[CAS NO. 681282-09-7] MYCMI-6
PRODUCTS SPECIFICATIONS [681282-09-7]
DESCRIPTION [681282-09-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 373.41 |
| Molecular Formula | C20H19N7O |
| SMILES | NC1=NC(N)=CC=C1/N=N/C2=CC3=NC4=CC=C(OCC)C=C4C(N)=C3C=C2 |
Summary
MYCMI-6 (NSC354961) is a potent and selective endogenous MYC:MAX protein interactions inhibitor. MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with a K d of 1.6 μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner (IC 50 <0.5 μM). MYCMI-6 is not cytotoxic to normal human cells. MYCMI-6 induces apoptosis [1] .
In Vitro
MYCMI-6 (NSC354961) (6.25 μM; 48 hours) selectively suppresses MYC-driven tumor cell growth with high efficacy
[1]
.
MYCMI-6 significantly inhibits growth of Burkitt’s lymphoma cells (Mutu, Daudi and ST486) - another classical example of a MYC-driven tumor, having translocations of
MYC
to one of the immunoglobulin loci - in a dose-dependent manner with an average GI
50
of 0.5 μM. Treatment of MCF7 cells with the MYCMI-6 for 24 hours significantly decreased MYC:MAX isPLA signals to 7%. Titration showed an IC
50
for inhibition of MYC:MAX of less than 1.5 μM for MYCMI-6 by isPLA. MYCMI-6 inhibits the MYC:MAX heterodimer formation with an IC
50
of 3.8 μM. MYCMI-6 efficiently inhibits anchorage-independent growth of
MYCN
-amplified neuroblastoma cells with GI
50
values of <0.4 μM
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | MYCN -amplified neuroblastoma cells (IMR-32, Kelly and SK-N-DZ), MYCN -non-amplified neuroblastoma cells (SK-N-F1, SK-N-AS and SK-N-RA) |
| Concentration: | 6.25 μM |
| Incubation Time: | 48 hours |
| Result: | Reduced growth of the MYCN -amplified cell lines significantly stronger than the MYCN -non-amplified cell lines. |
In Vivo
MYCMI-6 (20 mg/kg; i.p.; daily for 1-2 weeks) induces massive apoptosis and reduces tumor cell proliferation, tumor microvasculature density and MYC:MAX interaction in a MYC-dependent xenograft tumor model [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | 6-8 weeks old athymic nude mice (bearing MYCN-amplified SK-N-DZ neuroblastoma cells) [1] |
| Dosage: | 20 mg/kg body weight |
| Administration: | I.p.; daily for 1-2 weeks |
| Result: | A dramatic increase in the extension of apoptotic areas in the tumors and a significant increase in non-proliferative areas as determined by Ki67 staining in tumors. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 2.4 mg/mL ( 6.43 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.6780 mL | 13.3901 mL | 26.7802 mL |
| 5 mM | 0.5356 mL | 2.6780 mL | 5.3560 mL |
| 10 mM | --- | --- | --- |