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Isoforms Recommended: B-Raf
Results for "

B-RafV600E

" in MedChemExpress (MCE) Product Catalog:

30

Inhibitors & Agonists

3

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-11004
    AZ 628
    Maximum Cited Publications
    11 Publications Verification

    		 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.
    AZ 628
  • 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 Kd 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.
    PROTAC BRAF-V600E degrader-1
  • 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).
    Encorafenib-13C,d3
  • 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 .
    B-Raf IN 11
  • 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 .
    BRAFV600E-IN-2
  • 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.
    PLX-4720 (Standard)
  • 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 .
    Dabrafenib-d9
  • 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 .
    PLX-4720-d7
  • 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 .
    XL-281
  • 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)) .
    CST905
  • 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-109080A
    Belvarafenib TFA

    HM95573 TFA; GDC-5573 TFA; RG6185 TFA

    		 Raf Cancer
    Belvarafenib TFA (HM95573 TFA) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv 600E and C-RAF respectively .
    Belvarafenib TFA
  • HY-18957C
    Lifirafenib hydrochloride

    BGB-283 hydrochloride

    		 Endogenous Metabolite 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 .
    Lifirafenib hydrochloride
  • HY-178382
    BRAFV600E/ABL2-IN-1

    		Raf Bcr-Abl P-glycoprotein PERK Apoptosis Cancer
    BRAFV600E/ABL2-IN-1 is a BRAFV600E (IC50 = 0.088 μM)/ABL2 (IC50 = 0.3 μM) dual inhibitor. BRAFV600E/ABL2-IN-1 can diminish P-glycoprotein expression. BRAFV600E/ABL2-IN-1 effectively inhibits p-CrkL (Abl2 signaling) and p-ERK1/2 (BRAFV600E pathway) in A375-R melanoma cells. BRAFV600E/ABL2-IN-1 causes cell cycle arrest. BRAFV600E/ABL2-IN-1 significantly increases the percentage of late apoptotic cells. BRAFV600E/ABL2-IN-1 can be used for the study of melanoma .
    BRAFV600E/ABL2-IN-1
  • 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 .
    BRAFV600E-IN-1
  • 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 .
    EGFR/BRAFV600E-IN-3
  • 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 .
    BRAFV600E-IN-3
  • HY-172877
    EGFR/BRAFV600E-IN-5

    		Raf EGFR Apoptosis Bcl-2 Family Cancer
    EGFR/BRAFV600E-IN-5 (Compound 7I) is a dual BRAFV600E/EGFR inhibitor with IC50 of 0.048 μM and 0.037 μM, respectively. EGFR/BRAFV600E-IN-5 has significant anti-melanoma activity with IC50 of 3.16 μM and 2.50 μM against MALME-3M and LOX-IMVI cell lines, respectively. EGFR/BRAFV600E-IN-5 exerts anti-tumor effects by inducing G1 arrest, inhibiting DNA synthesis, and activating the mitochondrial apoptosis pathway. EGFR/BRAFV600E-IN-5 can be used for melanoma research, especially for combined inhibition of BRAFV600E mutation and EGFR signaling pathway .
    EGFR/BRAFV600E-IN-5
  • HY-173153
    BRAFV600E/JNK-IN-1

    		JNK PERK MEK NO Synthase Inflammation/Immunology Cancer
    BRAFV600E/JNK-IN-1 (Compound 14c) is an inhibitor of JNK1, JNK2, JNK3 and BRAFV600E, with IC50 values of 0.51 μM, 0.53 μM, 1.02 μM and 0.009 μM, respectively. BRAFV600E/JNK-IN-1 can inhibit the phosphorylation of MEK1/2 and ERK1/2. In addition, BRAFV600E/JNK-IN-1 can inhibit tumor cell proliferation, NO release and PGE2 production, and has anti-tumor and anti-inflammatory activities .
    BRAFV600E/JNK-IN-1
  • 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 .
    EGFR/BRAFV600E-IN-4
  • 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 .
    EGFR/BRAFV600E-IN-1
  • 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 .
    JNK-IN-18
  • 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 .
    EGFR/BRAFV600E-IN-2
  • 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 .
    B-Raf IN 19
  • 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 .
    MEK/RAF-IN-1
  • HY-180154
    EGFR/BRAFV600E-IN-6

