AZD3965
Based on 87 publication(s) in Google Scholar
AZD3965 is a selective MCT1 inhibitor with a Ki of 1.6 nM, showing 6-fold selectivity over MCT2.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.96%
- CAS 番号: 1448671-31-5
- 分子式: C21H24F3N5O5S
- 分子量:515.51
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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MedChemExpress（MCE）の使用を引用している文献 AZD3965
More- Nature. 2024 Oct;634(8036):1229-1237. [Abstract]
- Nature. 2023 Aug;620(7975):881-889. [Abstract]
- Cell. 2021 Jan 21;184(2):370-383.e13. [Abstract]
- Cell. 2019 Jul 11;178(2):330-345.e22. [Abstract]
- Cell Metab. 2026 Mar 24:S1550-4131(26)00093-8. [Abstract]
- Cell Metab. 2025 Oct 24:S1550-4131(25)00435-8. [Abstract]
- Cell Metab. 2025 Apr 1;37(4):903-919.e10. [Abstract]
- Cell Metab. 2021 Oct 5;33(10):2040-2058.e10. [Abstract]
- Nat Metab. 2021 Nov;3(11):1484-1499. [Abstract]
- Cell Stem Cell. 2022 Apr 7;29(4):545-558.e13. [Abstract]
- Bioact Mater. 2025 Nov 29:58:1-18. [Abstract]
- Cell Host Microbe. 2026 Feb 11;34(2):245-262.e8. [Abstract]
- ACS Nano. 2024 Jul 21. [Abstract]
- Nat Protoc. 2024 May;19(5):1311-1347. [Abstract]
- Nat Commun. 2025 Dec 19. [Abstract]
- Nat Commun. 2025 Oct 10;16(1):9034. [Abstract]
- Nat Commun. 2025 Sep 30;16(1):8639. [Abstract]
- Nat Commun. 2024 Jan 12;15(1):499. [Abstract]
- Adv Sci (Weinh). 2024 Dec 4:e2411276. [Abstract]
- J Exp Clin Cancer Res. 2026 Jun 23;45:143.
- J Exp Clin Cancer Res. 2021 Aug 27;40(1):273. [Abstract]
- Microbiome. 2023 Jan 31;11(1):17. [Abstract]
- Metabolism. 2020 Jan;102:154011. [Abstract]
- J Immunother Cancer. 2023 Jun;11(6):e006287. [Abstract]
- Pharmacol Res. 2026 Feb:224:108110. [Abstract]
- Cell Death Dis. 2025 Apr 5;16(1):253. [Abstract]
- Genome Biol. 2025 Oct 30;26(1):377. [Abstract]
- Cell Commun Signal. 2025 Oct 14;23(1):438. [Abstract]
- Phytomedicine. 2025 Sep:145:157009. [Abstract]
- ACS Appl Mater Interfaces. 2021 Jun 9;13(22):25727-25737. [Abstract]
- Biomed Pharmacother. 2023 Jul:163:114717. [Abstract]
- Int Endod J. 2026 Mar 8. [Abstract]
- Arch Toxicol. 2022 Nov;96(11):2913-2926. [Abstract]
- Arch Toxicol. 2022 Jul;96(7):2113-2122. [Abstract]
- Cell Rep. 2020 Dec 8;33(10):108487. [Abstract]
- J Agric Food Chem. 2021 Nov 3;69(43):12862-12869. [Abstract]
- Front Immunol. 2021 Nov 24;12:777665. [Abstract]
- ACS Biomater Sci Eng. 2026 Feb 9;12(2):1018-1031. [Abstract]
- Inflamm Res. 2026 Jun 11;75(1):137. [Abstract]
- Cells. 2024 Jan 23;13(3):206. [Abstract]
- Crit Rev Anal Chem. 2022;52(7):1557-1571. [Abstract]
- NPJ Genom Med. 2022 Oct 27;7(1):63. [Abstract]
- Am J Physiol Cell Physiol. 2026 Jun 1;330(6):C1561-C1573. [Abstract]
- Biosci Rep. 2024 Jul 11:BSR20240752. [Abstract]
- Brain Commun. 2024 Jun 3;6(3):fcae182. [Abstract]
- Cancers. 2020 Jan 10;12(1):181. [Abstract]
- J Physiol Biochem. 2023 Feb;79(1):147-161. [Abstract]
- Poult Sci. 2024 Jun;103(6):103717. [Abstract]
- Fish Shellfish Immunol. 2022 Oct:129:22-29. [Abstract]
- Fish Shellfish Immunol. 2022 Dec:131:264-273. [Abstract]
- Neurophotonics. 2025 Jun;12(Suppl 2):S22807. [Abstract]
- ACS Chem Biol. 2018 Jun 15;13(6):1480-1486. [Abstract]
- Cell Signal. 2025 May 17:111877. [Abstract]
- AAPS J. 2019 Jan 7;21(2):13. [Abstract]
- Am J Pathol. 2024 Oct;194(10):1857-1878. [Abstract]
- Exp Cell Res. 2023 Jan 24;424(1):113492. [Abstract]
- Food Chem Toxicol. 2021 Feb:148:111926. [Abstract]
