[CAS NO. 1179347-65-9] MT 63-78
PRODUCTS SPECIFICATIONS [1179347-65-9]
DESCRIPTION [1179347-65-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 326.35 |
| Molecular Formula | C21H14N2O2 |
| SMILES | N#CC1=CNC2=C1C=C(C3=CC=C(C4=C(O)C=CC=C4O)C=C3)C=C2 |
Summary
IC50 & Target
|
AMPK 25 μM (EC 50 ) |
mTORC1
|
In Vitro
MT 63-78 (0-50 μM; 4 days; LNCaP and PC3 cells) treatment shows a dose-dependent decrease in cell number, and concomitant to the activation of AMPK signaling
[1]
.
MT 63-78 (25 μM; 24 hours; LNCaP and CRPC cells) treatment induces a significant enrichement in the G2/M population
[1]
.
MT 63-78 (0-50 μM; 24 hours; LNCaP, PC3, C4-4, C4-2B, CL1and 22RV1cells) treatment induces reduction of anti-apoptotic Mcl-1 in concert with accumulation of the pro-apoptotic BH3-only protein Puma
[1]
.
MT 63-78 (0-50 μM; 30 minutes; LNCaP and PC3 cells) treatment shows a dose-dependent phosphorylation of the two major AMPK targets Acetyl-CoA Carboxylase (ACC) on Ser79 and of Raptor on Ser792. And also increases Thr172 phosphorylation on the AMPK α subunit
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | LNCaP and PC3 cells |
| Concentration: | 0 μM, 1 μM, 5 μM, 10 μM, 25 μM, 50 μM |
| Incubation Time: | 4 days |
| Result: | A dose-dependent decrease in cell number, concomitant to the activation of AMPK signaling was observed. |
Cell Cycle Analysis [1]
| Cell Line: | LNCaP and CRPC cells |
| Concentration: | 25 μM |
| Incubation Time: | 24 hours |
| Result: | Induced a significant enrichement in the G2/M population in both androgen sensitive and CRPC cell models. |
Apoptosis Analysis [1]
| Cell Line: | LNCaP, PC3, C4-4, C4-2B, CL1and 22RV1cells |
| Concentration: | 0 μM, 10 μM, 25 μM, 50 μM |
| Incubation Time: | 24 hours |
| Result: | Induced reduction of anti-apoptotic Mcl-1 in concert with accumulation of the pro-apoptotic BH3-only protein Puma in all PCa cells. |
Western Blot Analysis [1]
| Cell Line: | LNCaP and PC3 cells |
| Concentration: | 0 μM, 0.25 μM, 0.5 μM, 1 μM, 5 μM, 25 μM, 50 μM |
| Incubation Time: | 30 minutes |
| Result: | Observed a dose-dependent phosphorylation of the two major AMPK targets Acetyl-CoA Carboxylase (ACC) on Ser79 and of Raptor on Ser792. A corresponding increase in Thr172 phosphorylation on the AMPK α subunit was also observed. |
In Vivo
MT 63-78 (30 mg/kg; intraperitoneal injection; daily; for 14 days; C57 BL/6 male mice) treatment leads to a 33% inhibition of tumor growth [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | C57 BL/6 male mice bearing LNCaP tumors [1] |
| Dosage: | 30 mg/kg |
| Administration: | Intraperitoneal injection; daily; for 14 days |
| Result: | Led to a 33% inhibition of tumor growth. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 125 mg/mL ( 383.02 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.0642 mL | 15.3210 mL | 30.6419 mL |
| 5 mM | 0.6128 mL | 3.0642 mL | 6.1284 mL |
| 10 mM | 0.3064 mL | 1.5321 mL | 3.0642 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (6.37 mM); Clear solution