[CAS NO. 66592-89-0] Kevetrinhydrochloride

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PRODUCTS SPECIFICATIONS [66592-89-0]

Catalog

HY-16271

Brand

MCE

CAS

66592-89-0

DESCRIPTION [66592-89-0]

Overview

MDL	MFCD22572767
Molecular Weight	179.67
Molecular Formula	C5H10ClN3S
SMILES	NC(SCCCC#N)=N.[H]Cl

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

Summary

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] .

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

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] .

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

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03042702	Innovation Pharmaceuticals, Inc.	Ovarian Cancer	February 9, 2017	Phase 2

Appearance

Solid

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:

H ₂ O : 100 mg/mL ( 556.58 mM ; Need ultrasonic)

DMSO : ≥ 40 mg/mL ( 222.63 mM )

* "≥" 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
10 mM	0.5566 mL	2.7829 mL	5.5658 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 100 mg/mL (556.58 mM); Clear solution; Need ultrasonic
2.

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
3.

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
4.

Add each solvent one by one: 10% DMSO >> 90% corn oil

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

* All of the co-solvents are available by MCE.