MBM-55S

SKU: orb1709183

Description

MBM-55S

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2083624-07-9
• MW: 734.73
• Purity: 98.38% (May vary between batches)
• Formula: C₃₆H₃₉FN₆O₁₀
• 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
• Target: CDK,Bcr-Abl,MAPK,GSK-3,DYRK,Akt,Aurora Kinase,Apoptosis,S6 Kinase
• Solubility: DMSO:22.5 mg/mL (30.62 mM)

Bioactivity

• Target IC50:
  DYRK1A:6.5 nM |Chk1:57 nM |Aurora A:5300 nM |CDK4:441nM |CDK2:370 nM |Abl:20 nM |NEK2:1 nM |GSK-3β:91 nM |Akt1:608 nM |RSK1:5.4 nM
• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CDK2, CDK4, CHK1, DYRK1a, AuroraKinase, Aurora Kinase, Aurora A, BcrAbl, AKT1, ABL, MBM 55S, MBM55S, MBM-55S, GSK-3β, GSK3, Nek2, S6 Kinase, S6Kinase, RSK1

Compound Identifiers

PubChem CID

137639660