- J Immunol. 2026 May 14;215(5):vkag085. [Abstract]
- Toxicol Appl Pharmacol. 2025 May 4:500:117371. [Abstract]
- EJNMMI Radiopharm Chem. 2025 Jul 8;10(1):40. [Abstract]
- J Inorg Biochem. 2022 Apr 20;233:111838. [Abstract]
- J Inorg Biochem. 2022 Apr:229:111725. [Abstract]
- Mol Immunol. 2025 May 9:183:93-103. [Abstract]
- PLoS One. 2021 May 17;16(5):e0251765. [Abstract]
- Theriogenology. 2024 May 24:225:152-161. [Abstract]
- Biochem Biophys Res Commun. 2026 Apr 16:809:153492. [Abstract]
- Vet Parasitol. 2025 Apr 15:337:110471. [Abstract]
- Biochem Biophys Res Commun. 2017 Apr 8;485(3):665-671. [Abstract]
- Eur J Integr Med. 2025 Aug 28;78:102545.
- Res Sq. 2026 Jun 15.
- bioRxiv. 2022 Nov 18.
- bioRxiv. 2026 Jun 18.
- bioRxiv. 2026 May 21.
- bioRxiv. 2026 Apr 28.
- SSRN. 2025 Dec 2.
- bioRxiv. 2025 Dec 19.
- Jacobs J Environ Sci. 2025 Sep 12.
- bioRxiv. 2025 Jun 24.
- bioRxiv. 2025 May 7:2025.05.01.650510. [Abstract]
- University of Oxford. 2025.
- bioRxiv. 2025 Feb 20:2025.02.19.639048. [Abstract]
- bioRxiv. 2025 Feb 26:2025.02.24.639075. [Abstract]
- bioRxiv. 2025 February 07.
- bioRxiv. 2023 Mar 21:2023.03.17.532101. [Abstract]
- J Oncol. 2022 Dec 12:2022:3425841. [Abstract]
- Research Square Preprint. 2020 Sep.
- Patent. US20190263931A1.
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Bio/Physico-chemical Assay
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Cell Migration/Invasion Assay
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
生物活性
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MCT1 |
AZD3965 is designed to selectively inhibit Monocarboxylate transporter-1 (MCT1) and will therefore be expected to influence the movement of lactate into and out of cells[1]. AZD3965 treatment causes a 3.7 fold increase in intracellular lactate in hypoxic COR-L103 and 3.7 fold and 3.9 fold increases in normoxic and hypoxic NCI-H1048 cells respectively. In all other cases a <1.9 fold increase is observed. These data are consistent with AZD3965 blocking lactate transport in cells where AZD3965 also reduces cell number and is consistent with AZD3965 acting via inhibition of MCT1. When MCT1 is overexpressed the EC50 of NCI-H1048 is increased from 0.14 nM to 10.5 nM in NCI-H1048 cells. This is consistent with AZD3965 acting via MCT1 inhibition[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1448671-31-5
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性状 Solid
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分子量 515.51
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分子式 C21H24F3N5O5S
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Color White to off-white
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SMILES
O=C1N(C(C)C)C2=C(C(C(N3OC[C@@](C)(O)C3)=O)=C(CC4=C(C)NN=C4C(F)(F)F)S2)C(N1C)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (87)
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Journal Impact Factor
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Most Recent
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Nature
2024 Oct;634(8036):1229-1237. PMID: 39322678
AZD3965 purchased from MedChemExpress. Usage Cited in: Nature. 2024 Oct;634(8036):1229-1237. [Abstract]
Measurement of intracellular L-lactate in PBMCs, BMDMs, CT26 and HCT116 cells. PBMCs and BMDMs were pre-treated with control DMSO, AR-C155858 (100 nM), Oxamate (50 mM) or AZD3965 (100 nM) for 4 h, followed by incubation for 24 h with NaCl (25 mM) or NaLac (25 mM).
