MPT0B392

Modify Date: 2024-01-10 16:48:28

MPT0B392 Structure
MPT0B392 structure
Common Name MPT0B392
CAS Number 1346169-92-3 Molecular Weight 404.44
Density N/A Boiling Point N/A
Molecular Formula C19H20N2O6S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of MPT0B392


MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis[1].

 Names

Name MPT0B392

 MPT0B392 Biological Activity

Description MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis[1].
Related Catalog
Target

JNK and apoptosis[1]

In Vitro MPT0B392 (B392) (0.001-0.1 μM; 24 and 48 hours) inhibits the cell viability of HL60, MOLT-4, and CCRF-CEM cells with IC50s of 0.02 μM, 0.03 μM and 0.02 μM, respectively[1]. MPT0B392 (0.1 μM; 48 hours) induces apoptosis in HL60 cancer cells[1]. MPT0B392 (0.1 μM for 6-48 hours; 0.01-0.1 μM for 24 and 48 hours) triggers cells arrest in the G2/M phase, followed by accumulation in subG1 phase in a concentration and time-dependent manner[1]. MPT0B392 (0.1 μM; 48 hours) increases the phosphorylation of Bcl-2, Mcl-1S and decreased in Mcl-1L[1]. Cell Viability Assay[1] Cell Line: HL60 (acute promyelocytic leukemia), MOLT-4 (acute lymphoblastic leukemia), CCRF-CEM (acute lymphoblastic leukemia) cells Concentration: 0.001, 0.003, 0.01, 0.03, 0.1 μM Incubation Time: 24 and 48 hours Result: Inhibited the cell viability. Apoptosis Analysis[1] Cell Line: HL60 cells Concentration: 0.1 μM Incubation Time: 48 hours Result: Induced apoptosis in cancer cells. Cell Cycle Analysis[1] Cell Line: HL60 cells Concentration: 0.1 μM or 0.01, 0.03, 0.1 μM Incubation Time: 0.1 μM for 6-48 hours; 0.01-0.1 μM for 24 and 48 hours Result: Triggered cells arrest in the G2/M phase, followed by accumulation in subG1 phase in a concentration and time-dependent manner. Western Blot Analysis[1] Cell Line: HL60 cells Concentration: 0.1 μM Incubation Time: 48 hours Result: Increased the phosphorylation of Bcl-2, Mcl-1S and decreased in Mcl-1L.
In Vivo The effects of MPT0B392 (oral gavage; 50 mg/kg or 100 mg/kg for 12 or 14 days) shows relative potent anti-leukemia activity in a vivo xenograft model[1]. Animal Model: Severe combined immunodeficient (SCID) mice [1] Dosage: 50 mg/kg or 100 mg/kg Administration: Oral gavage; 12 or 14 days Result: Resulted in significant tumor growth delay (83.3%) and tumor volume inhibition without loss of body weight.
References

[1]. Chao MW, et al. An oral quinoline derivative, MPT0B392, causes leukemic cells mitotic arrest and overcomes drug resistant cancer cells. Oncotarget. 2017 Apr,8(17):27772-27785.

 Chemical & Physical Properties

Molecular Formula C19H20N2O6S
Molecular Weight 404.44
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