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

PP58 

Cat. No.: HY-18622 Purity: 98.07%
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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 422 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
1 mg USD 168 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 1800 Get quote
100 mg   Get quote  
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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].

In Vivo

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

Solvent & Solubility
In Vitro: 

10 mM in DMSO

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.
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
Molecular Weight

456.32

Formula

C₂₂H₁₉Cl₂N₅O₂

CAS No.

212391-58-7

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
PP58
Cat. No.:
HY-18622
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PP58

Cat. No.: HY-18622