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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
71 Results for "
B-Raf V600E
" in MedChemExpress (MCE) Product Catalog:
Products (71)
71 Results for "B-Raf V600E" in MCE Product Catalog:
104
104 Publications Verification
Synonyms: PLX4032; RG7204; RO5185426
Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAF V600E and c-RAF-1, respectively . Vemurafenib induces cell autophagy .
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47
Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAF V600E (EC50=4 nM).
20
PLX8394 is a potent and selective BRaf inhibitor, with an IC50 of appr 5 nM for BRAF V600E.
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17 Cited Publications
Cat. No.: HY-51424
CAS No.: 918505-84-7
PLX-4720 is a potent and selective inhibitor of B-Raf V600E 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-Raf V600E than wild-type B-Raf.
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11
11 Cited Publications
Synonyms: RG 7421; MEK inhibitor 1
GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAF V600E, EC50=7 nM).
8
8 Cited Publications
Synonyms: CEP-32496; RXDX-105
Agerafenib (CEP-32496; RXDX-105) is a highly potent and orally efficacious inhibitor of BRAF V600E with a Kd of 14 nM.
7
7 Cited Publications
Cat. No.: HY-17598
CAS No.: 22662-39-1
Rafoxanide is a poent, orally active halogenated salicylaniline agent with antiparasitic activity. Rafoxanide interferes with energy metabolism in trematodes by uncoupling oxidative phosphorylation. Rafoxanide is also found to be a potent inhibitor of the BRAF V600E mutant protein, which is important in colorectal cancer. Rafoxanide can be used for the control of infestation with Hemonchus species or Fasciola species in sheep and cattle as well as Oestrus ovis in sheep. Rafoxanide can also be used for cancer research .
6
Avutometinib (Ro 5126766) is a first-in-class dual MEK/RAF inhibitor that allosterically inhibits BRAF V600E, CRAF, MEK, and BRAF (IC50: 8.2, 56, 160 nM, and 190 nM, respectively).
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6 Cited Publications
Synonyms: HM95573; GDC-5573; RG6185
Belvarafenib (HM95573) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAF v600E and C-RAF respectively .
5
5 Cited Publications
Target:
Research Areas:
TAK-632 is a potent pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAF V600E, BRAF WT, respectively.
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3
3 Cited Publications
Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively.
3
3
3 Cited Publications
Cat. No.: HY-14177A
CAS No.: 1191385-19-9
B-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively.
Synonyms: HL-085
Tunlametinib is a highly selective, orally active MEK1/2 inhibitor (IC50=1.9 nM, MEK1). Tunlametinib blocks the RAS-RAF-MEK-ERK signaling pathway, arrests tumor cell cycle and promotes apoptosis. Tunlametinib potently inhibits the proliferation of RAS/RAF mutant cancer cells (such as BRAF V600E, KRAS G12C mutant cells). Tunlametinib shows synergistic anti-tumor effects with BRAF/KRASG12C/SHP2 inhibitors, Docetaxel (HY-B0011). Tunlametinib can be used to study targeted therapy for RAS/RAF mutation-driven malignancies (such as melanoma, colorectal cancer, and non-small cell lung cancer) .
Synonyms: CFT1946
Tagarafdeg (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. Tagarafdeg is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAF V600E splice variant. Tagarafdeg can be used in tumor research .
SJF-0628 is a PROTAC degrader of BRAF mutants, with a DC50 of 6.8 nM against BRAF V600E. SJF-0628 induces the ubiquitination and degradation of BRAF mutants in various cancer cell lines. SJF-0628 reduces pMEK and pErk levels. SJF-0628 exhibits antitumor activity. SJF-0628 can be used in research on colorectal cancer, melanoma, lung cancer, and triple-negative breast 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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
