MBM-55

Research use only, not for human use.

MBM-55 is an effective inhibitor of NIMA related kinase 2 (NEK2) with an IC50 of 1 nM. MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis.

MBM-55 is an effective inhibitor of NIMA related kinase 2 (NEK2) with an IC50 of 1 nM. MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis.(In Vitro):MBM-55 (0.5-1 μM; 24 hours) induces G2/M phase arrest and accumulation of cells with >4N content in HCT-116 cells. MBM-55 (0.5-1 μM; 24 hours) causes cell apoptosis in a concentration-dependent manner in HCT-116 cells.MBM-55 inhibits MGC-803, HCT-116, Bel-7402 cells proliferation with IC50s of 0.53, 0.84, 7.13 μM, respectively.(In Vivo):In female BALB/c nu/nu mice bearing HCT-116 xenografts, MBM-55 (20 mg/kg; i.p.) exhibits good antitumor activity and a well-tolerated dose schedule. MBM-55 (1.0 mg/kg; i.v.) shows the CL, Vss, T1/2, AUC0-t, and AUC0-∞ values of 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, 495 ng/h/mL and 507 ng/h/mL, respectively.

Cell Cycle Analysis Cell Line:HCT-116 cells Concentration:0.5, 1 μM Incubation Time:24 hours Result:Induced G2/M phase arrest and accumulation of cells with >4N content.Apoptosis Analysis Cell Line:HCT-116 cells Concentration:0.5, 1 μM Incubation Time:24 hours Result:Caused cell apoptosis in a concentration-dependent manner.

Animal Model:Female BALB/c nu/nu mice (5-6 weeks, bearing HCT-116 xenografts) Dosage:20 mg/kg Administration:Intraperitoneal injection; twice a day for 21 days Result:Significantly suppressed tumor growth.Animal Model:Male Sprague Dawley (SD) rats Dosage:1.0 mg/kg Administration:IV injection (Pharmacokinetic Analysis)Result:The CL, Vss, T1/2, AUC0-t, and AUC0-∞ values were 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, 495 ng/h/mL and 507 ng/h/mL, respectively.

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PI3K/Akt/mTOR signaling

GSK-3

AChE

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2083622-09-5

498.562

C28H27FN6O2

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (250.73 mM)

CN(C)CCn1cc(cn1)-c1ccn2c(cnc2c1)-c1ccc(C(N)=O)c(OCc2cccc(F)c2)c1

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(-20℃)

With Ice Pack

≥ 2 years