- Cart - 0 item(s)
- $0.00
Your shopping cart is empty!
- Chemistry
- Bioactive Molecules
- Anti-infection
- Apoptosis
- Autophagy
- Cell Cycle/DNA Damage
- Cytoskeleton
- Epigenetics
- GPCR/G Protein
- Immunology/Inflammation
- JAK/STAT Signaling
- MAPK/ERK Pathway
- Membrane Transporter/Ion Channel
- Metabolic Enzyme/Protease
- Neuronal Signaling
- NF-κB
- PI3K/Akt/mTOR
- PROTAC
- Protein Tyrosine Kinase/RTK
- Stem Cell/Wnt
- TGF-beta/Smad
- Vitamin D Related/Nuclear Receptor
- Others
- Methylation
- Cytoskeletal Signaling
- Natural Products
- Alkaloids
- Amino acid
- Anthraquinones
- Cerebrosides
- Chalcones
- Coumarins
- Diterpenoids
- Flavonoids
- Iridoids
- Lignans
- Lipids
- Miscellaneous
- Monoterpenoids
- Other terpenes
- Phenols
- Phenylpropanoids
- Quinones
- Saccharides
- Sesquiterpenoids
- Steroids
- Tetraterpenoids
- Thiophenes
- Triterpenoids
- Xanthones
- Polyphenols
- Stibene glucosides
- Oligose
- Anthocyanins
- Miscellaneous
- Chromones
- Terpenoids
- Indoles
- Procyanidins
- Aliphatics
- Botanical Cyclopeptides
- ADCs
- Antibodies
- Multiplex IHC
- Material Science
- Others
[CAS NO. 1448671-31-5] AZD3965
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-12750 |
| Brand: | MCE |
| CAS: | 1448671-31-5 |
Overview
| MDL | MFCD28963899 |
|---|---|
| Molecular Weight | 515.51 |
| Molecular Formula | C21H24F3N5O5S |
| 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 |
30 Publications Citing Use of MCE
- [1]Cell. 2021 Jan 21;184(2):370-383.e13.
- [2]Cell. 2019 Jul 11;178(2):330-345.e22.
- [3]Cell Metab. 2021 Sep 17;S1550-4131(21)00421-6.
- [4]Cell Stem Cell. 2022 Apr 7;29(4):545-558.e13.
- [5]Nat Metab. 2021 Nov 11.
- [6]Microbiome. 2023 Jan 31;11(1):17.
- [7]ACS Appl Mater Interfaces. 2021 May 28.
- [8]Cell Rep. 2020 Dec 8;33(10):108487.
- [9]J Exp Clin Cancer Res. 2021 Aug 27;40(1):273.
- [10]Metabolism. 2020 Jan;102:154011.
- [11]Cancers. 2020 Jan 10;12(1):181.
- [12]NPJ Genom Med. 2022 Oct 27;7(1):63.
- [13]Front Immunol. 2021 Nov 24;12:777665.
- [14]Arch Toxicol. 2022 May 4.
- [15]Food Chem Toxicol. 2020 Dec 24;148:111926.
- [16]Crit Rev Anal Chem. 2021 Mar 10;1-15.
- [17]ACS Chem Biol. 2018 Jun 15;13(6):1480-1486.
- [18]J Agric Food Chem. 2021 Oct 25.
- [19]AAPS J. 2019 Jan 7;21(2):13.
- [20]Exp Cell Res. 2023 Jan 24;424(1):113492.
- [21]Fish Shellfish Immunol. 5 August 2022.
- [22]Fish Shellfish Immunol. 2022 Aug 3;S1050-4648(22)00414-4.
- [23]J Inorg Biochem. 2022 Apr 20;233:111838.
- [24]J Inorg Biochem. 13 January 2022, 111725.
- [25]Biochem Biophys Res Commun. 2017 Apr 8;485(3):665-671.
- [26]J Physiol Biochem. 2022 Nov 7.
- [27]PLoS One. 2021 May 17;16(5):e0251765.
- [28]J Oncol. 2022.
- [29]Research Square Preprint. 2020 Sep.
- [30]Patent. US20190263931A1.
Summary
AZD3965 is a selective MCT1 inhibitor with a K i of 1.6 nM, showing 6-fold selectivity over MCT2.
IC50 & Target
Ki: 1.6 nM (MCT1) [1]
In Vitro
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 EC 50 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
COR-L103 tumor bearing mice are treated with 100 mg/kg AZD3965 or vehicle BIDfor 21 days and the tumor volume monitored. Pharmacokinetic analysis demonstrates that 100 mg/kg AZD3965 BID results in concentrations of free AZD3965 predicted to inhibit lactate transport. AZD3965 treatment significantly reduces the growth of COR-L103 tumors, although tumor regression is not seen, consistent with AZD3965 only targeting the hypoxic fraction of the tumor [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01791595 | Cancer Research UK|AstraZeneca |
Adult Solid Tumor|Diffuse Large B Cell Lymphoma|Burkitt Lymphoma
|
April 23, 2013 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 193.98 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9398 mL | 9.6991 mL | 19.3983 mL |
| 5 mM | 0.3880 mL | 1.9398 mL | 3.8797 mL |
| 10 mM | 0.1940 mL | 0.9699 mL | 1.9398 mL |
-
1.
Add each solvent one by one: 0.5% HPMC >> 0.2%Tween80
Solubility: 5 mg/mL (9.70 mM); Suspended solution; Need ultrasonic
-
2.
Add each solvent one by one: 20% HP-β-CD in saline
Solubility: 5 mg/mL (9.70 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C
-
3.
-
4.
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
-
5.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution
References
- [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.
- [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.
Arctom is a premier supply platform offering over 600K unique items of Building Blocks, Bioactive Molecules, Natural Products, ADC PEG Linkers, Antibodies, and other Research Chemicals for global pharmaceutical, biotech, university, and industrial customers. We accelerate your research by providing better and faster purchasing experience & services.