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MedKoo Cat#: 577162 | Name: Merestinib HCl
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Description:

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

Merestinib is a potent, orally bioavailable, multi-kinase inhibitor primarily targeting MET (c-Met), with reported IC₅₀ values in the low nanomolar range (e.g., ~2–3 nM for MET). It also inhibits a range of receptor tyrosine kinases including AXL, RON, ROS1, NTRK1/2/3, FLT3, and DDR1/2. In preclinical studies, Merestinib demonstrated strong anti-proliferative effects in MET-amplified and MET-mutant cancer cell lines, with dose-dependent inhibition of MET phosphorylation and downstream signaling pathways (e.g., ERK and AKT). In xenograft models, Merestinib suppressed tumor growth in MET-driven tumors. It has also shown activity against NTRK fusion-positive cancers, leading to tumor regression in relevant models

Chemical Structure

Merestinib HCl
Merestinib HCl
CAS#1206801-37-7 (HCl)

Theoretical Analysis

MedKoo Cat#: 577162

Name: Merestinib HCl

CAS#: 1206801-37-7 (HCl)

Chemical Formula: C30H24Cl2F2N6O3

Exact Mass: 624.1255

Molecular Weight: 625.46

Elemental Analysis: C, 57.61; H, 3.87; Cl, 11.34; F, 6.08; N, 13.44; O, 7.67

Price and Availability

Size Price Availability Quantity
10mg USD 385.00 2 Weeks
50mg USD 950.00 2 Weeks
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Related CAS #
1206799-15-6 (free base) 1206801-37-7 (HCl)
Synonym
Merestinib dihydrochloride; Merestinib 2HCl
IUPAC/Chemical Name
3-Pyridinecarboxamide, N-(3-fluoro-4-((1-methyl-6-(1H-pyrazol-4-yl)-1H-indazol-5-yl)oxy)phenyl)-1-(4-fluorophenyl)-1,2-dihydro-6-methyl-2-oxo-, hydrochloride (1:2)
InChi Key
NNYNNMGUBHQQLZ-UHFFFAOYSA-N
InChi Code
InChI=1S/C30H22F2N6O3.2ClH/c1-17-3-9-23(30(40)38(17)22-7-4-20(31)5-8-22)29(39)36-21-6-10-27(25(32)12-21)41-28-11-18-16-35-37(2)26(18)13-24(28)19-14-33-34-15-19;;/h3-16H,1-2H3,(H,33,34)(H,36,39);2*1H
SMILES Code
Cl.Cl.CC1=CC=C(C(=O)Nc2ccc(Oc3cc4cnn(C)c4cc3c5cn[nH]c5)c(F)c2)C(=O)N1c6ccc(F)cc6
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
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

