[CAS NO. 1190277-80-5]  MKI-1

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PRODUCTS SPECIFICATIONS [1190277-80-5]

Catalog
HY-137552
Brand
MCE
CAS
1190277-80-5

DESCRIPTION [1190277-80-5]

Overview

MDL-
Molecular Weight302.33
Molecular FormulaC18H14N4O
SMILESO=C(NC1=NC2=CC=CC=C2N1)C3=CC=CC(N4C=CC=C4)=C3

For research use only. We do not sell to patients.

Summary

MKI-1, an inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC 50 of 9.9 μM, exerts antitumor and radiosensitizer activities through PP2A activation in breast cancer [1] .


In Vitro

MKI-1 (5-20 μM) inhibits the activity of MASTL in breast cancer cells [1] .
MKI-1 (100 μM, 72 h) inhibits various oncogenic properties of breast cancer cells but showed much weaker effects on the viability of normal breast cells [1] .
MKI-1 clearly reduces both serine 62-phosphorylation of c-Myc and total c-Myc, with a decrease in ENSA phosphorylation [1] .
MKI-1 (20 μM, 16 h) reduces c-Myc stability through PP2A activation in MCF7 cells [1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis [1]

Cell Line: MCF7 and T47D cells.
Concentration: 5-20 μM.
Incubation Time: 24 h.
Result: Inhibited the phosphorylation of ENSA in MCF7 and T47D cells.
Significantly inhibited the phosphorylation of ENSA in mitotic cells.

In Vivo

MKI-1 (50 mg/kg, ip, twice a week) reduces tumor growth and enhances the radiosensitivity of BT549 xenograft model in response to 6 Gy irradiation compared with the control group, with no notable changes in body weight, suggesting the absence of gross toxicity in the treated mice [1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Five-week-old female BALB/c nude mice (BT549 cells) [1] .
Dosage: 50 mg/kg.
Administration: Twice per week by intraperitoneal (i.p.) injection.
Result: Reduced tumor growth.

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

In Vitro:

DMSO : 250 mg/mL ( 826.91 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3076 mL 16.5382 mL 33.0764 mL
5 mM 0.6615 mL 3.3076 mL 6.6153 mL
10 mM 0.3308 mL 1.6538 mL 3.3076 mL
* Please refer to the solubility information to select the appropriate solvent.