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Isoforms Recommended:	BRaf

Results for "

BRafV600E

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (4) Caspase (1) EGFR (4) Haspin Kinase (2) Isotope-Labeled Compounds (2) JNK (1) MEK (1) Microtubule/Tubulin (1) p38 MAPK (1) PARP (1) PROTACs (3) Raf (15)
By Research Areas:	Cancer (21)

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-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.

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-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-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-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-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-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-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-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 .

HY-149517

*EGFR/BRAFV600E-IN-2*	EGFR	Cancer
E07 aptamer is an aptamer that targets human epidermal growth factor receptor (hEGFR). E07 aptamer can compete with EGF for binding, binds to a novel epitope on EGFR. E07 aptamer binds to cells expressing EGFR, blocks receptor autophosphorylation, and prevents proliferation of tumor cells in three-dimensional matrices. E07 aptamer can be used for tomor disease research .

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-157800

Trilexium TRX-E-009-1	Microtubule/Tubulin Apoptosis PARP Caspase	Cancer
Trilexium (TRX-E-009-1) is a third-generation of benzopyran structurally related to TRX-E-002-1 (HY-114250). Trilexium increases p21 protein expression and induces apoptosis. Trilexium depolymerizes microtubules. Trilexium shows broad anti-cancer activity .

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-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-15217

CHR-6494 5+ Cited Publications	Haspin Kinase	Cancer
CHR-6494 is a potent inhibitor of haspin, with an IC₅₀ of 2 nM. CHR-6494 inhibits histone H3T3 phosphorylation. CHR-6494 can be used in the research of cancer .

HY-110350

CHR-6494 TFA	Haspin Kinase	Cancer
CHR-6494 TFA is a potent inhibitor of haspin, with an IC₅₀ of 2 nM. CHR-6494 TFA inhibits histone H3T3 phosphorylation. CHR-6494 TFA induces the apoptosis of cancer cells, including melanoma and breast cancer. CHR-6494 TFA can be used in the research of 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].

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