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MedKoo Cat#: 592963 | Name: Pexmetinib HCl

Description:

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

Pexmetinib (ARRY-614) is an orally bioavailable, dual inhibitor of p38 MAPK (mitogen-activated protein kinase) and Tie2 (tyrosine kinase with immunoglobulin-like and EGF-like domains 2), developed primarily for treating myelodysplastic syndromes (MDS). In preclinical studies, pexmetinib potently inhibits p38α with an IC₅₀ of ~11 nM and Tie2 with an IC₅₀ of ~14 nM, effectively blocking proinflammatory cytokine production and modulating hematopoietic signaling.

Chemical Structure

Pexmetinib HCl
Pexmetinib HCl
CAS#1416216-01-7 (HCl)

Theoretical Analysis

MedKoo Cat#: 592963

Name: Pexmetinib HCl

CAS#: 1416216-01-7 (HCl)

Chemical Formula: C31H34ClFN6O3

Exact Mass: 592.2365

Molecular Weight: 593.10

Elemental Analysis: C, 62.78; H, 5.78; Cl, 5.98; F, 3.20; N, 14.17; O, 8.09

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
945614-12-0 (free base) 1416216-01-7 (HCl)
Synonym
Pexmetinib hydrochloride; ARRY614; ARRY-614; ARRY 614; Pexmetinib;
IUPAC/Chemical Name
Urea, N-(3-(1,1-dimethylethyl)-1-(4-methylphenyl)-1H-pyrazol-5-yl)-N'-((5-fluoro-2-((1-(2-hydroxyethyl)-1H-indazol-5-yl)oxy)phenyl)methyl)-, hydrochloride (1:1)
InChi Key
JHEYROZAEFXENN-UHFFFAOYSA-N
InChi Code
InChI=1S/C31H33FN6O3.ClH/c1-20-5-8-24(9-6-20)38-29(17-28(36-38)31(2,3)4)35-30(40)33-18-22-15-23(32)7-12-27(22)41-25-10-11-26-21(16-25)19-34-37(26)13-14-39;/h5-12,15-17,19,39H,13-14,18H2,1-4H3,(H2,33,35,40);1H
SMILES Code
Urea, N-(3-(1,1-dimethylethyl)-1-(4-methylphenyl)-1H-pyrazol-5-yl)-N'-((5-fluoro-2-((1-(2-hydroxyethyl)-1H-indazol-5-yl)oxy)phenyl)methyl)-, hydrochloride (1:1)
Appearance
Solid powder
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
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.03.00
More Info
In a Phase I clinical trial in lower-risk MDS patients, pexmetinib showed hematologic improvements in ~32% of evaluable patients, with reductions in bone marrow blast counts and inflammatory cytokine levels (notably TNF-α and IL-6). The drug was generally well tolerated, with manageable adverse effects such as fatigue and gastrointestinal symptoms. Overall, pexmetinib demonstrates promising bioactivity by targeting both inflammatory and angiogenic signaling pathways implicated in MDS pathogenesis.

