Kevetrin hydrochloride

Research use only, not for human use.

Kevetrin hydrochloride is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.

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.

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,×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 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 AnalysisCell 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.

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.

4-Isothioureidobutyronitrile hydrochloride

Cytoskeleton/Cell Adhesion Molecules

Glucokinase

Mdm2| p53

Cancer

——

66592-89-0

179.67

C5H10ClN3S

>98% (HPLC)

DMSO : ≥ 40 mg/mL; 222.63 mM

C(CC#N)CSC(=N)N.Cl

——

(-20℃)

With Ice Pack

≥ 2 years