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Isoforms Recommended:	BRaf

Results for "

BRAF V600E

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (7) Aurora Kinase (1) Autophagy (3) c-Met/HGFR (1) CDK (1) EGFR (5) MEK (2) Oxidative Phosphorylation (2) p38 MAPK (3) Parasite (2) PROTACs (4) Raf (46) Src (1) VEGFR (2)
By Research Areas:	Cancer (46) Infection (2)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-137487

*PROTAC BRAF-V600E* degrader-1**	PROTACs Raf	Cancer
PROTAC BRAF-V600E degrader-1 is a potent PROTAC BRAF-V600E degrader with K_d value 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). PROTAC BRAF-V600E degrader-1 can inhibit melanoma cell growth .

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-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-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-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-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-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 .

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-147405

Tinlorafenib PF-07284890; ARRY-461	Raf	Cancer
Tinlorafenib (PF-07284890) (compound 10) is an orally active BRAF kinase inhibitor, with IC₅₀s of 4.25 and 2.7 nM for BRAF ^V600E/V600K respectively. 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 (ZINC72115182) is a selective B-Raf ^V600E inhibitor (IC₅₀=76 nM), shows selectivity for B-Raf ^V600E over B-Raf ^WT with selectivity of 3.1-fold. B-Raf IN 11 can be used in colorectal cancer research

HY-153341

CFT1946	PROTACs Raf	Cancer
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. CFT1946 is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAF ^V600E splice variant. CFT1946 can be used in tumor research .

HY-18972

Plixorafenib

15+ Cited Publications

PLX8394; FORE8394

PLX8394 is a potent and selective BRaf inhibitor, with an IC₅₀ of appr 5 nM for BRAF ^V600E.

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

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-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.

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-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-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-14177A

Raf inhibitor 1 dihydrochloride	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-15767

TAK-632

3 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.

TAK-632 3 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-15605

Encorafenib 15+ 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-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) .

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-51424

PLX-4720 5+ 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-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-18652

Avutometinib 1 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-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.

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-18957

Lifirafenib 1 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-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-14660

Dabrafenib 40+ 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-18957B

Lifirafenib maleate BGB-283 maleate	EGFR Raf	Others
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-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-109080

Belvarafenib 1 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-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 .

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-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-12057

Vemurafenib Maximum Cited Publications 65 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-17598

Rafoxanide 3 Publications Verification	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-12291

HG6-64-1 HMSL 10017-101-1	Raf	Cancer
HG6-64-1 is a potent and selective *B-Raf* inhibitor extracted from patent WO 2011090738 A2, example 9 (XI-1); has a IC₅₀ of 0.09 μM on B-raf V600E transformed Ba/F3 cells.

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-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-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-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-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-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-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-136420

SJF-0628	PROTACs Raf	Cancer
SJF-0628 (compound 512) is a PROTAC RAF degrader. SJF-0628 induces targeted degradation of BRAF mutants (DC₅₀: 5.4 nM, 4.64 nM, 15.5 nM, 2.11 nM, 63.9 nM for BRAF V600E, V600K, G464V, G469A, K601E respectively). SJF-0628 has anti-tumor activity. SJF-0628 can be used for research of disorders that result from aggregation or accumulation of RAF, or the constitutive activation of RAF .

HY-17598R

Rafoxanide (Standard)	Oxidative Phosphorylation 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-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-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-148059

Uplarafenib

B-Raf IN 10
Raf Cancer

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

HY-150639

Everafenib	Raf	Cancer
Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of ^V600EBRAF melanoma cell lines with IC₅₀ values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma .

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BRAF V600E

Inhibitors & Agonists