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Isoforms Recommended:	B-Raf

Results for "

BRAF-V600E

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (15) Aurora Kinase (1) Autophagy (2) Bcl-2 Family (5) Bcr-Abl (1) c-Fms (1) Caspase (3) EGFR (10) Endogenous Metabolite (1) ERK (3) Isotope-Labeled Compounds (3) JNK (2) Ligands for E3 Ligase (1) MEK (7) NO Synthase (1) Oxidative Phosphorylation (2) P-glycoprotein (2) p38 MAPK (3) Parasite (2) PERK (3) PROTACs (4) Raf (55) Ras (1) Reference Standards (3) Tie (1) VEGFR (3)
By Research Areas:	Cancer (63) Infection (2) Inflammation/Immunology (2)

Inhibitors & Agonists

Peptides

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15605

Encorafenib Maximum Cited Publications 45 Publications Verification 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-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-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-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-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-11004

AZ 628 10+ Cited Publications	Raf Apoptosis	Cancer
AZ 628 is a pan-Raf kinase inhibitor with IC₅₀s of 105, 34 and 29 nM for *B-Raf, B-RafV600E, and c-Raf-1*, respectively.

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-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-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-15605S

Encorafenib-13C,d3 LGX818-¹³C,d₃	Isotope-Labeled Compounds Raf	Cancer
Encorafenib- ¹³C,d₃ is the ¹³C- and deuterium labeled Encorafenib. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).

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-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-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-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-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-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-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-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-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-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 .

HY-178995

BRAFV600E-IN-3	Raf	Cancer
BRAFV600E-IN-3 (Compound AV05) is a *BRAF ^V600E* inhibitor with an IC₅₀ value of 0.89 μM. BRAFV600E-IN-3 inhibits the proliferation of melanoma cells. BRAFV600E-IN-3 can be used for the study of melanoma .

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-51424R

PLX-4720 (Standard)	Raf	Cancer
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.

HY-173164

EGFR/BRAFV600E-IN-4	EGFR Raf Apoptosis	Cancer
EGFR/BRAFV600E-IN-4 (Compound 10f) is a dual EGFR and *BRAF ^V600E* inhibitor with IC₅₀ values of 61 nM and 43 nM, respectively. EGFR/BRAFV600E-IN-4 arrests cell cycle, induces apoptosis in both early and late stages and inhibits cancer cells growth in vitro, and has a broad anticancer activity .

HY-14660S

Dabrafenib-d9 GSK2118436A-d₉; GSK2118436-d₉	Isotope-Labeled Compounds Raf	Cancer
Dabrafenib-d₉ is the deuterium labeled Dabrafenib. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC₅₀s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively .

HY-19343

XL-281 BMS-908662	Raf	Cancer
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 .

HY-51424S

PLX-4720-d7	Isotope-Labeled Compounds Raf	Cancer
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 .

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-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-149517

EGFR/BRAFV600E-IN-2	EGFR Raf Caspase Bcl-2 Family Apoptosis	Inflammation/Immunology Cancer
EGFR/BRAFV600E-IN-2 (compound 3g) is a potential multi-target inhibitor of EGFR, *BRAF ^V600E, and EGFR ^T790M, and an inducer of apoptosis. EGFR/BRAFV600E-IN-2* can activate caspase-3, 8, and Bax, and downregulate the anti-apoptotic protein Bcl2, inducing apoptosis. EGFR/BRAF V600E-IN-2 also has antioxidant activity and DPPH free radical scavenging potency .

HY-147825

EGFR/BRAFV600E-IN-1	EGFR Raf Apoptosis	Cancer
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 .

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-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-108887

Anticancer agent 124	Raf	Cancer
Anticancer agent 124 is an orally active, highly selective and potent pan RAF inhibitor. Anticancer agent 124 inhibits MAPK signalling in BRAF V600E, NRAS and KRAS mutant tumor cells .

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 IC₅₀s of 2.0 and 0.8 μM. B-Raf IN 15 can be used for the research of cancer .

HY-169869

pan-Raf/RTK inhibitor 1	Raf	Cancer
Pan-Raf/RTK inhibitor 1 (compound I-16) is a potent pan-Raf inhibitor with IC₅₀ values of 3.49 nM (BRaf ^V600E), 8.86 nM (ARaf), 5.78 nM (BRaf ^WT), and 1.65 nM (CRaf). Pan-Raf/RTK inhibitor 1 exhibits antiproliferative activities against various cancer cell lines and can be utilized in cancer research .

HY-115933

*EGFR/BRAF-IN-1*	EGFR Raf	Cancer
EGFR/BRAF-IN-1 (compound 21), a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, is a potent *EGFR/BRAF* inhibitor with an IC₅₀ of 45 nM for BRAF ^V600E. EGFR/BRAF-IN-1 inhibits cancer cell proliferation (GI₅₀=35 nM). EGFR/BRAF-IN-1 shows good antioxidant activity .

HY-146492

*VEGFR-2/BRAF-IN-2*	VEGFR Raf Apoptosis	Cancer
VEGFR-2/BRAF-IN-2 (Compound 4a) is a dual VEGFR-2 and *BRAF* kinases inhibitor with IC₅₀ values of 0.111, 0.089 and 0.071 µM against VEGFR-2, *BRAF ^V600E* and BRAF ^WT, respectively. VEGFR-2/BRAF-IN-2 induces apoptosis and arrests the cell cycle mainly in the G1 phase .

HY-174274

ERK2-IN-6	ERK	Cancer
ERK2-IN-6 (Compound 20) is a highly selective ERK1/2 inhibitor with an IC₅₀ value of 7.9 nM for ERK2. ERK2-IN-6 inhibits the proliferation of BRAF ^V600E mutant cells (IC₅₀=250 nM in A375 cells). ERK2-IN-6 is promising for research of solid tumors, such as BRAF-mutated melanoma .

HY-146491

*VEGFR-2/BRAF-IN-1*	VEGFR Raf Apoptosis	Cancer
VEGFR-2/BRAF-IN-1 (Compound 4b) is a dual VEGFR-2 and *BRAF* kinases inhibitor with IC₅₀ values of 0.049, 0.063 and 0.005 µM against VEGFR-2, *BRAF ^V600E* and BRAF ^WT, respectively. VEGFR-2/BRAF-IN-1 induces apoptosis and arrests the cell cycle mainly in the G1/S phase .

HY-17598R

Rafoxanide (Standard)	Oxidative Phosphorylation Reference Standards Parasite p38 MAPK Raf Apoptosis	Infection Cancer
Rafoxanide (Standard) is the analytical standard of Rafoxanide. This product is intended for research and analytical applications. 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-164474

DS03090629	MEK	Cancer
DS03090629 is an orally active MEK inhibitor that inhibits MEK activity in an ATP-competitive manner. DS03090629 exhibits high affinity for both MEK and phosphorylated MEK, with K_d values of 0.11 and 0.15 nM, respectively. It effectively inhibits the proliferation of BRAF-mutant overexpressing melanoma cell lines, with IC₅₀ values of 74.3 and 97.8 nM for BRAF V600E and MEK1 F53L transfected A375 cells, respectively. DS03090629 holds potential value in the field of anti-melanoma therapy .

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 .

Cat. No.	Product Name	Chemical Structure

HY-15605S

Encorafenib-13C,d3
Encorafenib- ¹³C,d₃ is the ¹³C- and deuterium labeled Encorafenib. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).

HY-14660S

Dabrafenib-d9
Dabrafenib-d₉ is the deuterium labeled Dabrafenib. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC₅₀s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively .

HY-51424S

PLX-4720-d7
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 .

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