Preparing Stock Solutions

The following data is based on the product molecular weight 625.46 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: Luo X, Linghu M, Zhou X, Ru Y, Huang Q, Liu D, Ji S, Ma Y, Luo Y, Huang Y. Merestinib inhibits cuproptosis by targeting NRF2 to alleviate acute liver injury. Free Radic Biol Med. 2025 Mar 1;229:68-81. doi: 10.1016/j.freeradbiomed.2025.01.029. Epub 2025 Jan 15. PMID: 39824447. 2: Thawani R, Repetto M, Keddy C, Nicholson K, Jones K, Nusser K, Beach CZ, Harada G, Drilon A, Davare MA. TKI type switching overcomes ROS1 L2086F in ROS1 fusion-positive cancers. NPJ Precis Oncol. 2024 Aug 8;8(1):175. doi: 10.1038/s41698-024-00663-1. Erratum in: NPJ Precis Oncol. 2024 Aug 28;8(1):184. doi: 10.1038/s41698-024-00676-w. PMID: 39117775; PMCID: PMC11310217. 3: Devi GR, Pai P, Lee S, Foster MW, Sannareddy DS, Bertucci F, Ueno N, Van Laere S. Altered ribosomal profile in acquired resistance and reversal associates with pathological response to chemotherapy in inflammatory breast cancer. NPJ Breast Cancer. 2024 Jul 29;10(1):65. doi: 10.1038/s41523-024-00664-0. PMID: 39075068; PMCID: PMC11286775. 4: Thawani R, Repetto M, Keddy C, Nicholson K, Jones K, Nusser K, Beach CZ, Harada G, Drilon A, Davare MA. TKI Type Switching Overcomes ROS1 L2086F in ROS1 Fusion-Positive Cancers. bioRxiv [Preprint]. 2024 Jan 19:2024.01.16.575901. doi: 10.1101/2024.01.16.575901. Update in: NPJ Precis Oncol. 2024 Aug 8;8(1):175. doi: 10.1038/s41698-024-00663-1. PMID: 38293020; PMCID: PMC10827145. 5: Wang ML, Jurczak W, Zinzani PL, Eyre TA, Cheah CY, Ujjani CS, Koh Y, Izutsu K, Gerson JN, Flinn I, Tessoulin B, Alencar AJ, Ma S, Lewis D, Lech-Maranda E, Rhodes J, Patel K, Maddocks K, Lamanna N, Wang Y, Tam CS, Munir T, Nagai H, Hernandez-Ilizaliturri F, Kumar A, Fenske TS, Seymour JF, Zelenetz AD, Nair B, Tsai DE, Balbas M, Walgren RA, Abada P, Wang C, Zhao J, Mato AR, Shah NN. Pirtobrutinib in Covalent Bruton Tyrosine Kinase Inhibitor Pretreated Mantle- Cell Lymphoma. J Clin Oncol. 2023 Aug 20;41(24):3988-3997. doi: 10.1200/JCO.23.00562. Epub 2023 May 16. PMID: 37192437; PMCID: PMC10461952. 6: Chen EC, Gandler H, Tošić I, Fell GG, Fiore A, Pozdnyakova O, DeAngelo DJ, Galinsky I, Luskin MR, Wadleigh M, Winer ES, Leonard R, O'Day K, de Jonge A, Neuberg D, Look AT, Stone RM, Frank DA, Garcia JS. Targeting MET and FGFR in Relapsed or Refractory Acute Myeloid Leukemia: Preclinical and Clinical Findings, and Signal Transduction Correlates. Clin Cancer Res. 2023 Mar 1;29(5):878-887. doi: 10.1158/1078-0432.CCR-22-2540. PMID: 36534523; PMCID: PMC9992000. 7: Feng L, Wang Y, Xu H, Yi F. Comparison of Different First-Line Systemic Therapies in Advanced Biliary Tract Cancer Based on Updated Random Controlled Trials: A Systematic Review and Network Meta-Analysis. Biomed Res Int. 2022 Sep 9;2022:1720696. doi: 10.1155/2022/1720696. PMID: 36119936; PMCID: PMC9481325. 8: Fujino T, Suda K, Koga T, Hamada A, Ohara S, Chiba M, Shimoji M, Takemoto T, Soh J, Mitsudomi T. Foretinib can overcome common on-target resistance mutations after capmatinib/tepotinib treatment in NSCLCs with MET exon 14 skipping mutation. J Hematol Oncol. 2022 Jun 11;15(1):79. doi: 10.1186/s13045-022-01299-z. PMID: 35690785; PMCID: PMC9188708. 9: Bahcall M, Paweletz CP, Kuang Y, Taus LJ, Sim T, Kim ND, Dholakia KH, Lau CJ, Gokhale PC, Chopade PR, Hong F, Wei Z, Köhler J, Kirschmeier PT, Guo J, Guo S, Wang S, Jänne PA. Combination of Type I and Type II MET Tyrosine Kinase Inhibitors as Therapeutic Approach to Prevent Resistance. Mol Cancer Ther. 2022 Feb;21(2):322-335. doi: 10.1158/1535-7163.MCT-21-0344. Epub 2021 Nov 17. PMID: 34789563; PMCID: PMC8828669. 10: Valle JW, Vogel A, Denlinger CS, He AR, Bai LY, Orlova R, Van Cutsem E, Adeva J, Chen LT, Obermannova R, Ettrich TJ, Chen JS, Wasan H, Girvan AC, Zhang W, Liu J, Tang C, Ebert PJ, Aggarwal A, McNeely SC, Moser BA, Oliveira JM, Carlesi R, Walgren RA, Oh DY. Addition of ramucirumab or merestinib to standard first-line chemotherapy for locally advanced or metastatic biliary tract cancer: a randomised, double-blind, multicentre, phase 2 study. Lancet Oncol. 