Preparing Stock Solutions

The following data is based on the product molecular weight 593.10 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
1: Fontana D, Malighetti F, Villa M, Zambon A, Gambacorti-Passerini C, Mologni L. Repurposing pexmetinib as an inhibitor of TKI-resistant BCR::ABL1. Leukemia. 2024 Aug;38(8):1843-1847. doi: 10.1038/s41375-024-02282-y. Epub 2024 May 15. PMID: 38750137; PMCID: PMC11286508. 2: Sun X, Wu Y, Xu F, Liu C. Screening of potent RIPK3 inhibitors to attenuate necroptosis and inflammation in mouse traumatic brain injury models. Exp Neurol. 2024 Feb;372:114633. doi: 10.1016/j.expneurol.2023.114633. Epub 2023 Dec 5. PMID: 38061556. 3: Luke JJ, Dadey RE, Augustin RC, Newman S, Singh KB, Doerfler R, Behr S, Lee P, Isett B, Deitrick C, Li A, Joy M, Reeder C, Smith K, Urban J, Sellitto L, Jelinek M, Christner SM, Beumer JH, Villaruz LC, Kulkarni A, Davar D, Poklepovic AS, Najjar Y, Zandberg DP, Soloff AC, Bruno TC, Vujanović L, Skinner HD, Ferris RL, Bao R. Tumor cell p38 inhibition to overcome immunotherapy resistance. Res Sq [Preprint]. 2023 Aug 19:rs.3.rs-3183496. doi: 10.21203/rs.3.rs-3183496/v1. PMID: 37645831; PMCID: PMC10462255. 4: Jie Z, Wang S, Ma Q, Shen Y, Zhao X, Yu H, Xie Z, Jiang C. Pexmetinib suppresses osteoclast formation and breast cancer induced osteolysis via P38/STAT3 signal pathway. J Bone Oncol. 2022 Jun 11;35:100439. doi: 10.1016/j.jbo.2022.100439. PMID: 35800294; PMCID: PMC9253705. 5: Su H, Jiang M, Senevirathne C, Aluri S, Zhang T, Guo H, Xavier-Ferrucio J, Jin S, Tran NT, Liu SM, Sun CW, Zhu Y, Zhao Q, Chen Y, Cable L, Shen Y, Liu J, Qu CK, Han X, Klug CA, Bhatia R, Chen Y, Nimer SD, Zheng YG, Iancu-Rubin C, Jin J, Deng H, Krause DS, Xiang J, Verma A, Luo M, Zhao X. Methylation of dual- specificity phosphatase 4 controls cell differentiation. Cell Rep. 2021 Jul 27;36(4):109421. doi: 10.1016/j.celrep.2021.109421. PMID: 34320342; PMCID: PMC9110119. 6: Hou H, Ning F, Zhang JY, Lu Q, Zhang M, Wu P, Chen M, Lash GE. Angiopoietin 2 stimulates trophoblast invasion via a mechanism associated with JNK signaling. Mol Hum Reprod. 2021 Feb 27;27(3):gaab014. doi: 10.1093/molehr/gaab014. PMID: 33629098. 7: Bachegowda L, Morrone K, Winski SL, Mantzaris I, Bartenstein M, Ramachandra N, Giricz O, Sukrithan V, Nwankwo G, Shahnaz S, Bhagat T, Bhattacharyya S, Assal A, Shastri A, Gordon-Mitchell S, Pellagatti A, Boultwood J, Schinke C, Yu Y, Guha C, Rizzi J, Garrus J, Brown S, Wollenberg L, Hogeland G, Wright D, Munson M, Rodriguez M, Gross S, Chantry D, Zou Y, Platanias L, Burgess LE, Pradhan K, Steidl U, Verma A. Pexmetinib: A Novel Dual Inhibitor of Tie2 and p38 MAPK with Efficacy in Preclinical Models of Myelodysplastic Syndromes and Acute Myeloid Leukemia. Cancer Res. 2016 Aug 15;76(16):4841-4849. doi: 10.1158/0008-5472.CAN-15-3062. Epub 2016 Jun 10. PMID: 27287719; PMCID: PMC5398415. 8: Wollenberg LA, Corson DT, Nugent CA, Peterson FL, Ptaszynski AM, Arrigo A, Mannila CG, Litwiler KS, Bell SJ. An exploratory, randomized, parallel-group, open-label, relative bioavailability study with an additional two-period crossover food-effect study exploring the pharmacokinetics of two novel formulations of pexmetinib (ARRY-614). Clin Pharmacol. 2015 Sep 30;7:87-95. doi: 10.2147/CPAA.S83871. PMID: 26491375; PMCID: PMC4598228. 9: Gañán-Gómez I, Bohannan ZS, Garcia-Manero G. p38 MAPK in MDS. Aging (Albany NY). 2015 Jun;7(6):346-7. doi: 10.18632/aging.100757. PMID: 26081220; PMCID: PMC4505155. 10: Garcia-Manero G, Khoury HJ, Jabbour E, Lancet J, Winski SL, Cable L, Rush S, Maloney L, Hogeland G, Ptaszynski M, Calvo MC, Bohannan Z, List A, Kantarjian H, Komrokji R. A phase I study of oral ARRY-614, a p38 MAPK/Tie2 dual inhibitor, in patients with low or intermediate-1 risk myelodysplastic syndromes. Clin Cancer Res. 2015 Mar 1;21(5):985-94. doi: 10.1158/1078-0432.CCR-14-1765. Epub 2014 Dec 5. PMID: 25480830; PMCID: PMC4348327. 11: Bachegowda L, Gligich O, Mantzaris I, Schinke C, Wyville D, Carrillo T, Braunschweig I, Steidl U, Verma A. Signal transduction inhibitors in treatment of myelodysplastic syndromes. J Hematol Oncol. 2013 Jul 10;6:50. doi: 10.1186/1756-8722-6-50. PMID: 23841999; PMCID: PMC3716523.

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