Pexidartinib (hydrochloride)

Pexidartinib (hydrochloride)

• CAS Number: 2040295-03-0
• UNSPSC Description: Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib hydrochloride exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib hydrochloride induces cell apoptosis and has anti-cancer activity[1].
• Target Antigen: Apoptosis; c-Fms; c-Kit
• Type: Reference compound
• Related Pathways: Apoptosis;Protein Tyrosine Kinase/RTK
• Applications: Cancer-Kinase/protease
• Field of Research: Cancer
• Assay Protocol: https://www.medchemexpress.com/pexidartinib-hydrochloride.html
• Solubility: DMSO : 60 mg/mL (ultrasonic)|H2O : < 0.1 mg/mL (ultrasonic)
• Smiles: FC(C1=CC=C(CNC2=NC=C(CC3=CNC4=NC=C(Cl)C=C43)C=C2)C=N1)(F)F.Cl
• Molecular Weight: 454.28
• References & Citations: [1]DeNardo DG, et al. Leukocyte complexity predicts breast cancer survival and functionally regulates response to chemotherapy. Cancer Discov. 2011 Jun;1(1):54-67.|[2]Kuse Y, et al. Microglia increases the proliferation of retinal precursor cells during postnatal development. Mol Vis. 2018 Jul 30;24:536-545. eCollection 2018.|[3]Lee JH, et al. A phase I study of pexidartinib, a colony-stimulating factor 1 receptor inhibitor, in Asian patients with advanced solid tumors. Invest New Drugs. 2019 Mar 2.|[4]Merry TL, et al. The CSF1 receptor inhibitor pexidartinib (PLX3397) reduces tissue macrophage levels without affecting glucose homeostasis in mice. Int J Obes (Lond). 2020;44(1):245-253.|[5]Luo L, et al. Intermittent theta-burst stimulation improves motor function by inhibiting neuronal pyroptosis and regulating microglial polarization via TLR4/NFκB/NLRP3 signaling pathway in cerebral ischemic mice. J Neuroinflammation. 2022 Jun 11;19(1):141.|[6]Chadarevian JP, et al. Engineering an inhibitor-resistant human CSF1R variant for microglia replacement. J Exp Med. 2023 Mar 6;220(3):e20220857.Biomolecules. 2022 May 4;12(5):666.|Universität zu Köln. 2023 Sep 26.|ACS Nano. 2024 Jan 22.|Am J Physiol Cell Physiol. 2020 Sep 1;319(3):C605-C610.|Anti-Cancer Drug. 2022 Dec.|Behav Pharmacol. 2023 Sep 1;34(6):318-329.|Biochem Pharmacol. 2022 Feb 9;198:114952.|Biomedicines. 2021, 9(10), 1387.|Biomedicines. 2022, 10(7), 1653.|bioRxiv. 2023 Jul 25.|bioRxiv. 2023 Nov 14.|bioRxiv. 2023 Nov 17.|bioRxiv. 2023 Oct 12.|bioRxiv. 2024 Apr 14.|bioRxiv. 2024 Apr 16.|biorxiv. 2024 Jun 06.|bioRxiv. 2024 October 02.|bioRxiv. 2024 September 21.|BMC Med. 2023 Aug 4;21(1):286.|Brain Behav Immun. 2022 Oct 3;S0889-1591(22)00398-1.|Cancer Cell. 2021 Sep 1;S1535-6108(21)00445-1.|Cancer Cell. 2023 Nov 13;41(11):1911-1926.e8.|Cancer Lett. 2022 Jun 16;215795.|Cell Oncol. 