Description
MKI-1, an inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC50 of 9.9 μM, exerts antitumor and radiosensitizer activities through PP2A activation in breast cancer.
Product information
CAS Number: 1190277-80-5
Molecular Weight: 302.33
Formula: C18H14N4O
Chemical Name: N-(1H-1,3-benzodiazol-2-yl)-3-(1H-pyrrol-1-yl)benzamide
Smiles: O=C(NC1NC2=CC=CC=C2N=1)C1=CC(=CC=C1)N1C=CC=C1
InChiKey: XKDZPQAMBMLCDQ-UHFFFAOYSA-N
InChi: InChI=1S/C18H14N4O/c23-17(21-18-19-15-8-1-2-9-16(15)20-18)13-6-5-7-14(12-13)22-10-3-4-11-22/h1-12H,(H2,19,20,21,23)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 250 mg/mL (826.91 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
MKI-1 (5-20 μM) inhibits the activity of MASTL in breast cancer cells. 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. MKI-1 clearly reduces both serine 62-phosphorylation of c-Myc and total c-Myc, with a decrease in ENSA phosphorylation. MKI-1 (20 μM, 16 h) reduces c-Myc stability through PP2A activation in MCF7 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.
Products are for research use only. Not for human use.
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