PHA-793887

SKU: orb1306453

Description

PHA-793887 is a small molecule inhibitor investigated in clinical trials for advanced or metastatic solid tumors. It has been utilized in preclinical research to study its effects on cell cycle progression and antitumor activity in both cellular and animal models.

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 718630-59-2
• MW: 361.48
• Purity: >99.99% (May vary between batches)
• Formula: C₁₉H₃₁N₅O₂
• SMILES: CC(C)CC(=O)Nc1n[nH]c2c1CN(C(=O)C1CCN(C)CC1)C2(C)C
• Target: CDK,Apoptosis
• Solubility: Ethanol:67 mg/mL (185.35 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:55 mg/mL (152.15 mM);10% DMSO+90% Saline:2.5 mg/mL (6.92 mM)

Bioactivity

• Target IC50:
  CDK2-CyclinE:8 nM|CDK5-p25:5 nM|CDK7-CyclinH:10 nM|CDK2-CyclinA:8 nM|GSK-3β:79 nM|CDK1-CyclinB:60 nM|CDK9-CyclinT1:138 nM|Cdk4-CyclinD1:62 nM
• In Vivo:
  PHA-793887 induces cell cycle arrest and inhibits Rb protein and nuclear phosphorylation at concentrations ranging from 0.2-1 μM, while also regulating the expression of cyclin E and cdc6. At 5 μM, it prompts apoptosis. This compound displays cytotoxicity towards leukemia cell lines (including K562, KU812, KCL22, and TOM1) with an IC50 of 0.3-7 μM, yet it shows no cytotoxic effects on normal, unstimulated peripheral blood mononuclear cells or CD34+ hematopoietic stem cells. PHA-793887 exhibits high activity against leukemia cell lines with an IC50 of <0.1 μM. Furthermore, PHA-793887 inhibits the proliferation of several tumor cell lines (including A2780, HCT-116, COLO-205, C-433, DU-145, A375, PC3, MCF-7, and BX-PC3) with IC50 values ranging from 88 nM to 3.4 μM.
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• In Vitro:
  PHA-793887, at a dosage of 20 mg/kg, has been demonstrated to be effective in treating transplant tumor models carrying K562 and HL60 cells, primary leukemia dissemination cell models, and high-burden disseminated ALL-2 models in relapsed Philadelphia-positive acute lymphoblastic leukemia patients. Additionally, PHA-793887 (administered at doses ranging from 10-30 mg/kg) exhibits good efficacy in xenograft models of human ovarian A2780, colon HCT-116, and pancreatic BX-PC3 cancers.
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• Cell Research:
  Cells are seeded into 96- or 384-wells plates at final concentration ranging from 1 × 104 to 3 × 104 per cm2. After 24 hours, cells are treated using serial dilution of PHA-793887. At 72 hours after the treatment, the amount of cells are evaluated using the CellTiter-Glo assay. IC50 values are calculated using a sygmoidal fitt(Only for Reference)
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Storage & Handling

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

Alternative Names

Inhibitor, inhibit, Apoptosis, CDK, CDK2/CyclinA, CDK2/CyclinE, CDK1/CyclinB, CDK7/CyclinH, CDK5/p25, Cyclin dependent kinase, PHA793887, PHA-793887, PHA 793887

Compound Identifiers

PubChem CID

46191454