PHA-793887

Catalog No.S1487

PHA-793887 Chemical Structure

Molecular Weight(MW): 361.48

PHA-793887 is a novel and potent inhibitor of CDK2, CDK5 and CDK7 with IC50 of 8 nM, 5 nM and 10 nM. It is greater than 6-fold more selective for CDK2, 5, and 7 than CDK1, 4, and 9. Phase 1.

Size Price Stock Quantity  
In DMSO USD 250 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

2 Customer Reviews

  • J558 cells were treated with PHA793887 (0.02–5 umol/L) for 6 hours, after which Western blot analysis was performed to monitor XBP-1s expression. Tub, tubulin.

    Mol Cancer Ther 2014 13(3), 662-74. PHA-793887 purchased from Selleck.

    PHA-793887 purchased from Selleck.

Purity & Quality Control

Choose Selective CDK Inhibitors

Biological Activity

Description PHA-793887 is a novel and potent inhibitor of CDK2, CDK5 and CDK7 with IC50 of 8 nM, 5 nM and 10 nM. It is greater than 6-fold more selective for CDK2, 5, and 7 than CDK1, 4, and 9. Phase 1.
Features Multi-CDK inhibitor.
Targets
CDK5/p25 [1]
(Cell-free assay)
CDK2/CyclinA [1]
(Cell-free assay)
CDK2/CyclinE [1]
(Cell-free assay)
CDK7/CyclinH [1]
(Cell-free assay)
CDK1/CyclinB [1]
(Cell-free assay)
5 nM 8 nM 8 nM 10 nM 60 nM
In vitro

PHA-793887 has low activity against CDK1, CDK4, CDK9 and GSK3β with IC50 of 60 nM, 62 nM, 138 nM and 79 nM, respectively. PHA-793887 inhibits cell proliferation of many tumor cell lines, including A2780, HCT-116, COLO-205, C-433, DU-145, A375, PC3, MCF-7, and BX-PC3, with IC50 of 88 nM–3.4 μM. PHA-793887 (1 μM) shows a decrease in the S phase, a subsequent increase of the G1 phase and a slight accumulation of G2/M phase in A2780 cells. PHA-793887 (3 μM) significantly increases G2/M phase and reduces DNA synthsis. [1] PHA-793887 is cytotoxic for leukemic cell lines, including K562, KU812, KCL22, and TOM1, with IC50 of 0.3–7 μM, but it is not cytotoxic for normal unstimulated peripheral blood mononuclear cells or CD34+ hematopoietic stem cells. In colony assays, PHA-793887 shows very high activity against leukemia cell lines with IC50 less than 0.1 μM. PHA-793887 induces cell-cycle arrest, inhibits Rb and nucleophosmin phosphorylation, and modulates cyclin E and cdc6 expression at 0.2−1 μM and induces apoptosis at 5 μM. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human A2780 cells MoL0VJJwdGmoZYLheIlwdiCjc4PhfS=> MVy3NkBp NWjSRmp[SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bi\nSncjC3NkBpenNiYomg[ox2d3Knc3PlcoNmKGG|c3H5MEBKSzVyPUCuNFkh|ryP NI\BW4UzODF3M{KwOC=>
human HCT116 cells M3vrNHBzd2yrZnXyZZRqd25iYYPzZZk> Mnr1O|IhcA>? NI\vdphCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNVY{KM7:TR?= NIW5d4czODF3M{KwOC=>
human COLO205 cells NIKzO5JRem:uaX\ldoF1cW:wIHHzd4F6 M13EVFczKGh? NVKybGVmSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDU2xQOjB3IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4yQDhizszN NYHlfXFqOjBzNUOyNFQ>
human C-433 cells MYjQdo9tcW[ncnH0bY9vKGG|c3H5 NW[0WJJ2PzJiaB?= NYLtOVZwSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDMVQ{OyClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNlg2KM7:TR?= M1rndVIxOTV|MkC0
human DU145 cells M3;zZ3Bzd2yrZnXyZZRqd25iYYPzZZk> MoLaO|IhcA>? NWX4WmRpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuN|A{KM7:TR?= NGPjSm8zODF3M{KwOC=>
human A375 cells NV7TfpJWWHKxbHnm[ZJifGmxbjDhd5NigQ>? NELKOoI4OiCq MYrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF|N{WgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjN7NjFOwG0> MX:yNFE2OzJyNB?=
human PC3 cells NYXMS5VCWHKxbHnm[ZJifGmxbjDhd5NigQ>? NWS4eY5IPzJiaB?= NHnlNZVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDDN{Bk\WyuczDh[pRmeiB5MjDodpMh[nliU2LCJIF{e2G7LDDJR|UxRTBwNkCxJO69VQ>? MkPLNlAyPTN{MES=
human MCF7 cells NEDhTWdRem:uaX\ldoF1cW:wIHHzd4F6 Mo\hO|IhcA>? M13CRWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiB5MjDodpMh[nliU2LCJIF{e2G7LDDJR|UxRTFwMki0JO69VQ>? MoXmNlAyPTN{MES=
human BxPC3 cells NFP0UnZRem:uaX\ldoF1cW:wIHHzd4F6 M{HablczKGh? MV;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEK6UFOzJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFnDOVA:Oy52NESg{txO MoC4NlAyPTN{MES=
human A2780 cells MYnGeY5kfGmxbjDhd5NigQ>? MVezJO69VQ>? NYH2c4c{UW6qaXLpeIlwdiCxZjDDSGshcW5iaIXtZY4hSTJ5OECgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKG:oIHj5dI9xcG:|cHjvdplt[XSnZDDmc5JuKG:oIILleIlvd2KuYYP0c41iKHC{b4TlbY4h[XRiMzD1UUBjgSCrbX31co9pcXO2b3Po[Y1qe3S{eR?= NGPsdZQzODF3M{KwOC=>

... Click to View More Cell Line Experimental Data

In vivo PHA-793887 (10–30 mg/kg) shows good efficacy in the human ovarian A2780, colon HCT-116, and pancreatic BX-PC3 carcinoma xenograft models. [1] PHA-793887 (20 mg/kg) is effective in xenograft models of K562 and HL60 cells, primary leukemic disseminated model, and a high-burden disseminated ALL-2 model derived from a relapsed Philadelphia-positive acute lymphoid leukemia patient. [2]

Protocol

Kinase Assay:[3]
+ Expand

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:[1]
+ Expand
  • Cell lines: A2780 cells
  • Concentrations: 0.1 nM-1 μM, dissolved in DMSO
  • Incubation Time: 72 hours
  • Method: 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)
Animal Research:[1]
+ Expand
  • Animal Models: Mouse xenograft models of human ovarian A2780, colon HCT-116 and pancreatic BX-PC3 carcinoma
  • Formulation: Dissolved in 5% dextrose solution
  • Dosages: 10, 20, and 30 mg/kg
  • Administration: Intravenous injection once daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 72 mg/mL (199.18 mM)
Ethanol 72 mg/mL (199.18 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
15 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 361.48
Formula

C19H31N5O2

CAS No. 718630-59-2
Storage powder
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00996255 Terminated Advanced/Metastatic Solid Tumors Nerviano Medical Sciences November 2006 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

CDK Signaling Pathway Map

CDK Inhibitors with Unique Features

Related CDK Products

Tags: buy PHA-793887 | PHA-793887 supplier | purchase PHA-793887 | PHA-793887 cost | PHA-793887 manufacturer | order PHA-793887 | PHA-793887 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID