21 nM, 30 nM and 392 nM for C-RAF ^340D/Y341D, B-RAF ^V600E and B-RAF ^WT, respectively .

HY-15199

Agerafenib hydrochloride CEP-32496 hydrochloride; RXDX-105 hydrochloride	Raf	Cancer
Agerafenib hydrochloride is a highly potent and orally efficacious inhibitor of BRAF ^V600E with a K_d of 14 nM.

HY-144271

RAF-IN-1	Raf	Cancer
RAF-IN-1 is a potent b/cRAF inhibitor with an IC₅₀s of 3.8 nM, 36 nM, 29.4 nM for cRAF, bRAF ^wt, and bRAF ^V600E. RAF-IN-1 shows cell growth inhibition with GI₅₀s of 3.4 and 2.9 nM for H358 and A375 cell line bearing bRAF ^V600E mutation, respectively .

HY-146442

BRAF V600E/CRAF-IN-1	Raf	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 .

HY-14177A

Raf inhibitor 1 dihydrochloride 3 Publications Verification	Raf	Cancer
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.

HY-146443

BRAF V600E/CRAF-IN-2	Raf	Cancer
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 .

HY-175435

CST905	PROTACs Raf	Cancer
CST905 is a potent PROTAC degrader of *BRAF-V600E* with a DC₅₀ of 18 nM. CST905 is suitable for cancer research. (Structure Note: Pink: target protein ligand (HY-41747); Blue: E3 ligase ligand (HY-125845); Black: linker (HY-78378)) .

HY-107415

PLX7922	Raf	Cancer
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 .

HY-179098

Multi-target kinase-IN-8	Raf c-Met/HGFR Pim EGFR VEGFR Apoptosis	Cancer
Multi-target kinase-IN-8 (3d) is an anti-cancer agent. Multi-target kinase-IN-8 exhibits inhibitory activity against various protein kinases (B-Raf *V600E* (IC₅₀ = 0.078 µg/mL), c-Met (IC₅₀ = 0.405 µg/mL), Pim-1 (IC₅₀ = 1.053 µg/mL), EGFR WT (IC₅₀ = 0.177 µg/mL), VEGFR-2 (IC₅₀ = 0.275 µg/mL)). Multi-target kinase-IN-8 can induce cell cycle arrest and promote early and late apoptosis. Multi-target kinase-IN-8 is commonly used in cancer research .

HY-15605R

Encorafenib (Standard) LGX818 (Standard)	Reference Standards Raf	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).

HY-117707

EBI-907	Raf	Cancer
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 .

HY-150250

B-Raf IN 13	Raf	Cancer
B-Raf IN 13 is a BRAF inhibitor with an IC₅₀ of 3.55 nM in BRAF V600E enzyme assay. B-Raf IN 13 has anticaner effects (WO2020261156A1, Example 74) .

HY-153603

B-Raf IN 15	Raf	Cancer
B-Raf IN 15 (Compound 7) is a *BRAF* inhibitor. B-Raf IN 15 inhibits BRAF WT and **BRAF V600E with IC₅₀*s of 2.0 and 0.8 μM. B-Raf* IN 15 can be used for the research of cancer .

HY-155942

B-Raf IN 19	p38 MAPK Raf	Cancer
B-Raf IN 19 (compound 31) is a *BRAF* inhibitor that inhibits BRAF(WT) and BRAF(V600E) (IC₅₀: 0.57 μM and 0.28 μM, respectively). B-Raf IN 19 inhibits MAPK signaling in melanoma cells .

HY-14660R

Dabrafenib (Standard) GSK2118436A (Standard); GSK2118436 (Standard)	Reference Standards Raf	Cancer
Dabrafenib (Standard) is the analytical standard of Dabrafenib. This product is intended for research and analytical applications. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC₅₀s of 5 nM and 0.6 nM for C-Raf and B-Raf ^V600E, respectively .

HY-12057R

Vemurafenib (Standard) PLX4032 (Standard); RG7204 (Standard); RO5185426 (Standard)	Reference Standards Raf Autophagy	Cancer
Vemurafenib (Standard) is the analytical standard of Vemurafenib. This product is intended for research and analytical applications. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of *B-RAF* kinase, with IC₅₀s of 31 and 48 nM for RAF ^V600E and c-RAF-1, respectively . Vemurafenib induces cell autophagy .

HY-18957B

Lifirafenib maleate BGB-283 maleate	EGFR Raf	Others 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 .

HY-168125

JNK-IN-18	JNK	Cancer
JNK-IN-18 (compund 23b) is a JNK1 inhibitor with IC₅₀ of 2 nM, compared to JNK2 and BRAF(V600E) with IC₅₀ of 125 nM and 98 nM, respectively .

Cat. No.	Product Name	Target	Research Area

HY-P11706

MS1 peptide	Bcl-2 Family	Cancer
MS-1 peptide is a peptide for BH3 profiling. MS-1 peptide triggers higher depolarization of mitochondrial membrane in melanoma cells pre-treated with Encorafenib (HY-15605). MS1 peptide can be used for the research of BRAF ^V600E melanoma .

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