2021 Feb;44(1):193-204.|Cell Rep. 2023 Sep 22;42(10):113128.|Cell Rep. 2024 Oct 23;43(11):114894.|Cell Stem Cell. 2024 Oct 30:S1934-5909(24)00367-9.|Cells. 2021, 10(4), 874.|Cells. 2021, 10(8), 1862|Chem Biol Interact. 2022: 110255.|Circ Res. 2021 Sep 17;129(7):e121-e140.|CNS Neurosci Ther. 2023 Mar 16.|Diabetes. 2023 Sep 8;db230173.|Endocrinology. 2024 Jan 16:bqae003.|eNeuro. 2023 Oct 27:ENEURO.0323-23.2023.|Eur J Immunol. 2024 Sep 23:e2451139.|Front Immunol. 2022 May 13;13:866073.|Glia. 2021 Apr;69(4):943-953.|Glia. 2021 Feb 15.|Glia. 2022 Jun 30.|Inflamm Regen. 2024 Jun 6;44(1):30.|Int Immunopharmacol. 2023 May.|Int J Mol Sci. 2024 Jun 26;25(13):7001.|J Am Heart Assoc. 2023 Jun 15;e029053.|J Anat. 2023 Apr 11.|J Exp Med. 2023 Mar 6;220(3):e20220857.|J Neuroinflammation. 2020 Jan 23;17(1):31.|J Neuroinflammation. 2022 Jan 21;19(1):20.|J Neuroinflammation. 2023 Feb 25;20(1):51.|J Neuroinflammation. 2024 Nov 14;21(1):295.|J Neuroinflammation. 2024 Oct 21;21(1):270.|J Neuroinflammation. 2024 Sep 01.|J Neurooncol. 2021 May 8.|J Neurosci Res. 2021 Feb 20.|J Neurosci. 2020 May 6;40(19):3862-3879.|J Ocul Pharmacol Ther. 2020 Jun;36(5):311-319.|Karolinska Institutet. Dept of Clinical Neuroscience. 2021 Feb.|Life Sci Alliance. 2023 Aug 7;6(11):e202302020.|Life Sci. 2020 Oct 1;258:118099.|Methods Mol Biol. 2018;1711:351-398.|Mol Pharmacol. April 5, 2022.|Molecules. 2022, 27(1), 297.|Nat Biomed Eng. 2018 Aug;2(8):578-588.|Nat Commun. 2024 Jul 5;15(1):5654.|Nat Commun. 2024 Oct 13;15(1):8837.|Nat Immunol. 2023 May;24(5):827-840.|Nat Metab. 2024 Jul 24.|Nature Cardiovascular Research. 2023 Jun 8.|Nature. 2022 Mar;603(7899):138-144.|Nature. 2024 Apr;628(8006):145-153.|Neural Regen Res. 2023.|Neuron. 2021 Aug 18;109(16):2573-2589.e9.|Neuropharmacology. 2019 Apr 4;151:33-44.|Neuropharmacology. 2020 Aug 1;172:108132.|Patent. US20230203500A1.|Pharmacol Res. 2023 Apr 15;106773.|Prog Neuropsychopharmacol Biol Psychiatry. 2020 Jul 13;101:109931.|Res Sq. 2024 Nov 19.|Res Sq. 2024 Sep 03.|Research Square Preprint. 2021 Sep.|Research Square Preprint. 2022 Jul.|Research Square Preprint. 2023 Sep 12.|Research Square Preprint. 2024 Feb 15.|Research Square Print. 2022 Jun.|Sci Rep. 2021 Aug 6;11(1):15989.|Sci Rep. 2024 Aug 4;14(1):18031.|SSRN. 2023 Jun 29.|STAR Protoc. 2023 Jul 29;4(3):102490.|The Ohio State University. 2023 Oct.|Theranostics. 2020 Jan 1;10(1):74-90.|Transl Psychiatry. 2020 Jan 27;10(1):32.|Transl Psychiatry. 2024 Aug 23;14(1):338.|Transl Stroke Res. 2024 Aug 5.|Universität zu Köln. 2023 Sep 26.|University of Washington. 2024.
• Shipping Conditions: Room Temperature
• Clinical Information: Launched