Imatinib

Imatinib

• CAS Number: 152459-95-5
• UNSPSC Description: Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively[1][2][3][4]. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV[5].
• Target Antigen: Autophagy; Bcr-Abl; c-Kit; PDGFR; SARS-CoV
• Type: Reference compound
• Related Pathways: Anti-infection;Autophagy;Protein Tyrosine Kinase/RTK
• Applications: Cancer-Kinase/protease
• Field of Research: Cancer
• Assay Protocol: https://www.medchemexpress.com/Imatinib.html
• Solubility: DMSO : 12.5 mg/mL (ultrasonic)|H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C)
• Smiles: CN(CC1)CCN1CC2=CC=C(C(NC3=CC=C(C)C(NC4=NC(C5=CC=CN=C5)=CC=N4)=C3)=O)C=C2
• Molecular Weight: 493.60
• References & Citations: [1]Heinrich MC, et al. Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor. Blood. 2000 Aug 1;96(3):925-32.|[2]Guida T, et al. Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants. Clin Cancer Res. 2007 Jun 1;13(11):3363-9.|[3]Iqbal N, et al. Imatinib: a breakthrough of targeted therapy in cancer. Chemother Res Pract. 2014;2014:357027.|[4]Okuda K, et al. ARG tyrosine kinase activity is inhibited by STI571.Blood. 2001 Apr 15;97(8):2440-8|[5]Yao JC, et al. Clinical and in vitro studies of imatinib in advanced carcinoid tumors. Clin Cancer Res. 2007 Jan 1;13(1):234-40.|[6]Sun XC, et al. Depletion of telomerase RNA inhibits growth of gastrointestinal tumors transplanted in mice. World J Gastroenterol. 2013 Apr 21;19(15):2340-7.|[7]Yildiz C, et al. Effect of imatinib on growth of experimental endometriosis in rats. Eur J Obstet Gynecol Reprod Biol. 2016 Feb;197:159-63.|[8]Jeanne M Sisk, et al. Coronavirus S Protein-Induced Fusion Is Blocked Prior to Hemifusion by Abl Kinase Inhibitors. J Gen Virol. 2018 May;99(5):619-630.|[9]Coleman CM, et al, Frieman MB. Abelson Kinase Inhibitors Are Potent Inhibitors of Severe Acute Respiratory Syndrome Coronavirus and Middle East Respiratory Syndrome Coronavirus Fusion. J Virol. 2016;90(19):8924‐8933. Published 2016 Sep 12.Acta Pharmacol Sin. 2022 Nov 30.|Arch Pharm (Weinheim). 2022 Oct 10;e2200367.|Bioanalysis. 2018 Jul;10(14):1099-1113.|Biochem Pharmacol. 2023 Jan 30.|Biomed Pharmacother. 2023 Dec 22:170:115778.|Biomolecules. 2022 Jun 11;12(6):819.|bioRxiv. 2024 June 09.|Cancer Biol Ther. 2019;20(6):877-885.|Cancer Lett. 2019 Apr 10;447:105-114.|Cancer Med. 2019 Sep;8(11):5352-5366.|Cancer Res. 2024 Oct 22.|Cell Biosci. 2020 Feb 12;10:16.|Cell Biosci. 2024 Jun 29;14(1):87.|Cell Chem Biol. 2018 Aug 16;25(8):996-1005.e4.|Cell Death Dis. 2022 Apr 20;13(4):384.|Cell Metab. 2022 Feb 7;34(3):424-440.e7.|Cell Rep Methods. 2023 Oct 23;3(10):100599.|Clin Cancer Res. 2020 Aug 15;26(16):4349-4359.