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Purity: ≥98%
Kevetrin hydrochloride (also known as thioureidobutyronitrile; 4-Isothioureidobutyronitrile hydrochloride; thioureidobutyronitrile hydrochloride; thioureido butyronitrile hydrochloride), is a water-soluble, small molecule activator of the tumor suppressor protein p53. Potentially, it has anti-cancer properties. After being injected, thioureidobutyronitrile activates p53, which in turn triggers the expression of p21 and PUMA (p53 up-regulated modulator of apoptosis), inhibiting the growth of cancer cells and causing tumor cell apoptosis. In drug-resistant cancers with mutated p53, thioureidobutyronitrile might be useful. In cancer cells, the p53 tumor suppressor, a transcription factor controlling the expression of numerous stress response genes and mediating various anti-proliferative processes, is frequently mutated. a little chemical that has the potential to be anti-cancer and activates the p53 tumor suppressor protein.
| ln Vitro |
The proliferation of KASUMI-1 cells was considerably suppressed, dose-wise, by kevetrin hydrochloride (85, 170, 340 μM; 6 h), but not that of MOLM-13 [1]. Kevetrin hydrochloride (340 μM; 6) induces metallothionein (MT) expression in acute myeloid leukemia (AML) cells and downregulates p53 activity. Kevetrin hydrochloride (340 μM; 24 hours) induces KASUMI-1 cell line cells without causing changes to the cell cycle. Kevetrin hydrochloride is the forkhead box K2 regulator of WNT/β-catenin signaling Regulator-related gene signal transducer and regulatory activator 5A (STAT5A). P53 is increased by kevetrin hydrochloride (100, 200, and 400 μM; 48 h)[1].
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| ln Vivo |
In tumor xenograft models, kevetrin hydrochloride (150–200 mg/kg; i.p.; 20 days) suppresses tumor development and prolongs focus, and it promotes about 40% cell death in OV-90 or OVCAR-3 xenograft tumors.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: MOLM-13 and KASUMI-1 cells Tested Concentrations: 85, 170 and 340 µM Incubation Duration: 6 h, 6 h + mRNA and protein levels, and induce A2780 cells to produce p21 protein[1]. 66 h Wash-out (wo,×1), 6 h + 66 h wo (×2), 6 h + 66 h wo (×3) Experimental Results: Only inhibited the cell viability of KASUMI-1 cells, reducing the cell viability dose and time dependent manner. Apoptosis analysis[1] Cell Types: MOLM-13, KASUMI-1, TP53-wt OCI-AML3 and TP53 mutant NOMO-1 Cell Tested Concentrations: 85, 170 and 340 µM Incubation Duration: 24, 48 and 72 hrs (hours) Experimental Results: Induces apoptosis of KASUMI-1 cells at 340 μM concentration for 24 hrs (hours) and inhibits MOLM-13 at 340 μM concentration for 48 hrs (hours). Cell cycle analysis[1] Cell Types: MOLM-13, KASUMI-1, TP53-wt OCI-AML3 and TP53 mutant NOMO-1 Cell Tested Concentrations: 340 µM Incubation Duration: 24 and 48 hrs (hours) Experimental Results: Cell cycle arrest OCI-AML3 and NOMO-1 cells are in the G0/G1 phase, and does not change the cell cycle of MOLM-13 and KASUMI-1 cells. |
| Animal Protocol |
Animal/Disease Models: A2780 nude mouse xenograft tumor model [2]
Doses: 200 mg/kg Route of Administration: intraperitoneal (ip) injection; time [2]. 3 times a week for 20 days Experimental Results: Inhibition of tumor growth and suppression of tumor volume. Animal/Disease Models: Mouse SKOV-3 xenograft ascites model [2] Doses: 150 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Prolonged mouse survival time, maintaining 100% survival rate for more than 35 days. |
| References |
[1]. Napolitano R, et al. Kevetrin induces apoptosis in TP53 wildtype and mutant acute myeloid leukemia cells. Oncol Rep. 2020 Oct;44(4):1561-1573.
[2]. Kumar A, et al. Abstract 3221: kevetrin induces p53-dependent and independKumar A, et al. Abstract 3221: kevetrin induces p53-dependent and independent cell cycle arrest and apoptosis in ovarian cancer cell lines representing heterogeneous histologies. Cancer Research. 2017. 77(13 Supplement), 3221-3221. |
| Molecular Formula |
C5H10CLN3S
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| Molecular Weight |
179.67
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| Exact Mass |
179.0283962
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| Elemental Analysis |
C, 33.43; H, 5.61; Cl, 19.73; N, 23.39; S, 17.84
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| CAS # |
66592-89-0
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| Related CAS # |
Kevetrin hydrochloride-13C2,15N3;2300178-72-5
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| Appearance |
white solid powder
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| SMILES |
C(CC#N)CSC(=N)N.Cl
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| InChi Key |
NCXJZJFDQMKRKM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C5H9N3S.ClH/c6-3-1-2-4-9-5(7)8;/h1-2,4H2,(H3,7,8);1H
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| Chemical Name |
3-cyanopropyl carbamimidothioate;hydrochloride
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (13.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (13.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (13.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (556.58 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.5658 mL | 27.8288 mL | 55.6576 mL | |
| 5 mM | 1.1132 mL | 5.5658 mL | 11.1315 mL | |
| 10 mM | 0.5566 mL | 2.7829 mL | 5.5658 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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