1215208-59-5
1215208-59-5 structure
- Name: MPT0B014
- Chemical Name: MPT0B014
- CAS Number: 1215208-59-5
- Molecular Formula: C19H17NO4
- Molecular Weight: 323.343
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2021-09-10 10:30:28
- Modify Date: 2024-01-08 23:47:41
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MPT0B014 is a tubulin polymerization inhibitor. MPT0B014 induces cancer cell apoptosis. MPT0B014 can be used for the research of cancer[1].
| Name | MPT0B014 |
|---|---|
| Synonyms |
Methanone, 6-quinolinyl(3,4,5-trimethoxyphenyl)-
MPT0B014 6-Quinolinyl(3,4,5-trimethoxyphenyl)methanone |
| Description | MPT0B014 is a tubulin polymerization inhibitor. MPT0B014 induces cancer cell apoptosis. MPT0B014 can be used for the research of cancer[1]. |
|---|---|
| Related Catalog | |
| Target |
Tubulin polymerization[1] |
| In Vitro | MPT0B014 (0-1 μM; 48 h) 以剂量依赖的方式抑制 A549、H1299 和 H226 细胞的生长[1]。 MPT0B014 (0.05-0.3 μM; 24 and 48 h) 在 A549 细胞中使细胞周期阻滞于 G2/M 期和 sub-G1 期，诱导细胞凋亡[1]。 Cell Viability Assay[1] Cell Line: A549, H1299, H226 and HUVEC cells Concentration: 0, 0.025, 0.05, 0.075 and 1 μM Incubation Time: 48 h Result: Inhibited cell viability with IC50s of 0.109±0.01, 0.055±0.004, 0.077±0.005 and 0.536±0.166 μM against A549, H1299, H226 and HUVEC cells, respectively. Cell Cycle Analysis[1] Cell Line: A549, H1299 and H226 Concentration: 0.05, 0.1 and 0.3 μM Incubation Time: 24 and 48 h Result: Treatment for 24 h led to notable accumulation of cells in the G2/M phase. At 48 h, sub-G1 apoptotic cell populations were increased in a concentration-dependent manner. Cells in the G2/M phase began to rise at 12 h post-treatment and peaked at 24 h. Following this, there was an emergence of cells in the sub-G1 population phase until 48 h. Western Blot Analysis[1] Cell Line: A549, H1299 and H226 Concentration: 0.05, 0.1 and 0.3 μM Incubation Time: 24 h Result: Resulted in a marked increase in expression of the mitosis marker MPM2 and the proteins cyclin B1, Cdc2, Thr161, Aurora A and Aurora B in a concentration-dependent manner. Decreased the expression of Cdc (Tyr15) and Cdc25C, whereas total protein levels of Cdc2 did not change. Apoptosis Analysis[1] Cell Line: A549 Concentration: 0.05, 0.075, 0.1 and 0.3 μM Incubation Time: 48 h Result: Induced apoptosis in a concentration-dependent manner. Western Blot Analysis[1] Cell Line: A549 Concentration: 0.05, 0.1 and 0.3 μM Incubation Time: 24, 36 and 48 h Result: Induced activation of caspases-3, -7, -8 and -9, and cleavage of PARP in a time- and concentration-dependent manner. Significantly induced Bcl-2 phosphorylation. Down-regulated Mcl-1 expression in a concentration-dependent manner. |
| In Vivo | MPT0B014 (100 mg/kg; i.v./i.p.; daily for 25 days) 和 25 mg/kg Erlotinib (HY-50896) 联用显著改善小鼠 A549 肿瘤抑制[1]。 Animal Model: Nude athymic mice, A549 xenografts[1] Dosage: 100 mg/kg alone or in combination with 25 mg/kg Erlotinib (HY-50896) Administration: i.v./i.p., daily for 25 days Result: The combined treatment resulted in more significant tumor growth delay (28%) compared with treatment alone (7%). The combination produced significantly higher anti-tumor activity. The growth of A549 cancer cell xenografts was suppressed by 11, 21 and 49% (tumor growth inhibition) after treatment with MPT0B014, Erlotinib and MPT0B014 plus Erlotinib, respectively. |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 513.5±50.0 °C at 760 mmHg |
| Molecular Formula | C19H17NO4 |
| Molecular Weight | 323.343 |
| Flash Point | 264.4±30.1 °C |
| Exact Mass | 323.115753 |
| LogP | 3.17 |
| Vapour Pressure | 0.0±1.3 mmHg at 25°C |
| Index of Refraction | 1.606 |
| Storage condition | 2-8°C |
| Symbol |
GHS06 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H301 |
| Precautionary Statements | P301 + P310 |
| Hazard Codes | T+ |
| RIDADR | UN 2811 6.1 / PGIII |