[CAS NO. 1190277-80-5] MKI-1

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

Overview

MDL	-
Molecular Weight	302.33
Molecular Formula	C18H14N4O
SMILES	O=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.

References

[1] Ah-Young Kim, et al. MKI-1, a Novel Small-Molecule Inhibitor of MASTL, Exerts Antitumor and Radiosensitizer Activities Through PP2A Activation in Breast cancer. Front Oncol. 2020 Sep 29;10:571601.

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