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PHA-793887

Catalog No. T2113 CAS 718630-59-2

Synonyms: PHA 793887, PHA793887

PHA-793887 has been used in trials studying the treatment of Advanced/Metastatic Solid Tumors.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

PHA-793887, CAS 718630-59-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 45.00
2 mg	In stock	$ 64.00
5 mg	In stock	$ 107.00
10 mg	In stock	$ 162.00
25 mg	In stock	$ 325.00
50 mg	In stock	$ 556.00
100 mg	In stock	$ 783.00
500 mg	In stock	$ 1,650.00
1 mL * 10 mM (in DMSO)	In stock	$ 108.00

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Purity: 100%

Purity: 99.19%

Purity: 98.02%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PHA-793887 has been used in trials studying the treatment of Advanced/Metastatic Solid Tumors.
Targets&IC50	CDK5-p25:5 nM, CDK2-CyclinE:8 nM, CDK7-CyclinH:10 nM, CDK2-CyclinA:8 nM, CDK1-CyclinB:60 nM
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.
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.
Kinase Assay	CDK Kinase Assay: The biochemical activity of compounds is determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylated product. PHA-793887 (1.5 nM–10 μM) is incubated for 30?90 min at room temperature in the presence of ATP/33P-γ-ATP mix, substrate, and the specific enzyme (0.7?100 nM) in a final volume of 30 μL of kinase buffer, using 96 U bottom plates. After incubation, the reaction is stopped and the phosphorylated substrate is separated from nonincorporated radioactive ATP using SPA beads, Dowex resin, or Multiscreen phosphocellulose filter as follows: (1) For SPA Assays. The reaction is stopped by the addition of 100 μL of PBS + 32 mM EDTA + 0.1% Triton X-100 + 500 μM ATP, containing 1 mg of streptavidin-coated SPA beads. After 20 min of incubation for substrate capture, 100 μL of the reaction mixture is transferred into Optiplate 96-well plates containing 100 μL of 5 M CsCl, left to stand for 4 hours to allow stratification of beads to the top of the plate, and counted using TopCount to measure substrate-incorporated phosphate. (2) For Dowex Resin Assay. An amount of 150 μL of resin/formate, pH 3.00, is added to stop the reaction and capture unreacted 33P-γ-ATP, separating it from the phosphorylated substrate in solution. After 60 min of rest, 50 μL of supernatant is transferred to Optiplate 96-well plates. After the additon of 150 μL of Microscint 40, the radioactivity is counted in the TopCount. (3) For Multiscreen Assay. The reaction is stopped with the addition of 10 μL of EDTA (150 mM). An amount of 100 μL is transferred to a MultiScreen plate to allow substrate binding to phosphocellulose filter. Plates are then washed three times with 100 μL of H2PO4 (75 mM) filtered by a MultiScreen filtration system, and dried. After the additon of 100 μL of Microscint 0, radioactivity is counted in the TopCount. IC50 values are obtained by nonlinear regression analysis.
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)

Synonyms	PHA 793887, PHA793887
Molecular Weight	361.48
Formula	C19H31N5O2
CAS No.	718630-59-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 67 mg/mL (185.3 mM)

DMSO: 67 mg/mL (185.3 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Brasca MG, et al. Bioorg Med Chem, 2010, 18(5), 1844-1853. 2. Alzani R, et al. Exp Hematol, 2010, 38(4), 259-269. 3. Pevarello P, et al. J Med Chem, 2004, 47(13), 3367-3380. 4. Ou J, Li H, Qiu P, et al. CDK9 modulates circadian clock by attenuating REV-ERBα activity[J]. Biochemical and biophysical research communications. 2019 Jun 11;513(4):967-973.

Citations

1. Ou J, Li H, Qiu P, et al. CDK9 modulates circadian clock by attenuating REV-ERBα activity. Biochemical and Biophysical Research Communications. 2019 Jun 11;513(4):967-973

Related compound libraries

This product is contained In the following compound libraries：

Cell Cycle Compound Library Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library ReFRAME Related Library Apoptosis Compound Library Anti-Pancreatic Cancer Compound Library Clinical Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PHA-793887 718630-59-2 Apoptosis Cell Cycle/Checkpoint CDK PHA 793887 Inhibitor inhibit PHA793887 Cyclin dependent kinase inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.