AZD3965 purchased from MedChemExpress. Usage Cited in: Nature. 2024 Oct;634(8036):1229-1237. [Abstract]
Immunoblot of the total cell lysate (TCL) and immunoaffinity purified proteins in PBMCs or BMDMs isolated from mice. Wild-type mice were given NT or RS for seven consecutive days and treated with control vehicle or 50 mg/kg AZD3965 orally twice daily, followed by behavioral test and HSV-1 infection.
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Nature
2023 Aug;620(7975):881-889. PMID: 37558878 -
Cell
Structural basis of human monocarboxylate transporter 1 inhibition by anti-cancer drug candidates. [Abstract]2021 Jan 21;184(2):370-383.e13. PMID: 33333023 -
Cell
2019 Jul 11;178(2):330-345.e22. PMID: 31257027
AZD3965 purchased from MedChemExpress. Usage Cited in: Cell. 2019 Jul 11;178(2):330-345.e22. [Abstract]
AZD3965 (1-10 μM; 24 h). Migration of cells incubated with 1 and 10 mM of the lactate secretion inhibitor AZD3965.
AZD3965 purchased from MedChemExpress. Usage Cited in: Cell. 2019 Jul 11;178(2):330-345.e22. [Abstract]
Lung tumor burden of NSG mice 3 weeks after i.v. injection of mTC and mTN cells.The mice were injected four times (1/day) with AZD3965 (100 mg/kg, oral gavage) or 3-BP (10 mg/kg, i.p.), starting the day after cell injection.
AZD3965 purchased from MedChemExpress. Usage Cited in: Cell. 2019 Jul 11;178(2):330-345.e22. [Abstract]
Viability of mTC and mTN cells incubated for 24 h with AZD3965 (0-20 μM).
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Cell Metab
2026 Mar 24:S1550-4131(26)00093-8. PMID: 41881014 -
Cell Metab
Induction of a metabolic switch from glucose to ketone metabolism programs ketogenic diet-induced therapeutic vulnerability in lung cancer. [Abstract]2025 Oct 24:S1550-4131(25)00435-8. PMID: 41138721 -
Cell Metab
2025 Apr 1;37(4):903-919.e10. PMID: 39933514 -
Cell Metab
Tumor-derived exosomes drive immunosuppressive macrophages in a pre-metastatic niche through glycolytic dominant metabolic reprogramming. [Abstract]2021 Oct 5;33(10):2040-2058.e10. PMID: 34559989 -
Nat Metab
Fibroblast pyruvate carboxylase is required for collagen production in the tumour microenvironment. [Abstract]2021 Nov;3(11):1484-1499. PMID: 34764457 -
Cell Stem Cell
A small-molecule cocktail promotes mammalian cardiomyocyte proliferation and heart regeneration. [Abstract]2022 Apr 7;29(4):545-558.e13. PMID: 35395187 -
Bioact Mater
Designed bone-targeting ROS-responsive nanoplatform for precision glycolysis inhibition in postmenopausal osteoporosis. [Abstract]2025 Nov 29:58:1-18. PMID: 41403870 -
Cell Host Microbe
Enterococcus faecalis-derived lactic acid suppresses macrophage activation to facilitate persistent and polymicrobial wound infections. [Abstract]2026 Feb 11;34(2):245-262.e8. PMID: 41605216 -
ACS Nano
Carrier-Free Photodynamic Bioregulators Inhibiting Lactic Acid Efflux Combined with Immune Checkpoint Blockade for Triple-Negative Breast Cancer Immunotherapy. [Abstract]2024 Jul 21. PMID: 39034461 -
Nat Protoc
Comprehensive multiscale analysis of lactate metabolic dynamics in vitro and in vivo using highly responsive biosensors. [Abstract]2024 May;19(5):1311-1347. PMID: 38307980 -
Nat Commun
IDH2 lactylation promotes angiogenesis in murine diabetic myocardial infarction via blocking Cav1-eNOS interaction. [Abstract]2025 Dec 19. PMID: 41419771 -
Nat Commun
