2. Apoptosis
  3. MDM-2/p53 Apoptosis
  4. Kevetrin hydrochloride

Kevetrin hydrochloride  (Synonyms: 4-Isothioureidobutyronitrile hydrochloride; thioureidobutyronitrile hydrochloride; thioureido butyronitrile hydrochloride)

Cat. No.: HY-16271 Purity: ≥98.0%
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Kevetrin hydrochloride is a potent activator of p53, induces apoptosis in TP53 wild-type and mutant acute myeloid leukemia cells. Kevetrin a preferential cytotoxic activity against blast cells.

For research use only. We do not sell to patients.

Kevetrin hydrochloride Chemical Structure

Kevetrin hydrochloride Chemical Structure

CAS No. : 66592-89-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 85 In-stock
Solution
10 mM * 1 mL in DMSO USD 85 In-stock
Solid
5 mg USD 49 In-stock
10 mg USD 77 In-stock
50 mg USD 242 In-stock
100 mg USD 407 In-stock
500 mg USD 1221 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Kevetrin hydrochloride:

Kevetrin hydrochloride Related Antibodies

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1 Publications Citing Use of MCE Kevetrin hydrochloride

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Kevetrin hydrochloride is a potent activator of p53, induces apoptosis in TP53 wild-type and mutant acute myeloid leukemia cells. Kevetrin a preferential cytotoxic activity against blast cells[1][2].

In Vitro

Kevetrin hydrochloride (85, 170, 340 μM; 6 h) significantly inhibits KASUMI-1 cells growth in a dose-dependent manner, without affecting MOLM-13 cells[1].
Kevetrin hydrochloride (340 μM; 6 h) induces metallothionein (MT) expression in acute myeloid leukemia (AML) cells, and also down-regulates genes in relation to p53 activity, the regulator of WNT/β-catenin signaling forkhead box K2 and the transcription factor signal transducer and activator of transcription 5A (STAT5A)[1].
Kevetrin hydrochloride (340 μM; 24 h) induces apoptosis on KASUMI-1 cell line, without leading cell cycle alteration[1].
Kevetrin hydrochloride (100, 200, 400 μM; 48 h) increases the mRNA and protein level of p53 and induces p21 protein production in A2780 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Kevetrin hydrochloride Related Antibodies

Cell Viability Assay[1]

Cell Line: MOLM-13 and KASUMI-1 cells
Concentration: 85, 170 and 340 µM
Incubation Time: 6 h, 6 h + 66 h wash-out (wo,×1), 6 h + 66 h wo (×2), 6 h + 66 h wo (×3)
Result: Only inhibited the cell viability of KASUMI-1 cells and decreased cells viability in a dose- and time-dependent manner.

Apoptosis Analysis[1]

Cell Line: MOLM-13, KASUMI-1, TP53-wt OCI-AML3, and TP53-mutant NOMO-1 cells
Concentration: 85, 170 and 340 µM
Incubation Time: 24, 48, and 72 hours
Result: Induced KASUMI-1 apoptosis at 340 μM on 24 hours and inhibited MOLM-13 at 340 μM on 48 h.

Cell Cycle Analysis[1]

Cell Line: MOLM-13, KASUMI-1, TP53-wt OCI-AML3, and TP53-mutant NOMO-1 cells
Concentration: 340 µM
Incubation Time: 24, and 48 hours
Result: Arrested cell cycle of OCI-AML3 and NOMO-1 cells at G0/G1 phase, without altering cell cycle of MOLM-13 and KASUMI-1 cells.
In Vivo

Kevetrin hydrochloride (150-200 mg/kg; i.p.; 20 d) induces ~40% cell death in OV-90 or OVCAR-3 xenograft tumors, also inhibits tumor growth and extents survival time of mice with tumor xenograft mode[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: A2780 xenograft tumor model in nude mice[2]
Dosage: 200 mg/kg
Administration: Intraperitoneal injection; 3 times per week, for 20 days
Result: Inhibited tumor growth and suppressed the tumor volume.
Animal Model: SKOV-3 xenograft ascites model in mice[2]
Dosage: 150 mg/kg
Administration: Intraperitoneal injection
Result: Prolonged the survival time of mice, and maintained 100% survival rate more over 35 days.
Clinical Trial
Molecular Weight

179.67

Formula

C5H10ClN3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC(SCCCC#N)=N.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (556.58 mM; Need ultrasonic)

DMSO : ≥ 40 mg/mL (222.63 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (13.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (13.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (556.58 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 5.5658 mL 27.8288 mL 55.6576 mL 139.1440 mL
5 mM 1.1132 mL 5.5658 mL 11.1315 mL 27.8288 mL
10 mM 0.5566 mL 2.7829 mL 5.5658 mL 13.9144 mL
15 mM 0.3711 mL 1.8553 mL 3.7105 mL 9.2763 mL
20 mM 0.2783 mL 1.3914 mL 2.7829 mL 6.9572 mL
25 mM 0.2226 mL 1.1132 mL 2.2263 mL 5.5658 mL
30 mM 0.1855 mL 0.9276 mL 1.8553 mL 4.6381 mL
40 mM 0.1391 mL 0.6957 mL 1.3914 mL 3.4786 mL
50 mM 0.1113 mL 0.5566 mL 1.1132 mL 2.7829 mL
60 mM 0.0928 mL 0.4638 mL 0.9276 mL 2.3191 mL
80 mM 0.0696 mL 0.3479 mL 0.6957 mL 1.7393 mL
100 mM 0.0557 mL 0.2783 mL 0.5566 mL 1.3914 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Kevetrin hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Kevetrin66592-89-04-Isothioureidobutyronitrilethioureidobutyronitrilethioureido butyronitrileMDM-2/p53ApoptosisMOLM-13KASUMI-1TP53-wt OCI-AML3TP53-mutant NOMO-1myeloid leukemiaTP53 wild-typemutant primarypreferential cytotoxic activityblast cellsInhibitorinhibitorinhibit

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