    		EGFR Raf Caspase Bcl-2 Family Apoptosis Cancer
    EGFR/BRAFV600E-IN-6 (Compound 7c) is a dual EGFR/BRAF V600E inhibitor with IC50 values of 0.12 and 0.05 μM. EGFR/BRAFV600E-IN-6 can activate caspase-3/8/9, unregulate Bax expression and downregulate Bcl-2 levels. EGFR/BRAFV600E-IN-6 can induce apoptosis and shows antioxidant activity. EGFR/BRAFV600E-IN-6 can be used for the research of cancer, such as colon cancer .
    EGFR/BRAFV600E-IN-6
  • HY-181726
    BRAFV600E/ABL2-IN-2

    		PERK P-glycoprotein Apoptosis Cancer
    BRAFV600E/ABL2-IN-2 is a dual BRAFV 600E and ABL2 kinase inhibitor, with an IC50 of 0.088 μM against human BRAFV 600E and an IC50 of 0.3 μM against human ABL2. BRAFV600E/ABL2-IN-2 reduces the phosphorylation levels of downstream ERK1/2 and CrkL in melanoma cells. BRAFV600E/ABL2-IN-2 decreases the expression of P-glycoprotein (P-glycoprotein) in melanoma cells. BRAFV600E/ABL2-IN-2 induces G1 cell cycle arrest and apoptosis (Apoptosis) in melanoma cells. BRAFV600E/ABL2-IN-2 is applicable to relevant research on melanoma .
    BRAFV600E/ABL2-IN-2
  • HY-182763
    EGFR/BRAFV600E-IN-7

    		EGFR Raf Caspase Apoptosis Bcl-2 Family Cancer
    EGFR/BRAFV600E-IN-7 is a dual EGFR and BRAF V600E kinase inhibitor with human IC50 values of 0.12 μM, 0.80 μM, 1.20 μM for EGFR and 0.05 μM, 0.22 μM, 0.78 μM for BRAF V600E.EGFR/BRAFV600E-IN-7 interacts with key ATP-binding site residues of EGFR and BRAF V600E, including hydrogen bonding with EGFR Met769 and BRAF V600E Cys532.EGFR/BRAFV600E-IN-7 induces apoptosis via caspase-3/8/9 activation, modulates Bax and Bcl-2 expression, scavenges free radicals, and exhibits antiproliferative activity against human cancer cell lines.EGFR/BRAFV600E-IN-7 displays drug-likeness with no PAINS/Brenk structural alerts per in silico predictions.EGFR/BRAFV600E-IN-7 can be used for the research of colon cancer, pancreatic cancer, lung cancer, breast cancer .
    EGFR/BRAFV600E-IN-7
  • HY-107779R
    BI-882370 (Standard)

    		Reference Standards Raf Cancer
    BI-882370 (Standard) is the analytical standard of BI-882370 (HY-107779). This product is intended for research and analytical applications. 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 BRAFV600E-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 (Standard)
  • HY-182103
    ZAK-IN-2

    		MAP3K Caspase p38 MAPK Cardiovascular Disease
    ZAK-IN-2 (Compound 8) is a selective, covalent ZAK inhibitor with an IC50 of 11.5 nM. ZAK-IN-2 forms a covalent bond with Cys22 in the P-loop of ZAK to inhibit its kinase activity. ZAK-IN-2 inhibits the phosphorylation of the downstream target p38. ZAK-IN-2 blocks Doxorubicin (HY-15142A)-induced cleavage of Caspase 3. ZAK-IN-2 is applicable to research related to myocardial hypertrophy .
    ZAK-IN-2

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