1. Protein Tyrosine Kinase/RTK
  2. Src FGFR PDGFR
  3. PP58

PP58 

Cat. No.: HY-18622 Purity: 99.75%
COA Handling Instructions

PP58 is a pyrido[2,3-d]pyrimidine-based compound that inhibits PDGFR, FGFR and Src family activities with nanomolar IC50 values.

For research use only. We do not sell to patients.

PP58 Chemical Structure

PP58 Chemical Structure

CAS No. : 212391-58-7

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 126 In-stock
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10 mg USD 180 In-stock
50 mg USD 490 In-stock
100 mg USD 780 In-stock
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

PP58 is a pyrido[2,3-d]pyrimidine-based compound that inhibits PDGFR, FGFR and Src family activities with nanomolar IC50 values.

IC50 & Target[1]

PDGFR

 

In Vitro

PP58 inhibits Src with a subnanomolar IC50 value in the assays. PP58 behaves as a titration reagent at higher Src protein concentrations. As analyzed by immunoblotting with specific antiserum, the PP58 matrix specifically depletes Src from total lysate, whereas binding to the PP58 beads is prevented when free inhibitor is included. The ectopically expressed FGFR1 receptor tyrosine kinase is specifically retained on PP58 beads. PP58 matrix could be a novel affinity reagent for the purification of cellular pyrido[2,3-d]pyrimidine inhibitor targets. PP58 affinity chromatography leads to the identification of protein kinases belonging to various different groups and families, indicating that the pyrido[2,3-d]pyrimidine inhibitor is not selective for a set of phylogenetically related members of the human kinome. The Ki values of PP58 for p38α and JNK2 are 3.8±1.9 nM and 0.32±0.04 μM, respectively. PP58 affinity matrix also serves as an efficient purification reagent for a variety of protein kinases, which lack this structural feature and have much lower affinities for the pyrido[2,3-d]pyrimidine inhibitor PP58. PP58 inhibits anisomycin activated p38 in a dose-dependent manner with an IC50 below 10 nM. LPS-stimulated TNF-α production is potently inhibited by PP58 with a cellular IC50 value of around 3 nM[1]. The T341M mutation abrogates the sensitivity to PP58 inhibition by increasing the cellular IC50 value of about 10 nM by more than 1000-fold. The cellular wild-type FGFR1 activity is potently inhibited by low nanomolar concentrations of PP58, whereas dramatic resistance formation is detected for the FGFR1-V561M mutant. PP58 inhibits CSK activity with an IC50 value of around 100 nM[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PP58 can exhibit some degree of selectivity at low nanomolar concentrations in vivo[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

456.32

Formula

C22H19Cl2N5O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

NCCOC1=CC=C(NC(N=C2N3C)=NC=C2C=C(C4=C(Cl)C=CC=C4Cl)C3=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (136.97 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1914 mL 10.9572 mL 21.9144 mL
5 mM 0.4383 mL 2.1914 mL 4.3829 mL
10 mM 0.2191 mL 1.0957 mL 2.1914 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (4.56 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.75%

References
Kinase Assay
[1]

MEK1 and Aurora A activities are tested at 37 °C in a total volume of 30 μL. The kinases are assayed using 50 μM ATP and 1 μCi [γ-32P]ATP in the presence of different PP58 concentrations. Kinase substrate proteins included are 0.25 mg/mL inactive GST-ERK2 for MEK1 and 0.025 mg/mL kemptide for Aurora A, respectively. Reactions are stopped by addition of SDS sample buffer. Determination of IC50 [0–100%] values is performed using GraFit software[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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PP58 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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