B-Raf 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.

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.

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.

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

Takeda-6D (compound 6d) is an orally active and potent BRAF/VEGFR2 inhibitor, with IC₅₀ values of 7.0 and 2.2 nM, respectively. Takeda-6D shows antiangiogenesis by suppressing the VEGFR2 pathway in 293/KDR and VEGF-stimulated HUVEC cells.Takeda-6D shows significant suppression of ERK1/2 phosphorylation. Takeda-6D shows antitumor activity.

SB-590885 GMP is SB-590885 (HY-10966) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. SB-590885 is a BRAF/c-Raf kinase inhibitor that selectively targets B-Raf, and it amplifies the ERK/MAPK signaling pathway in RAS-activated cells. SB-590885 effectively inhibits the malignant proliferation, transformation and tumorigenicity of oncogenic B-Raf cells; it also induces the proliferation of erythroid progenitor cells, delays their differentiation and promotes hemoglobin synthesis, thereby improving ineffective erythropoiesis and reducing apoptosis. SB-590885 exerts a synergistic effect with TGF-β inhibitors and glucocorticoids, significantly promoting the formation of erythroid colonies in cells from patients with Diamond-Blackfan anemia (DBA). SB-590885 is mainly used in relevant studies on DBA, cisplatin-induced myelosuppression-related anemia, and pan-cancers such as melanoma and colorectal cancer.

COX/5-LO-IN-2 is a COX2, EGFR, COX1, 5-LOX, BRAF and FAK inhibitor with IC₅₀ of 1.22 μM, 2.5 μM, 2.95 μM, 4.65 μM, 7.4 μM, 12.2 μM, respectively. COX/5-LO-IN-2 induces cell growth arrest at G2/M phase. COX/5-LO-IN-2 triggers apoptotic activity by up-regulating proapoptotic proteins p53, Bax, and caspase-7 and down-regulating anti-apoptotic protein Bcl-2. COX/5-LO-IN-2 can be used for the research of breast 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.

RAF-IN-1 is a RAF inhibitor with IC₅₀ values ​​of 29.4 nM, 3.8 nM, and 36 nM against human recombinant bRAF^V600E, cRAF, and bRAF^WT enzymes, respectively. RAF-IN-1 suppresses RAF enzymatic activity and reduces cancer cell proliferation. RAF-IN-1 can be used for cancer research.

Multi-target kinase-IN-8 (3d) is an anti-cancer agent. Multi-target kinase-IN-8 exhibits inhibitory activity against various protein kinases (B-Raf V600E (IC₅₀ = 0.078 µg/mL), c-Met (IC₅₀ = 0.405 µg/mL), Pim-1 (IC₅₀ = 1.053 µg/mL), EGFR WT (IC₅₀ = 0.177 µg/mL), VEGFR-2 (IC₅₀ = 0.275 µg/mL)). Multi-target kinase-IN-8 can induce cell cycle arrest and promote early and late apoptosis. Multi-target kinase-IN-8 is commonly used in cancer research.

Multi-kinase-IN-5 (compound 15c) is a promising multi-kinase inhibitory agent. Multi-kinase-IN-5 inhibits a panel of protein kinases (RET, KIT, cMet, VEGFR1,2, FGFR1, PDGFR and BRAF), showing % inhibition of 74%, 31%, 62%, 40%, 73%, 74%, 59%, and 69%, respectively, and IC₅₀ of 1.287, 0.117 and 1.185 μM against FGFR1, VEGFR, and RET kinases, respectively.

B-Raf-IN-20 (Compound Z-001) is a B-RAF inhibitor with an IC₅₀ value of 37.80 nM. B-Raf-IN-20 binds to DFG-out/C-helix-in conformation in the B-RAF kinase. B-Raf-IN-20 has anti-cancer activity against non-small cell lung cancer.

PROTAC BRAF-V600E degrader-2 is a PROTAC degrader targeting BRAF-V600E. The K_d values of PROTAC BRAF-V600E degrader-2 for BRAF and BRAF-V600E are 14.4 nM and 9 nM, respectively. PROTAC BRAF-V600E degrader-2 selectively degrades BRAF-V600E but does not degrade wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits the MEK/ERK kinase cascade and suppresses the growth of melanoma cells. PROTAC BRAF-V600E degrader-2 can be used in studies related to melanoma and colon 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.

B-Raf IN 8 (compound 7g) is a potent B-Raf inhibitor, with an IC₅₀ of 70.65 nM. B-Raf IN 8 exhibits antitumor activity against hepatocellular carcinoma (HEPG-2), colon carcinoma (HCT-116), mammary gland (MCF-7) and human prostate cancer (PC-3) cells, with IC₅₀ values of 9.78, 13.78, 18.52 and 29.85 µM.

BRAFV600E/ABL2-IN-1 is a BRAF^V600E (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 (BRAF^V600E 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.

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 18 (compound 26) is a B-Raf inhibitor, with IC₅₀ of 3.8 nM. B-Raf IN 18 can be used in anti-cancer related research.

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.

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.