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MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $195 | In Stock | |
2 mg | $293 | In Stock | |
5 mg | $449 | In Stock | |
10 mg | $659 | In Stock | |
25 mg | $987 | In Stock | |
50 mg | $1,390 | In Stock | |
100 mg | $1,880 | In Stock | |
500 mg | $3,780 | In Stock | |
1 mL x 10 mM (in DMSO) | $663 | In Stock |
Description | MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities. |
Targets&IC50 | NEK2:1 nM , CDK2:370 nM , Akt1:608 nM , RSK1:5.4 nM , GSK-3β:91 nM , DYRK1A:6.5 nM , Aurora A:5300 nM , Chk1:57 nM , CDK4:441nM , Abl:20 nM |
In vitro | MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 and DYRK1a with IC50s of 5.4 and 6.5 nM. MBM-55S inhibits MGC-803, HCT-116, and Bel-7402 the proliferation of cell with IC50s of 0.53, 0.84, and 7.13 μM, respectively. MBM-55S (0.5-1 μM) induces G2/M phase arrest and accumulation of cells with >4N content and causes cell apoptosis in a concentration-dependent manner in HCT-116 cells[1]. |
In vivo | In female BALB/c nu/nu mice, MBM-55S (20 mg/kg; i.p) exhibits good antitumor activity. In male Sprague Dawley rats, MBM-55S (1.0 mg/kg; i.v.) shows good pharmacokinetic profile with the CL, T1/2, Vss, AUC0-t, and AUC0-∞ values of 33.3 mL/min/kg, 1.72 hours, 2.53 L/kg, 495 ng/h/mL and 507 ng/h/mL, respectively[1]. |
Molecular Weight | 734.73 |
Formula | C36H39FN6O10 |
Cas No. | 2083624-07-9 |
Smiles | O=C(CCC(O)=O)O.O=C(C1=C(OCC2=CC(F)=CC=C2)C=C(C3=CN=C4C=C(C5=CN(CCN(C)C)N=C5)C=CN43)C=C1)N.O=C(CCC(O)=O)O |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 22.5 mg/mL (30.62 mM) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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