SCH900776 (S-isomer)

SKU: orb1303875

Description

SCH900776 S-isomer (MK-8776 S-isomer) is a potent, selective, and orally active Chk1 inhibitor with an IC50 of 3 nM, showing weaker activity against Chk2 and CDK2. It is widely used in cancer research to study DNA damage response and has demonstrated chemosensitizing effects in various preclinical in vitro and in vivo models.

Research Area

Cell Biology

Key Properties

• CAS Number: 891494-64-7
• MW: 376.25
• Purity: 99.95% (May vary between batches)
• Formula: C₁₅H₁₈BrN₇
• SMILES: Cn1cc(cn1)-c1cnn2c(N)c(Br)c(nc12)[C@H]1CCCNC1
• Target: Others,CDK,Chk
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (10.63 mM);DMSO:100 mg/mL (265.78 mM)

Bioactivity

• Target IC50:
  Chk1:3 nM|CDK2:160 nM|Chk2:1500 nM
• In Vivo:
  After pretreatment 30 minutes with gemcitabine, SCH 900776 (4 mg/kg) is sufficient to induce the γ-H2AX biomarker while 8 mg/kg leads to enhanced tumor pharmacodynamic and regression responses relative to gemcitabine or SCH 900776 alone. SCH 900776 (16/32 mg/kg) dose-dependently induces improvements in tumor response. Doses of SCH 900776 associate with robust biomarker activation and improved tumor response are not associated with enhanced toxicity of gemcitabine on hematological parameters in BALB/c mice.
• In Vitro:
  SCH 900776 does not significantly inhibit HLMs CYP450 isoforms 1A2, 2C9, 2C19, 2D6, and 3A4. SCH 900776 induces a dose-dependent loss of DNA replication capability 24 hours after hydroxyurea exposure. In combination with an antimetabolite, SCH 900776 induces accumulation of γ-H2AX within 2 hours, indicative of replication fork collapse and double-stranded DNA breaks. SCH 900776 also dose-dependently suppresses accumulation of the Chk1 pS296 autophosphorylation.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CDK2, Chk1, Chk2, Inhibitor, MK-8776 S-isomer, inhibit, SCH900776, SCH-900776, SCH900776 (S isomer), SCH900776 (Sisomer), SCH-900776 (S-isomer), SCH900776 (S-isomer), SCH900776 S-isomer, SCH 900776, S-isomer

Compound Identifiers

PubChem CID

46239014