| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
UMK57 targets the kinetochore-microtubule (k-MT) attachment machinery during mitosis, specifically by activating MCAK (mitotic centromere-associated kinesin), a microtubule depolymerase that is a member of the kinesin-13 family. MCAK plays a critical role in correcting erroneous k-MT attachments by destabilizing microtubule ends at the kinetochore. By potentiating MCAK activity, UMK57 enhances the correction of k-MT attachment errors, thereby increasing chromosome segregation fidelity. The compound also destabilizes kinetochore-microtubule attachments during mitosis, reducing the occurrence of lagging chromosomes and chromosome mis-segregation in CIN cancer cells. Its mechanism involves reversible modulation of the Aurora B signaling pathway.
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| ln Vitro |
In vitro, UMK57 is a small-molecule compound that specifically promotes k-MT attachment error correction and inhibits chromosome mis-segregation. It acts as an activator of MCAK and a destabilizer of kinetochore-microtubule attachments. UMK57 enhances MCAK-dependent microtubule depolymerization, increases kinetochore-microtubule turnover efficiency, and reduces chromosome mis-segregation and lagging chromosomes. The compound inhibits cancer cell proliferation. Its effects on mitotic progression and chromosome segregation have been characterized in cell-based assays using CIN cancer cell lines.
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| ln Vivo |
In vivo, UMK57 potentiates MCAK activity and transiently suppresses chromosome mis-segregation in CIN cancer cells. The compound has been shown to inhibit cancer cell proliferation. By promoting faithful chromosome segregation, UMK57 has the potential to reduce aneuploidy and genomic instability in cancer cells. However, detailed in vivo efficacy data from animal models are limited. Further studies are needed to fully characterize its therapeutic potential.
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| Enzyme Assay |
In vitro enzyme/receptor binding (non-cell) assays for UMK57 involve studying its effects on microtubule dynamics and MCAK activity. Microtubule polymerization assays are performed using purified tubulin and varying concentrations of UMK57 to assess its effects on microtubule assembly and disassembly. MCAK activity is measured using microtubule depolymerization assays, where the rate of microtubule depolymerization by MCAK is monitored in the presence of UMK57. The compound's ability to destabilize microtubules and enhance MCAK activity is quantified.
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| Cell Assay |
In vitro cell-based experiments for UMK57 are conducted using CIN cancer cell lines. Cells are treated with UMK57 at varying concentrations, and mitotic progression is assessed by immunofluorescence staining of kinetochore and microtubule markers (e.g., CREST, α-tubulin, Aurora B). The frequency of chromosome mis-segregation and lagging chromosomes is quantified by live-cell imaging or by scoring mitotic cells. Cell proliferation is assessed using standard viability assays. The compound's effects on Aurora B signaling are evaluated by Western blot analysis of Aurora B substrates.
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| Animal Protocol |
In vivo animal experiments for UMK57 are performed in xenograft mouse models of cancer. UMK57 is administered, and tumor growth, mitotic index, and chromosome segregation fidelity are assessed. However, detailed in vivo efficacy data are limited. Further studies are needed to evaluate the compound's therapeutic potential in animal models of CIN cancers.
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| ADME/Pharmacokinetics |
UMK57 is a small molecule (MW 295.4, formula C17H17N3S) with suitable physicochemical properties for research use. Detailed pharmacokinetic parameters are limited in available literature. The compound is soluble in DMSO. Its stability in solution has rarely been reported.
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| Toxicity/Toxicokinetics |
Preclinical toxicology data for UMK57 are limited. The compound is supplied for laboratory research use only. As a compound that modulates mitotic progression and microtubule dynamics, potential effects on normal cell division should be considered.
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| References | |
| Additional Infomation |
UMK57 is a research compound used primarily for studying mitotic regulation, chromosomal instability, aneuploidy, and potential cancer treatments involving microtubule dynamics. Its ability to promote k-MT attachment error correction and inhibit chromosome mis-segregation makes it a valuable tool for exploring the mechanisms of chromosomal instability in cancer and for identifying new therapeutic strategies targeting mitotic fidelity. The compound is not approved for clinical use.
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| Molecular Formula |
C17H17N3S
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| Molecular Weight |
295.401982069016
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| Exact Mass |
295.114
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| Elemental Analysis |
C, 69.12; H, 5.80; N, 14.22; S, 10.85
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| CAS # |
342595-74-8
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| PubChem CID |
693939
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
492.5±45.0 °C at 760 mmHg
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| Flash Point |
251.7±28.7 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.673
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| LogP |
4.12
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
350
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C=C(C2C=CC(C)=CC=2)C2C1=NC=NC=2N1CCCC1
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| InChi Key |
VOAWQTDHSSKEKA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H17N3S/c1-12-4-6-13(7-5-12)14-10-21-17-15(14)16(18-11-19-17)20-8-2-3-9-20/h4-7,10-11H,2-3,8-9H2,1H3
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| Chemical Name |
5-(4-methylphenyl)-4-pyrrolidin-1-ylthieno[2,3-d]pyrimidine
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| Synonyms |
UMK57, UMK-57, UMK 57
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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 : ~2 mg/mL (~6.77 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3852 mL | 16.9262 mL | 33.8524 mL | |
| 5 mM | 0.6770 mL | 3.3852 mL | 6.7705 mL | |
| 10 mM | 0.3385 mL | 1.6926 mL | 3.3852 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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