Histone lactylation promotes rheumatoid arthritis progression by increasing NFATc2 expression and the production of anti-lactylated histone autoantibodies. [Abstract]2025 Oct 10;16(1):9034. PMID: 41073397 -
Nat Commun
Keratinocyte-specific H4K12 lactylation drives a non-canonical IL-17-dependent signaling in psoriasis progression in mice. [Abstract]2025 Sep 30;16(1):8639. PMID: 41027887 -
Nat Commun
Mutant KRAS-activated circATXN7 fosters tumor immunoescape by sensitizing tumor-specific T cells to activation-induced cell death. [Abstract]2024 Jan 12;15(1):499. PMID: 38216551 -
Adv Sci (Weinh)
Single-Cell Simultaneous Metabolome and Transcriptome Profiling Revealing Metabolite-Gene Correlation Network. [Abstract]2024 Dec 4:e2411276. PMID: 39629980 -
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J Exp Clin Cancer Res
Cyclin G2 reverses immunosuppressive tumor microenvironment and potentiates PD-1 blockade in glioma. [Abstract]2021 Aug 27;40(1):273. PMID: 34452627 -
Microbiome
Gut microbiota-derived metabolites mediate the neuroprotective effect of melatonin in cognitive impairment induced by sleep deprivation. [Abstract]2023 Jan 31;11(1):17. PMID: 36721179 -
Metabolism
LSD1 mediates microbial metabolite butyrate-induced thermogenesis in brown and white adipose tissue. [Abstract]2020 Jan;102:154011. PMID: 31734274 -
J Immunother Cancer
Inhibition of lactate transport by MCT-1 blockade improves chimeric antigen receptor T-cell therapy against B-cell malignancies. [Abstract]2023 Jun;11(6):e006287. PMID: 37399358 -
Pharmacol Res
YBX1-LDHB axis orchestrates pyruvate production from lactate to promote ICC initiation and development. [Abstract]2026 Feb:224:108110. PMID: 41577157 -
Cell Death Dis
Mitochondrial, metabolic and bioenergetic adaptations drive plasticity of colorectal cancer cells and shape their chemosensitivity. [Abstract]2025 Apr 5;16(1):253. PMID: 40185729 -
Genome Biol
Lactate-binding protein DNMT3A in HRMECs promotes angiogenesis by upregulating VEGFA through HIF-1α lactylation. [Abstract]2025 Oct 30;26(1):377. PMID: 41168862 -
Cell Commun Signal
Lactate shuttle between cytotrophoblast and syncytiotrophoblast in the placenta enhances ferroptosis resistance and maintains placental homeostasis: implications for early pregnancy loss. [Abstract]2025 Oct 14;23(1):438. PMID: 41088442 -
Phytomedicine
Jing An decoction alleviates neuroinflammation in Tourette syndrome by regulating butyrate-mediated microbiota-gut-brain axis. [Abstract]2025 Sep:145:157009. PMID: 40674913 -
ACS Appl Mater Interfaces
Multifunctional Spiky Topological Nanocapsules for the Discrimination and Differential Inhibition of Inflammation and Cancer. [Abstract]2021 Jun 9;13(22):25727-25737. PMID: 34048646 -
Biomed Pharmacother
Pyruvate-conjugation of PEGylated liposomes for targeted drug delivery to retinal photoreceptors. [Abstract]2023 Jul:163:114717. PMID: 37435722 -
Int Endod J
2026 Mar 8. PMID: 41796430 -
Arch Toxicol
CuO-NPs-triggered heterophil extracellular traps exacerbate liver injury in chicks by promoting oxidative stress and inflammatory responses. [Abstract]2022 Nov;96(11):2913-2926. PMID: 35962800 -
Arch Toxicol
Chicken heterophils extracellular traps act as early effectors against cyclopiazonic acid dependent upon NADPH oxidase, ROS and glycolysis. [Abstract]2022 Jul;96(7):2113-2122. PMID: 35508807 -
