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V600E BRAF

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55

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Products

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 Kd 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 .
    PROTAC BRAF-V600E degrader-1
  • 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
  • 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 .
    Tinlorafenib
  • 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
    B-Raf IN 11
  • 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 .
    CFT1946
  • HY-137488
    PROTAC BRAF-V600E degrader-2

    		PROTACs Raf Cancer
    PROTAC BRAF-V600E degrader-2 (compound 12) is a potent BRAF-V600E degrader with Kds 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 .
    PROTAC BRAF-V600E degrader-2
  • 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 .
    BRAF V600E/CRAF-IN-1
  • 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 .
    BRAF V600E/CRAF-IN-2
  • 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 .
    RAF-IN-1
  • 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 .
    Anticancer agent 124
  • 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.
    Plixorafenib
  • 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 Kd of 14 nM.
    Agerafenib hydrochloride
  • 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 .
    EBI-907
  • 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
  • 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.
    STAT3-IN-19
  • 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 .
    SHR902275
  • 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 Kd of 14 nM.
    Agerafenib
  • HY-14177A
    Raf inhibitor 1 dihydrochloride

    		Raf Cancer
    B-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively.
    Raf inhibitor 1 dihydrochloride
  • 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.
    TAK-632
  • HY-15605
    Encorafenib
    20+ 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).
    Encorafenib
  • 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
  • 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.
    PLX-4720
  • HY-14177
    Raf inhibitor 1
    3 Publications Verification

    		 Raf Cancer
    Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively.
    Raf inhibitor 1
  • 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).
    Avutometinib
  • 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
  • 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.
    Lifirafenib
  • 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 .
    B-Raf IN 15
  • HY-14660
    Dabrafenib
    50+ 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 .
    Dabrafenib
  • 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 .
    Lifirafenib maleate
  • 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.
    LY3009120
  • HY-109080
    Belvarafenib
    3 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 .
    Belvarafenib
  • 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
  • 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).
    Encorafenib (Standard)
  • 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 .
    RAF mutant-IN-1
  • HY-14660R
    Dabrafenib (Standard)

    		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 .
    Dabrafenib (Standard)
  • HY-12057
    Vemurafenib
    Maximum Cited Publications
    73 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 .
    Vemurafenib
  • 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 .
    Rafoxanide
  • 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.
    HG6-64-1
  • 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 .
    CCT241161
  • 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 .
    EGFR/BRAF-IN-1
  • 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 .
    VEGFR-2/BRAF-IN-2
  • 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 .
    AZ304
  • 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 .
    VEGFR-2/BRAF-IN-1
  • HY-12057R
    Vemurafenib (Standard)

    		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 .
    Vemurafenib (Standard)
  • 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 .
    BI-882370
  • 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 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAF V600E, EC50=7 nM).
    GDC-0623
  • 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 .
    Vem-L-Cy5
  • 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 .
    SJF-0628
  • 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 Kd 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 .
    DS03090629
  • 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 .
    Rafoxanide (Standard)

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