Apratastat (Synonyms: TMI-005) |
| Catalog No.GC35377 |
An inhibitor of ADAM17 and MMPs
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 287405-51-0
Sample solution is provided at 25 µL, 10mM.
TMI-005 is an inhibitor of disintegrin and metalloproteinase domain-containing protein 17/TNF-α converting enzyme (ADAM17/TACE), matrix metalloproteinase-1 (MMP-1), and MMP-13 (IC50s = 20, 33, and 8.1 nM, respectively).[1] It inhibits LPS-induced TNF-α release in isolated human whole blood (IC50 = 144 ng/ml).[2] TMI-005 (25 μM) reduces basal and ionizing radiation-induced secretion of the ADAM17/TACE substrates ALCAM and amphiregulin from A549 and NCI H125 cells.[3]It inhibits proliferation of A549 cells when used at concentrations of 25 and 50 μM and sensitizes A549 and NCI H125 cells to ionizing radiation at 25 μM. TMI-005 (25 mg/kg twice per day) reduces tumor growth in an A549 mouse xenograft model when administered in combination with ionizing radiation.
Reference:
[1]. Levin, J.I., Chen, J.M., and Cole, D.C. Acetylenic α-amino acid-based sulfonamide hydroxamic acid tace inhibitors. WO 00/44709, (2000).
[2]. Shu, C., Zhou, H., Afsharvand, M., et al. Pharmacokinetic-pharmacodynamic modeling of apratastat: A population-based approach. J. Clin. Pharmacol. 51(4), 472-481 (2011).
[3]. Sharma, A., Bender, S., Zimmerman, M., et al. Secretome signature identifies ADAM17 as novel target for radiosensitization of non-small cell lung cancer. Clin. Cancer Res. 22(17), 4428-4439 (2016).
| Cas No. | 287405-51-0 | SDF | |
| Synonyms | TMI-005 | ||
| Chemical Name | (3S)-N-hydroxy-4-[[4-[(4-hydroxy-2-butyn-1-yl)oxy]phenyl]sulfonyl]-2,2-dimethyl-3-thiomorpholinecarboxamide | ||
| Canonical SMILES | CC1(C)[C@H](C(NO)=O)N(S(=O)(C2=CC=C(OCC#CCO)C=C2)=O)CCS1 | ||
| Formula | C17H22N2O6S2 | M.Wt | 414.5 |
| Solubility | 10mg/mL in ethanol, 25mg/mL in DMSO, or in DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4125 mL | 12.0627 mL | 24.1255 mL |
| 5 mM | 0.4825 mL | 2.4125 mL | 4.8251 mL |
| 10 mM | 0.2413 mL | 1.2063 mL | 2.4125 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)
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