Cell Rep
HCAR1/MCT1 Regulates Tumor Ferroptosis through the Lactate-Mediated AMPK-SCD1 Activity and Its Therapeutic Implications. [Abstract]2020 Dec 8;33(10):108487. PMID: 33296645 -
J Agric Food Chem
Glycolysis and Reactive Oxygen Species Production Participate in T-2 Toxin-Stimulated Chicken Heterophil Extracellular Traps. [Abstract]2021 Nov 3;69(43):12862-12869. PMID: 34694797 -
Front Immunol
Lactic Acid-Producing Probiotic Saccharomyces cerevisiae Attenuates Ulcerative Colitis via Suppressing Macrophage Pyroptosis and Modulating Gut Microbiota. [Abstract]2021 Nov 24;12:777665. PMID: 34899735 -
ACS Biomater Sci Eng
Metabolic Radiosensitization by Targeting Lactate Metabolism with Microfluidic Liposomal Nanocarriers. [Abstract]2026 Feb 9;12(2):1018-1031. PMID: 41603671 -
Inflamm Res
Lactate acts as a metabolic brake on inflammation by repressing NLRP3 transcription via NF-κB inhibition. [Abstract]2026 Jun 11;75(1):137. PMID: 42274732 -
Cells
Blastocyst-Derived Lactic Acid May Regulate S100A6 Expression and Function in Mouse Decidualization via Stimulation of Uterine Epithelial Arachidonic Acid Secretion. [Abstract]2024 Jan 23;13(3):206. PMID: 38334598 -
Crit Rev Anal Chem
A Critical Review on Advancement in Analytical Strategies for the Quantification of Clinically Relevant Biological Transporters. [Abstract]2022;52(7):1557-1571. PMID: 33691566 -
NPJ Genom Med
Direct cell-to-cell transfer in stressed tumor microenvironment aggravates tumorigenic or metastatic potential in pancreatic cancer. [Abstract]2022 Oct 27;7(1):63. PMID: 36302783 -
Am J Physiol Cell Physiol
β-Hydroxybutyrate attenuates bronchial smooth muscle proinflammatory cytokine production and contraction. [Abstract]2026 Jun 1;330(6):C1561-C1573. PMID: 42021684 -
Biosci Rep
Metabolic profiling and combined therapeutic strategies unveil the cytotoxic potential of selenium-chrysin (SeChry) in NSCLC cells. [Abstract]2024 Jul 11:BSR20240752. PMID: 38990147 -
Brain Commun
2024 Jun 3;6(3):fcae182. PMID: 38894951 -
Cancers
Inhibition of Alternative Cancer Cell Metabolism of EGFR Mutated Non-Small Cell Lung Cancer Serves as a Potential Therapeutic Strategy. [Abstract]2020 Jan 10;12(1):181. PMID: 31936895 -
J Physiol Biochem
2023 Feb;79(1):147-161. PMID: 36342616 -
Poult Sci
2024 Jun;103(6):103717. PMID: 38643746 -
Fish Shellfish Immunol
Zinc oxide nanoparticles (ZnO-NPs) exhibit immune toxicity to crucian carp (Carassius carassius) by neutrophil extracellular traps (NETs) release and oxidative stress. [Abstract]2022 Oct:129:22-29. PMID: 35932984 -
Fish Shellfish Immunol
Acute hypoxia promotes the liver angiogenesis of largemouth bass (Micropterus salmoides) by HIF - Dependent pathway. [Abstract]2022 Dec:131:264-273. PMID: 35940542 -
Neurophotonics
Two-point calibration protocol for the Förster Resonance Energy Transfer indicator Pyronic in neurons. [Abstract]2025 Jun;12(Suppl 2):S22807. PMID: 41141230 -
ACS Chem Biol
Detection of Chemical Engagement of Solute Carrier Proteins by a Cellular Thermal Shift Assay. [Abstract]2018 Jun 15;13(6):1480-1486. PMID: 29851333
AZD3965 purchased from MedChemExpress. Usage Cited in: ACS Chem Biol. 2018 Jun 15;13(6):1480-1486. [Abstract]
For analysis of dose responses, levels of thermostable SLC16A1 and SLCO1A2 are analyzed in lysates heated to 65 or 75℃, at 0, 5, 10, 20, 50, 100, and 1000 nM AZD3965.
