B-Raf Inhibitor

B-Raf Inhibitors (78):

Art. -Nr.	Produktname	Wirkung	Reinheit

HY-144269

SHR902275	Inhibitor	99.80%
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-12847

CCT241161	Inhibitor	99.77%
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-15199

Agerafenib hydrochloride	Inhibitor
Agerafenib hydrochloride is a highly potent and orally efficacious inhibitor of BRAF^V600E with a K_d of 14 nM.

HY-117273

AZ304	Inhibitor	99.77%
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-15198

KG5	Inhibitor	99.79%
KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities.

HY-10331B

Regorafenib mesylate	Inhibitor
Regorafenib (BAY 73-4506) mesylate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC₅₀ values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib mesylate shows very robust antitumor and antiangiogenic activity.

HY-126298

RAF mutant-IN-1	Inhibitor
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-115933

EGFR/BRAF-IN-1	Inhibitor
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-13810

PF-04880594	Inhibitor
PF-04880594 is a potent and selective RAF inhibitor. PF-04880594 inhibits both wild-type and mutant BRAF and CRAF. PF-04880594 shows antitumor activity.

HY-178995

BRAFV600E-IN-3	Inhibitor
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.

HY-150250

B-Raf IN 13	Inhibitor
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-146492

VEGFR-2/BRAF-IN-2	Inhibitor
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-175831

BRAFV600E-IN-2	Inhibitor
BRAFV600E-IN-2 is a BRAF V600E inhibitor with IC₅₀ ≤10 nM. BRAFV600E-IN-2 has anti-tumor activity.

HY-149517

EGFR/BRAFV600E-IN-2	Inhibitor
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.

HY-147854

B-Raf IN 9	Inhibitor
B-Raf IN 9 (compound 8b) is a potent B-Raf inhibitor, with an IC₅₀ of 24.79 nM. B-Raf IN 9 induces apoptosis and shows cell cycle arrest at G2/M phase. B-Raf IN 9 exhibits potent antitumor activity against human prostate cancer PC-3 cell line, with an IC₅₀ of 7.83 µM.

HY-146491

VEGFR-2/BRAF-IN-1	Inhibitor
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-147852

B-Raf IN 7	Inhibitor
B-Raf IN 7 (compound 6a) is a potent B-Raf inhibitor, with an IC₅₀ of 110.23 nM. B-Raf IN 7 exhibits antitumor activity against colon carcinoma (HCT-116), mammary gland (MCF-7), hepatocellular carcinoma (HEPG-2), human cervical carcinoma (Hela) and human prostate cancer (PC-3) cells, with IC₅₀ values of 7.50, 9.87, 10.57, 11.63 and 12.83 µM.

HY-168512

BRAFV600E-IN-1	Inhibitor
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-162873

MEK/RAF-IN-1	Inhibitor
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-16063

ARQ-736	Inhibitor
ARQ-736 is a potent and selective B-RAF inhibitor that plays an important role in cancer study.

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