Avutometinib | Dual MEK/RAF inhibitor
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $100.00 | ||
| 25 mg | $375.00 |
Avutometinib (946128-88-7) is a dual MEK/RAF inhibitor (IC50s: MEK = 160 nM; CRAF = 56 nM; BRAF = 19 nM; BRAF V600E = 8nM).1 It directly inhibits unphosphorylated MEK without causing induction of MEK phosphorylation by RAF. The avutemetinib-MEK adduct is a dominant-negative inhibitor of RAF, stabilizing the MEK/RAF complex and locking in an inactive form. Avutometinib displayed efficacy across multiple RAS-mutated cancer cell lines and an SK-MEL-2 xenograft model.2 It displayed synergistic effects with eribulin against triple-negative breast cancer cell lines.3 Avutometinib also displayed efficacy in combination with the FAK inhibitor Defactinib in KRAS-mutated NSCLC cells.4
References/Citations:
- Ishii et al. (2013), Enhanced inhibition of ERK signaling by a novel allosteric MEK inhibitor, CH5126766, that suppresses feedback reactivation of RAF activity; Cancer Res. 73 4050
- Wada et al. (2014The Dual RAF/MEK Inhibitor CH5126766/RO5126766 May Be a Potential Therapy for RAS-Mutated Tumor Cells; PLoS One 9 e113217
- Ono et al. (2021), Novel RAF/MEK inhibitor CH5126766/VS-6766 has efficacy in combination with eribulin for the treatment of triple-negative breast cancer; Cancer Sci. 112 4166
- Yoshimura et al. (2024), Epithelial-mesenchymal transition status is a remarkable biomarker for the combination treatment with avutometinib and defactinib in KRAS-mutated non-small cell lung cancer; Br. J. Cancer 131 361
C21H18FN5O5S
>98% HPLC
NMR: (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
Avutometinib (946128-88-7) is a dual MEK/RAF inhibitor (IC50s: MEK = 160 nM; CRAF = 56 nM; BRAF = 19 nM; BRAF V600E = 8nM).1 It directly inhibits unphosphorylated MEK without causing induction of MEK phosphorylation by RAF. The avutemetinib-MEK adduct is a dominant-negative inhibitor of RAF, stabilizing the MEK/RAF complex and locking in an inactive form. Avutometinib displayed efficacy across multiple RAS-mutated cancer cell lines and an SK-MEL-2 xenograft model.2 It displayed synergistic effects with eribulin against triple-negative breast cancer cell lines.3 Avutometinib also displayed efficacy in combination with the FAK inhibitor Defactinib in KRAS-mutated NSCLC cells.4
References/Citations:
- Ishii et al. (2013), Enhanced inhibition of ERK signaling by a novel allosteric MEK inhibitor, CH5126766, that suppresses feedback reactivation of RAF activity; Cancer Res. 73 4050
- Wada et al. (2014The Dual RAF/MEK Inhibitor CH5126766/RO5126766 May Be a Potential Therapy for RAS-Mutated Tumor Cells; PLoS One 9 e113217
- Ono et al. (2021), Novel RAF/MEK inhibitor CH5126766/VS-6766 has efficacy in combination with eribulin for the treatment of triple-negative breast cancer; Cancer Sci. 112 4166
- Yoshimura et al. (2024), Epithelial-mesenchymal transition status is a remarkable biomarker for the combination treatment with avutometinib and defactinib in KRAS-mutated non-small cell lung cancer; Br. J. Cancer 131 361
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Focus Biomolecules • Plymouth Meeting, PA USA • 1-855-FOCUS21
Focus Biomolecules
Plymouth Meeting, PA USA
1-855-FOCUS21
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