|Clin Chem. 2019 Dec;65(12):1522-1531. |Clin Sci. 2021 Jul 20;CS20210571.|Commun Biol. 2024 Jul 10;7(1):843.|Curr Res Toxicol. 2024 Jul 14:7:100187.|Drug Des Devel Ther. 2022 Aug 4;16:2545-2557.|EMBO Mol Med. 2021 Mar 4;e13144.|Eur J Pharmacol. 2021 Feb 10;173944.|Eur J Pharmacol. 2021 Jun 1;174217.|Eur J Pharmacol. 2021 Nov 26;174633.|Gastric Cancer. 2023 May 24.|Heliyon. 2024 Aug 22;10(16):e36640.|In Vivo. 2024 Sep-Oct;38(5):2310-2317.|Inflamm Regen. 2022 Sep 26;42(1):44.|Int J Mol Sci. 2023 Feb 2;24(3):2849.|J Biomed Inform. 2023 May 15;104383.|J Cell Biochem. 2023 Aug 11.|J Chromatogr B Analyt Technol Biomed Life Sci. 2024 Mar 26:1237:124100.|J Med Chem. 2016 Sep 22;59(18):8456-72. |J Med Chem. 2019 Jul 11;62(13):6083-6101.|J Med Chem. 2019 May 23;62(10):5006-5024. |J Med Chem. 2021 Mar 11;64(5):2725-2738.|J Tradit Complement Med. 2023 Nov 22.|Med Sci Monit. 2017 Aug 6;23:3808-3816.|Mol Carcinog. 2023 Sep 22.|Mol Carcinog. 2024 Apr 17|Mol Ther. 2022 Nov 15;S1525-0016(22)00662-1.|Nat Biomed Eng. 2018 Aug;2(8):578-588.|Nucleic Acids Res. 2021 Jan 8;49(D1):D1113-D1121.|Oncogene. 2022 Feb 9.|Oncogene. 2024 May 17.|Oncotarget. 2016 Jul 19;7(29):45562-45574.|Oncotarget. 2017 Nov 15;8(67):111110-111118. |Patent. US20200276189A1.|Patent. US20220064117A1.|Patent. US20220288064A1.|Patent. US20230158019A1.|Patent. US20230226111A1.|Patent. US20240238271A1.|Patent. US20240325538A1.|Research Square Preprint. 2021 May.|Sci Immunol. 2023 Mar 17;8(81):eade4656.|Sci Signal. 2019 Jul 16;12(590). pii: eaav7259.|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.|Sensor Actuat B-Chem. 2021, 128991.|Signal Transduct Target Ther. 2023 Mar 1;8(1):90.|Stem Cell Reports. 2017 Dec 12;9(6):1948-1960.|Ther Adv Med Oncol. 2019 May 17;11:1758835919849757. |Theranostics. 2021 Jan 1;11(6):2691-2705.|Toxicol Lett. 2022 Jun 6;S0378-4274(22)00117-5.|Toxicol Lett. 2022 May 18;363:11-26.|Viruses. 2021 May 31;13(6):1035.|Adv Sci (Weinh). 2024 Jul 2:e2402107.|Anticancer Drugs. 2014 Jul;25(6):673-82.|Biomed Chromatogr. 2019 Dec;33(12):e4674.|BMC Med. 2022 Aug 24;20(1):257|Bone Res. 2024 Apr 10;12(1):24.|Harvard Medical School LINCS LIBRARY|J Bioenerg Biomembr. 2012 Feb;44(1):155-61.|J Pers Med. 2023, 13(1), 146.|Mol Cell Biochem. 2020 Jan;463(1-2):67-78|Nat Immunol. 2023 Sep;24(9):1443-1457.|Oncotarget. 2018 Apr 24;9(31):22158-22183. |Patent. US20220242943A1.|Pharmaceutics. 2023 Sep 12, 15(9), 2305.|Phytomedicine. 2024 Nov:134:155937.|PLoS Negl Trop Dis. 2019 Aug 20;13(8):e0007681. |PLoS One. 2017 Jun 1;12(6):e0178619.|Research Square Preprint. 2023 Nov 20.
• Shipping Conditions: Room Temperature
• Clinical Information: Launched