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ProTAME is a novel inhibitor of APC/CFzr and APC/CCdc20 with anticancer activity. It acts as a cell permeable prodrug of TAME, which is an anaphase-promoting complex/cyclosome (APC/C) inhibitor that binds to the APC preferentially suppresses APC/C(Cdc20). It arrests cells in metaphase without perturbing the spindle, but is dependent on the spindle assembly checkpoint (SAC). Combinations of proTAME with topoisomerase inhibitors, etoposide and doxorubicin, significantly increase cell death in Multiple Myeloma (MM) cell lines and primary cells, particularly if TOPIIα levels are first increased through pre-treatment with ProTAME.
| ln Vitro |
ProTAME stops mouse and bovine oocytes, as well as mouse 2-cell embryos, from entering anaphase. Mammalian oocytes treated with proTAME (0-100 μM) exhibit dose-dependent metaphase arrest and early cleavage embryos. Furthermore, spindle assembly checkpoint (SAC) activity is not necessary for the drug-induced metaphase arrest [1]. Because ProTAME inhibits APC/C, it prevents mouse oocyte meiosis I. The arrest of oocytes and embryos is irreversible, in contrast to somatic cells [1]. In oocytes and embryos, proTAME (0–20 μM) dose-dependently alters spindle morphological characteristics [1]. ProTAME efficiently overcomes resistance resulting from Polo-like kinase 1 (PLK1)-based resistance in ovarian cancer cells, CDH1 hyperphosphorylation-based resistance in glioblastoma cells, and CDC20-based resistance in diffuse large B-cell lymphoma cells. therapeutic qualities [1]. OVCAR-3 cell growth is inhibited by proTAME, with an IC50 of 12.5 μM[2].
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| References |
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| Molecular Formula |
C34H38N4O12S
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| Molecular Weight |
726.75
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| Exact Mass |
726.22
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| Elemental Analysis |
C, 56.19; H, 5.27; N, 7.71; O, 26.42; S, 4.41
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| CAS # |
1362911-19-0
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| PubChem CID |
56924780
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.587
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| LogP |
6.05
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
23
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| Heavy Atom Count |
51
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| Complexity |
1210
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C(OC)(=O)[C@@H](NS(C1=CC=C(C)C=C1)(=O)=O)CCC/N=C(\NC(OCOC(CC1=CC=CC=C1)=O)=O)/NC(=O)OCOC(=O)CC1=CC=CC=C1
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| InChi Key |
MHYOVHULCQSDRZ-NDEPHWFRSA-N
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| InChi Code |
InChI=1S/C34H38N4O12S/c1-24-15-17-27(18-16-24)51(44,45)38-28(31(41)46-2)14-9-19-35-32(36-33(42)49-22-47-29(39)20-25-10-5-3-6-11-25)37-34(43)50-23-48-30(40)21-26-12-7-4-8-13-26/h3-8,10-13,15-18,28,38H,9,14,19-23H2,1-2H3,(H2,35,36,37,42,43)/t28-/m0/s1
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| Chemical Name |
methyl (2S)-5-[bis[(2-phenylacetyl)oxymethoxycarbonylamino]methylideneamino]-2-[(4-methylphenyl)sulfonylamino]pentanoate
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| Synonyms |
pro-Tosyl-L-Arginine Methyl Ester ProTAME
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~137.60 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.75 mg/mL (5.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 37.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3760 mL | 6.8799 mL | 13.7599 mL | |
| 5 mM | 0.2752 mL | 1.3760 mL | 2.7520 mL | |
| 10 mM | 0.1376 mL | 0.6880 mL | 1.3760 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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