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Cell Signal
2025 May 17:111877. PMID: 40389045 -
AAPS J
Cellular Uptake of MCT1 Inhibitors AR-C155858 and AZD3965 and Their Effects on MCT-Mediated Transport of L-Lactate in Murine 4T1 Breast Tumor Cancer Cells. [Abstract]2019 Jan 7;21(2):13. PMID: 30617815 -
Am J Pathol
Lactate Contributes to Remote Ischemic Preconditioning-Mediated Protection Against Myocardial Ischemia Reperfusion Injury by Facilitating Autophagy via the AMP-Activated Protein Kinase-Mammalian Target of Rapamycin-Transcription Factor EB-Connexin 43 Axis. [Abstract]2024 Oct;194(10):1857-1878. PMID: 39069170 -
Exp Cell Res
Lactate induced mesenchymal stem cells activation promotes gastric cancer cells migration and proliferation. [Abstract]2023 Jan 24;424(1):113492. PMID: 36702194 -
Food Chem Toxicol
Diacetoxyscirpenol-induced heterophil extracellular traps contribute to the immune toxicity of liver injury in chickens. [Abstract]2021 Feb:148:111926. PMID: 33352262 -
J Immunol
Acidosis enables the NLRP3 inflammasome-inhibiting effects of β-hydroxybutyrate and short-chain carboxylic acids. [Abstract]2026 May 14;215(5):vkag085. PMID: 42153447 -
Toxicol Appl Pharmacol
2025 May 4:500:117371. PMID: 40328338 -
EJNMMI Radiopharm Chem
Rapid cleavage of 6-[18F]fluoronicotinic acid prosthetic group governs BT12 glioblastoma xenograft uptake: implications for radiolabeling design of biomolecules. [Abstract]2025 Jul 8;10(1):40. PMID: 40629197 -
J Inorg Biochem
Nanosilver-stimulated heterophil extracellular traps promoted liver and kidney injury in chicken. [Abstract]2022 Apr 20;233:111838. PMID: 35504082 -
J Inorg Biochem
Alumina nanoparticles-induced heterophil extracellular traps exacerbate liver injury by regulating oxidative stress and inflammation in chickens. [Abstract]2022 Apr:229:111725. PMID: 35063926 -
Mol Immunol
Gastric cancer cells shuttle lactate to induce inflammatory CAF-like phenotype and function in bone marrow-derived mesenchymal stem cells. [Abstract]2025 May 9:183:93-103. PMID: 40347782 -
PLoS One
Targeting neovascularization and respiration of tumor grafts grown on chick embryo chorioallantoic membranes. [Abstract]2021 May 17;16(5):e0251765. PMID: 33999935 -
Theriogenology
MCT1-mediated transport of valeric acid promotes porcine preimplantation embryo development by improving mitochondrial function and inhibiting the autophagic AMPK-ULK1 pathway. [Abstract]2024 May 24:225:152-161. PMID: 38805997 -
Biochem Biophys Res Commun
Targeting Warburg effect: involvement of lactate transporter MCT1 and its chaperone in cancer cell killing by 18β-glycyrrhetinic acid. [Abstract]2026 Apr 16:809:153492. PMID: 41719881 -
Vet Parasitol
2025 Apr 15:337:110471. PMID: 40245810 -
Biochem Biophys Res Commun
MACC1 mediates chemotherapy sensitivity of 5-FU and cisplatin via regulating MCT1 expression in gastric cancer. [Abstract]2017 Apr 8;485(3):665-671. PMID: 28235486 -
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bioRxiv
Acidosis Licenses the NLRP3 Inflammasome-Inhibiting Effects of Beta-Hydroxybutyrate and Short-Chain Carboxylic Acids. [Abstract]2025 May 7:2025.05.01.650510. PMID: 40654769 -
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bioRxiv
Beta-Hydroxybutyrate Attenuates Bronchial Smooth Muscle Pro-Inflammatory Cytokine Production. [Abstract]2025 Feb 20:2025.02.19.639048. PMID: 40027689 -
bioRxiv
2025 Feb 26:2025.02.24.639075. PMID: 40060651 -
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bioRxiv
2023 Mar 21:2023.03.17.532101. PMID: 36993446 -
J Oncol
2022 Dec 12:2022:3425841. PMID: 36545125 -
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溶剤 & 溶解度