2021 Oct;22(10):1468-1482. doi: 10.1016/S1470-2045(21)00409-5. Erratum in: Lancet Oncol. 2021 Nov;22(11):e472. doi: 10.1016/S1470-2045(21)00586-6. PMID: 34592180. 11: Doi T, Yamamoto N, Naito Y, Kuboki Y, Koyama T, Piao Y, Tsujimoto N, Asou H, Inoue K, Kondo S. Merestinib monotherapy or in combination for japanese patients with advanced and/or metastatic cancer: A phase 1 study. Cancer Med. 2021 Oct;10(19):6579-6589. doi: 10.1002/cam4.4110. Epub 2021 Sep 9. PMID: 34499416; PMCID: PMC8495281. 12: Zhang S, Stroud PA, Zhu A, Johnson MJ, Lomeo J, Burcham CL, Hinds J, Allen- Francis Blakely K, Walworth MJ. Characterizing the Impact of Spray Dried Particle Morphology on Tablet Dissolution Using Quantitative X-Ray Microscopy. Eur J Pharm Sci. 2021 Oct 1;165:105921. doi: 10.1016/j.ejps.2021.105921. Epub 2021 Jul 3. PMID: 34229077. 13: Patnaik A, Yap TA, Chung HC, de Miguel MJ, Bang YJ, Lin CC, Su WC, Italiano A, Chow KH, Szpurka AM, Yu D, Zhao Y, Carlsen M, Schmidt S, Vangerow B, Gandhi L, Xu X, Bendell J. Safety and Clinical Activity of a New Anti-PD-L1 Antibody as Monotherapy or Combined with Targeted Therapy in Advanced Solid Tumors: The PACT Phase Ia/Ib Trial. Clin Cancer Res. 2021 Mar 1;27(5):1267-1277. doi: 10.1158/1078-0432.CCR-20-2821. Epub 2020 Nov 23. PMID: 33229456. 14: Saleh M, Cassier PA, Eberst L, Naik G, Morris VK, Pant S, Terret C, Gao L, Long A, Mao H, McNeely S, Wagner EK, Carlesi RM, Fu S. Phase I Study of Ramucirumab Plus Merestinib in Previously Treated Metastatic Colorectal Cancer: Safety, Preliminary Efficacy, and Pharmacokinetic Findings. Oncologist. 2020 Nov;25(11):e1628-e1639. doi: 10.1634/theoncologist.2020-0520. Epub 2020 Jul 17. PMID: 32537847; PMCID: PMC7648328. 15: Huang C, Zou Q, Liu H, Qiu B, Li Q, Lin Y, Liang Y. Management of Non-small Cell Lung Cancer Patients with MET Exon 14 Skipping Mutations. Curr Treat Options Oncol. 2020 Apr 18;21(4):33. doi: 10.1007/s11864-020-0723-5. PMID: 32306194. 16: Chu P, Batson S, Hodgson M, Mitchell CR, Steenrod A. Systematic review of neurotrophic tropomyosin-related kinase inhibition as a tumor-agnostic management strategy. Future Oncol. 2020 Feb;16(4):61-74. doi: 10.2217/fon-2019-0534. Epub 2020 Jan 16. PMID: 31942815. 17: He AR, Cohen RB, Denlinger CS, Sama A, Birnbaum A, Hwang J, Sato T, Lewis N, Mynderse M, Niland M, Giles J, Wallin J, Moser B, Zhang W, Walgren R, Plimack ER. First-in-Human Phase I Study of Merestinib, an Oral Multikinase Inhibitor, in Patients with Advanced Cancer. Oncologist. 2019 Sep;24(9):e930-e942. doi: 10.1634/theoncologist.2018-0411. Epub 2019 Mar 4. PMID: 30833489; PMCID: PMC6738318. 18: Ghanaatgar-Kasbi S, Khorrami S, Avan A, Aledavoud SA, Ferns GA. Targeting the C-MET/HGF Signaling Pathway in Pancreatic Ductal Adenocarcinoma. Curr Pharm Des. 2018;24(39):4619-4625. doi: 10.2174/1381612825666190110145855. PMID: 30636579. 19: Konicek BW, Capen AR, Credille KM, Ebert PJ, Falcon BL, Heady GL, Patel BKR, Peek VL, Stephens JR, Stewart JA, Stout SL, Timm DE, Um SL, Willard MD, Wulur IH, Zeng Y, Wang Y, Walgren RA, Betty Yan SC. Merestinib (LY2801653) inhibits neurotrophic receptor kinase (NTRK) and suppresses growth of NTRK fusion bearing tumors. Oncotarget. 2018 Feb 13;9(17):13796-13806. doi: 10.18632/oncotarget.24488. PMID: 29568395; PMCID: PMC5862616. 20: Yan SB, Um SL, Peek VL, Stephens JR, Zeng W, Konicek BW, Liu L, Manro JR, Wacheck V, Walgren RA. MET-targeting antibody (emibetuzumab) and kinase inhibitor (merestinib) as single agent or in combination in a cancer model bearing MET exon 14 skipping. Invest New Drugs. 2018 Aug;36(4):536-544. doi: 10.1007/s10637-017-0545-x. Epub 2017 Nov 29. PMID: 29188469; PMCID: PMC6061111.

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