B-Raf
B-Raf is a serine/threonine protein kinase encoded by BRAF and functions as a central signal transducer in the RAS-RAF-MEK-ERK signaling cascade that regulates cell proliferation, differentiation, and survival[1][2]. Mechanistically, activated B-Raf phosphorylates MEK, leading to ERK activation and propagation of mitogenic signaling, making B-Raf a critical regulator of MAPK pathway output[2]. Dysregulation of this pathway is strongly linked to oncogenesis, and somatic BRAF mutations are among the most common kinase alterations identified in human cancer, particularly melanoma, colorectal cancer, thyroid cancer, and non-small-cell lung cancer[1][3]. In disease models, the canonical BRAF V600E mutation constitutively activates kinase signaling and promotes tumor cell growth independent of normal upstream regulatory inputs[2][3]. Compared with the related RAF isoforms A-Raf and C-Raf (RAF1), B-Raf displays stronger basal kinase activity and is the most potent activator of MEK-ERK signaling, making it a dominant MAPK pathway driver in many BRAF-mutant tumors[2]. For experimental applications, selective B-Raf inhibitors have been widely used to suppress oncogenic MAPK signaling and to investigate pathway dependence in cancer models[4]. The development of mutation-selective inhibitors, including compounds targeting BRAF V600E, established B-Raf as a validated therapeutic and mechanistic target and continues to support research on signaling regulation, drug resistance, and combination treatment strategies[4][5].
References:
- [1]. Davies H, et al. Mutations of the BRAF gene in human cancer. Nature. 2002 Jun 27;417(6892):949-54. [Content Brief]
- [2]. Wan PT, et al. Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF. Cell. 2004 Mar 19;116(6):855-67. [Content Brief]
- [3]. B-Raf gene information from NCBI.
- [4]. Tsai J, et al. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci U S A. 2008 Feb 26;105(8):3041-6. [Content Brief]
- [5]. Bollag G, et al. Vemurafenib: the first drug approved for BRAF-mutant cancer. Nat Rev Drug Discov. 2012 Nov;11(11):873-86. [Content Brief]
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B-Raf Related Products (95)
Related Products (95)
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Antibodies (3)
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Sorafenib-13C,d3
0 ImagesSynonyms: Bay 43-9006-13C,d3Sorafenib-13C,d3 (Bay 43-9006-13C,d3) is the 13C, deuterated-labeled Sorafenib (HY-10201). Sorafenib (Bay 43-9006) is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.
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GNE-9815
0 ImagesGNE-9815 (compound 7) is a highly selective, pan-RAF inhibitor with good oral bioavailability. GNE-9815 exhibits Ki values of 0.062 and 0.19 nM for CRAF and BRAF, respectively. GNE-9815 combines with MEK inhibitor Cobimetinib (HY-13064) shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of KRAS mutant cancers.
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SHR902275
0 ImagesSHR902275 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, bRAFwt, and bRAFV600E, 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.
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CCT241161
0 ImagesCCT241161 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.
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Agerafenib hydrochloride
0 ImagesCat. No.: HY-15199CAS No.: 1227678-26-3Synonyms: CEP-32496 hydrochloride; RXDX-105 hydrochlorideAgerafenib hydrochloride is a highly potent and orally efficacious inhibitor of BRAFV600E with a Kd of 14 nM.
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AZ304
0 ImagesAZ304 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.
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Regorafenib mesylate
0 ImagesCat. No.: HY-10331BCAS No.: 835621-08-4Synonyms: BAY 73-4506 mesylateRegorafenib (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.
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Sorafenib-d4
0 ImagesSynonyms: Bay 43-9006-d4Sorafenib-d4 (Bay 43-9006-d4) is the deuterated-labeled Sorafenib (HY-10201). Sorafenib (Bay 43-9006) is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.
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EGFR/BRAF-IN-1
0 ImagesCat. No.: HY-115933CAS No.: 2906174-89-6EGFR/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 BRAFV600E. EGFR/BRAF-IN-1 inhibits cancer cell proliferation (GI50=35 nM). EGFR/BRAF-IN-1 shows good antioxidant activity.
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2,4,3',4',6'-Penta-O-(3-methylbutanoyl)sucrose
0 ImagesCat. No.: HY-N13841CAS No.: 150302-84-42,4,3',4',6'-Penta-O-(3-methylbutanoyl)sucrose is an FGFR3 and BRAF binder, and is an isovaleryl sucrose ester that can be found in Atractylodes japonica. 2,4,3',4',6'-Penta-O-(3-methylbutanoyl)sucrose shows low cytotoxicity against cancer cells.
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PF-04880594
0 ImagesCat. No.: HY-13810CAS No.: 1111636-35-1PF-04880594 is a potent and selective RAF inhibitor. PF-04880594 inhibits both wild-type and mutant BRAF and CRAF. PF-04880594 shows antitumor activity.
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B-Raf IN 13
0 ImagesCat. No.: HY-150250CAS No.: 2573782-74-6
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BRAFV600E-IN-2
0 ImagesCat. No.: HY-175831CAS No.: 3027070-47-6BRAFV600E-IN-2 is a BRAF V600E inhibitor with IC50 ≤10 nM. BRAFV600E-IN-2 has anti-tumor activity.
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EGFR/BRAFV600E-IN-2
0 ImagesCat. No.: HY-149517EGFR/BRAFV600E-IN-2 (compound 3g) is a potential multi-target inhibitor of EGFR, BRAFV600E, and EGFRT790M, 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.