DMSO : 40 mg/mL (77.59 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
Cells are plated overnight and treated with 100 nM AZD3965 or vehicle for 24 hours. The cells are then washed, once in PBS and twice with lysis buffer (50 mM Mops, 100 mM KCl, 5 mM MgCl2, 1 mM EDTA, 0.1 mM DTT, 1 mM PMSF supplemented with 1× mini complete protease inhibitor cocktail tablets. The cells are harvested by scraping and centrifugation, and the pellet snap frozen without buffer in liquid nitrogen. Frozen aliquots of cells are thawed on ice and re-suspended in lysis buffer. Cells are lysed by 3 rounds of freezing in liquid nitrogen and thawing at 37°C for 2 minutes each. Lysates are subsequently centrifuged (13000 g, 10min, 4°C) until clear and then stored on ice. Enzyme activity in the cell lysates is determined using a micro-plate reader to measure either production or depletion of NADH/NADPH, through its absorbance at 340/10 nm, occurring as a result of direct or coupled enzyme reactions. The 96 well plates used for the assays are pre-heated to 37°C for 10 minutes prior to starting reactions, initiated by the addition of 5 μL cell lysate to 95 μL of reaction buffer (50 mM Mops pH 7.4, 100 mM KCl, 5 mM free magnesium). The standard reaction buffer is supplemented to assay the kinetics of the different enzymes. Absorbance values for controls are subtracted from absorbance of corresponding reactions. Graphpad prism 6 is used to plot V0 values against substrate concentration and determine Vmax and Km values. The Vmax is then normalised to the protein concentration in the cell lysate[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
COR-L103 xenografts are grown by subcutaneous injection of 5×106 cells in 0.2 mL of 1:1 serum-free RPMI:Matrigel into the mid-dorsal flank of 8 to 14-week-old male NOD scid gamma mice. Mice are housed in individually vented caging systems in a 12-hour light/12-hour dark environment and maintained at uniform temperature and humidity. Tumor size is measured twice a week using calipers and the volume calculated as tumor length×tumor width2/2. 30 days after implantation, mice bearing tumors between 150 and 250mm3 are randomized into two groups of six and treated with 100 mg/kg BID AZD3965 in 0.5% hydroxypropyl methyl cellulose, 0.1% tween 80 or vehicle only by oral gavage for 21 days. Measurements are continued 3 times a week for the duration of drug treatment to assess tumor growth kinetics. At sacrifice tumors are collected to determine intra-tumor lactate concentration.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (287 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Bola BM, et al. Inhibition of monocarboxylate transporter-1 (MCT1) by AZD3965 enhances radiosensitivity by reducing lactate transport. Mol Cancer Ther. 2014 Dec;13(12):2805-16. [Content Brief]
[2]. Polanski R, et al. Activity of the monocarboxylate transporter 1 inhibitor AZD3965 in small cell lung cancer. Clin Cancer Res. 2014 Feb 15;20(4):926-37. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9398 mL | 9.6991 mL | 19.3983 mL | 48.4957 mL |
| 5 mM | 0.3880 mL | 1.9398 mL | 3.8797 mL | 9.6991 mL | |
| 10 mM | 0.1940 mL | 0.9699 mL | 1.9398 mL | 4.8496 mL | |
| 15 mM | 0.1293 mL | 0.6466 mL | 1.2932 mL | 3.2330 mL | |
| 20 mM | 0.0970 mL | 0.4850 mL | 0.9699 mL | 2.4248 mL | |
| 25 mM | 0.0776 mL | 0.3880 mL | 0.7759 mL | 1.9398 mL | |
| 30 mM | 0.0647 mL | 0.3233 mL | 0.6466 mL | 1.6165 mL | |
| 40 mM | 0.0485 mL | 0.2425 mL | 0.4850 mL | 1.2124 mL | |
| 50 mM | 0.0388 mL | 0.1940 mL | 0.3880 mL | 0.9699 mL | |
| 60 mM | 0.0323 mL | 0.1617 mL | 0.3233 mL | 0.8083 mL |
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