Avutometinib potassium

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 208439

CAS#: 946128-90-1

Description: Avutometinib potassium is a MEK inhibitor (MEKi) that enhanced the inhibition of pseudovirus infection by GLPG-0187. It Blocks SARS-CoV-2 Delta and Omicron Pseudovirus Infection of Airway Epithelial Cells In Vitro, Which Could Attenuate Disease Severity

Chemical Structure

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Avutometinib potassium
CAS# 946128-90-1
Instruction

Theoretical Analysis

MedKoo Cat#: 208439
Name: Avutometinib potassium
CAS#: 946128-90-1
Chemical Formula: C21H17FKN5O5S
Exact Mass: 509.06
Molecular Weight: 509.550
Elemental Analysis: C, 49.50; H, 3.36; F, 3.73; K, 7.67; N, 13.74; O, 15.70; S, 6.29

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: Avutometinib-potassium, VS-6766 potassium; RO5126766 potassium

IUPAC/Chemical Name: Potassium [3-fluoro-4-[(4-methyl-2-oxo-7-pyrimidin-2-yloxychromen-3-yl)methyl]pyridin-2-yl]-(methylsulfamoyl)azanide

InChi Key: KYKJFDDJHVJFIF-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H17FN5O5S.K/c1-12-15-5-4-14(31-21-25-7-3-8-26-21)11-17(15)32-20(28)16(12)10-13-6-9-24-19(18(13)22)27-33(29,30)23-2;/h3-9,11,23H,10H2,1-2H3;/q-1;+1

SMILES Code: O=S([N-]C1=NC=CC(CC(C2=O)=C(C)C3=C(O2)C=C(OC4=NC=CC=N4)C=C3)=C1F)(NC)=O.[K+]

Appearance: To be determined

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 509.55 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Huntington KE, Carlsen L, So EY, Piesche M, Liang O, El-Deiry WS. Integrin/TGF-β1 Inhibitor GLPG-0187 Blocks SARS-CoV-2 Delta and Omicron Pseudovirus Infection of Airway Epithelial Cells In Vitro, Which Could Attenuate Disease Severity. Pharmaceuticals (Basel). 2022 May 17;15(5):618. doi: 10.3390/ph15050618. PMID: 35631444; PMCID: PMC9143518.


2: Capelletto E, Bironzo P, Denis L, Koustenis A, Bungaro M, Novello S. Single agent VS-6766 or VS-6766 plus defactinib in KRAS-mutant non-small-cell lung cancer: the RAMP-202 phase II trial. Future Oncol. 2022 May;18(16):1907-1915. doi: 10.2217/fon-2021-1582. Epub 2022 Mar 14. PMID: 35285277.


3: Huntington KE, Carlsen L, So EY, Piesche M, Liang O, El-Deiry WS. Integrin/TGF-β1 inhibitor GLPG-0187 blocks SARS-CoV-2 Delta and Omicron pseudovirus infection of airway epithelial cells which could attenuate disease severity. medRxiv [Preprint]. 2022 Jan 3:2022.01.02.22268641. doi: 10.1101/2022.01.02.22268641. Update in: Pharmaceuticals (Basel). 2022 May 17;15(5): PMID: 35018385; PMCID: PMC8750711.


4: Ono H, Horinaka M, Sukeno M, Morita M, Yasuda S, Nishimoto E, Konishi E, Sakai T. Novel RAF/MEK inhibitor CH5126766/VS-6766 has efficacy in combination with eribulin for the treatment of triple-negative breast cancer. Cancer Sci. 2021 Oct;112(10):4166-4175. doi: 10.1111/cas.15071. Epub 2021 Aug 1. PMID: 34288272; PMCID: PMC8486178.


5: Guo C, Banerji U. Searching for treatments for non-G12C-KRAS mutant cancers. Br J Cancer. 2021 Aug;125(5):625-626. doi: 10.1038/s41416-021-01357-2. Epub 2021 Apr 15. PMID: 33859342; PMCID: PMC8405631.


6: Zhou L, Huntington K, Zhang S, Carlsen L, So EY, Parker C, Sahin I, Safran H, Kamle S, Lee CM, Geun Lee C, A Elias J, S Campbell K, T Naik M, J Atwood W, Youssef E, A Pachter J, Navaraj A, A Seyhan A, Liang O, El-Deiry WS. MEK inhibitors reduce cellular expression of ACE2, pERK, pRb while stimulating NK- mediated cytotoxicity and attenuating inflammatory cytokines relevant to SARS- CoV-2 infection. Oncotarget. 2020 Nov 17;11(46):4201-4223. doi: 10.18632/oncotarget.27799. PMID: 33245731; PMCID: PMC7679035.


7: Dual RAF-MEK Inhibitor Assessed. Cancer Discov. 2021 Jan;11(1):5-6. doi: 10.1158/2159-8290.CD-NB2020-101. Epub 2020 Nov 13. PMID: 33188055.


8: Guo C, Chénard-Poirier M, Roda D, de Miguel M, Harris SJ, Candilejo IM, Sriskandarajah P, Xu W, Scaranti M, Constantinidou A, King J, Parmar M, Turner AJ, Carreira S, Riisnaes R, Finneran L, Hall E, Ishikawa Y, Nakai K, Tunariu N, Basu B, Kaiser M, Lopez JS, Minchom A, de Bono JS, Banerji U. Intermittent schedules of the oral RAF-MEK inhibitor CH5126766/VS-6766 in patients with RAS/RAF-mutant solid tumours and multiple myeloma: a single-centre, open-label, phase 1 dose-escalation and basket dose-expansion study. Lancet Oncol. 2020 Nov;21(11):1478-1488. doi: 10.1016/S1470-2045(20)30464-2. Epub 2020 Oct 28. Erratum in: Lancet Oncol. 2021 Feb;22(2):e42. PMID: 33128873.


9: Zhou L, Huntington K, Zhang S, Carlsen L, So EY, Parker C, Sahin I, Safran H, Kamle S, Lee CM, Lee CG, Elias JA, Campbell KS, Naik MT, Atwood WJ, Youssef E, Pachter JA, Navaraj A, Seyhan AA, Liang O, El-Deiry WS. Natural Killer cell activation, reduced ACE2, TMPRSS2, cytokines G-CSF, M-CSF and SARS-CoV-2-S pseudovirus infectivity by MEK inhibitor treatment of human cells. bioRxiv [Preprint]. 2020 Sep 2:2020.08.02.230839. doi: 10.1101/2020.08.02.230839. PMID: 32793908; PMCID: PMC7418728.