Description
MBM-17S is a potent NIMA-related kinase 2 (Nek2) inhibitor, with an IC50 of 3 nM. MBM-17S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-17S shows antitumor activities, and no obvious toxicity to mice.
Product information
CAS Number: 2083621-91-2
Molecular Weight: 716.74
Formula: C36H40N6O10
Chemical Name: 2-(benzyloxy)-4-(7-{1-[2-(dimethylamino)ethyl]-1H-pyrazol-4-yl}imidazo[1,2-a]pyridin-3-yl)benzamide; bis(butanedioic acid)
Smiles: CN(C)CCN1C=C(C=N1)C1=CC2=NC=C(C3=CC(OCC4C=CC=CC=4)=C(C=C3)C(N)=O)N2C=C1.OC(=O)CCC(O)=O.OC(=O)CCC(O)=O
InChiKey: PCGUADBRTABDRN-UHFFFAOYSA-N
InChi: InChI=1S/C28H28N6O2.2C4H6O4/c1-32(2)12-13-33-18-23(16-31-33)21-10-11-34-25(17-30-27(34)15-21)22-8-9-24(28(29)35)26(14-22)36-19-20-6-4-3-5-7-20;2*5-3(6)1-2-4(7)8/h3-11,14-18H,12-13,19H2,1-2H3,(H2,29,35);2*1-2H2,(H,5,6)(H,7,8)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
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:
MBM-17S inhibits MGC-803, HCT-116, and Bel-7402 cells proliferation with IC50s of 0.48, 1.06, and 4.53 μM, respectively. MBM-17S (0.25-1.0 μM; 24 hours) induced G2/M phase arrest and accumulation of cells with >4N content. MBM-17S (0.5-1.0 μM; 24 hours) triggers apoptosis of cancer cells.
In Vivo:
MBM-17S (20 mg/kg; i.p.; twice a day for 21 days) exhibits good antitumor activity and a well-tolerated dose schedule. MBM-17S (1.0 mg/kg; i.v.) treatment shows CL, Vss, T1/2, AUC0-t, and AUC0-∞ values of 42.4 mL/min/kg, 4.06 L/kg, 2.42 hours, 386 ng/h/mL, and 405 ng/h/mL, respectively.
Products are for research use only. Not for human use.
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