Search Result

Isoforms Recommended:	BRaf

Results for "

BRAF-V600E

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (8) Aurora Kinase (1) Autophagy (2) c-Fms (1) EGFR (5) ERK (1) Isotope-Labeled Compounds (2) JNK (1) MEK (5) Oxidative Phosphorylation (2) p38 MAPK (2) Parasite (2) PROTACs (4) Raf (40) Ras (1) Tie (1) VEGFR (3)
By Research Areas:	Cancer (44) Infection (2)

Inhibitors & Agonists

Isotope-Labeled Compounds

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-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-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-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-168512

BRAFV600E-IN-1	Raf	Cancer
BRAFV600E-IN-1 (compound 9S) is a *BRAF* inhibitor. BRAFV600E-IN-1 has a significant apoptosis-inducing effect in cell lines expressing mutant KRAS and cancer cells expressing BRAFV600E .

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-155942

STAT3-IN-19	Others	Others
STAT3-IN-19 (compound 31) is a BRAF(V600E) inhibitor that has the function of inhibiting BRAF(V600E) activity. Its inhibitory mode and activity were determined through relevant screening and structural studies, and it has an inhibitory effect on MAPK signaling in melanoma cells.

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-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-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-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-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-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-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-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-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-15605

Encorafenib Maximum Cited Publications 27 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-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-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-18652

Avutometinib 3 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.

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-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-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-15605R

Encorafenib (Standard)	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-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-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-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-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-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-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-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-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-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 .

HY-149518

EGFR/BRAFV600E-IN-3	EGFR Apoptosis	Others
EGFR/BRAFV600E-IN-3 is a EGFR, *BRAFV600E* and EGFRT790M inhibitor with IC₅₀ value of 57 nM, 68 nM and 9.70 nM. EGFR/BRAFV600E-IN-3 is an apoptotic inducer and also displays promising antioxidant activity .

HY-18957C

Lifirafenib hydrochloride BGB-283 hydrochloride	Others	Cancer
Lifirafenib hydrochloride (BGB-283 hydrochloride) is a novel, reversible B-RAFV600E inhibitor with antitumor activity. Lifirafenib has shown potent antitumor activity against solid tumors with B-RAFV600E mutations, such as melanoma, thyroid cancer, and low-grade serous ovarian cancer. Lifirafenib exhibits selective cytotoxicity in vitro, preferentially inhibiting the proliferation of cancer cells with B-RAFV600E and EGFR mutations/amplification. Lifirafenib can achieve dose-dependent inhibition of tumor growth in animal models, accompanied by partial and complete tumor shrinkage .

HY-164529

SJ-C1044	Raf Ras MEK ERK VEGFR Tie c-Fms	Cancer
SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and *BRAF (V600E)* with IC₅₀ values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC₅₀ values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer .

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-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[4].

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-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	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[1][2].

HY-162873

MEK/RAF-IN-1	MEK Raf	Cancer
MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both MEK and RAF. It shows potent inhibition with IC₅₀ values of 28 nM for MEK1, and 3 nM each for *BRAF* and *BRAFV600E*. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer .

Cat. No.	Product Name	Chemical Structure

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[4].

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-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[1][2].

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: