Kevetrin hydrochloride

SKU: orb1223081

Description

Kevetrin hydrochloride is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.(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.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).Kevetrin hydrochloride (340 μM; 24 h) induces apoptosis on KASUMI-1 cell line, without leading cell cycle alteration.Kevetrin hydrochloride (100, 200, 400 μM; 48 h) increases the mRNA and protein level of p53 and induces p21 protein production in A2780 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.

Images & Validation

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Key Properties

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CAS Number	66592-89-0
MW	179.67
Purity	>98% (HPLC)
Formula	C₅H₁₀ClN₃S
SMILES	C(CC#N)CSC(=N)N.Cl
Target	Glucokinase
Solubility	DMSO : ≥ 40 mg/mL; 222.63 mM

Bioactivity

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In Vivo

Animal model: A2780 xenograft tumor model in nude mice. 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. Dosage: 150 mg/kg. Administration: Intraperitoneal injection. Result: Prolonged the survival time of mice, and maintained 100% survival rate more over 35 days.

In Vitro

Cell Viability Assay 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, x1), 6 h + 66 h wo (x2), 6 h + 66 h wo (x3). Result: Only inhibited the cell viability of KASUMI-1 cells and decreased cells viability in a dose- and time-dependent manner. Apoptosis Analysis 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 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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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4-Isothioureidobutyronitrile hydrochloride

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Gene Symbol

Glucokinase

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