Home Angiogenesis Bcr-Abl inhibitor PD173955

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PD173955 Bcr-Abl inhibitor

Cat.No.S7269

PD173955 is a potent Bcr-Abl inhibitor with IC50 of 1-2 nM, also inhibiting Src activity with IC50 of 22 nM.
PD173955 Bcr-Abl inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 443.35

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Quality Control

Batch: S726901 DMSO]15 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.78%
99.78

Chemical Information, Storage & Stability

Molecular Weight 443.35 Formula

C21H16Cl2N4OS

 Storage (From the date of receipt)
CAS No. 260415-63-2 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CN1C2=NC(=NC=C2C=C(C1=O)C3=C(C=CC=C3Cl)Cl)NC4=CC(=CC=C4)SC

Solubility

In vitro
Batch:

DMSO : 15 mg/mL ( (33.83 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
Bcr-Abl [1]
1 nM-2 nM
Src [2]
22 nM
In vitro
PD173955 potently inhibits Bcr-Abl-dependent cell growth with IC50 of 2-35 nM in Bcr-Abl-positive cell lines, about 100- to 200-fold more sensitive than in Bcr-Abl-negative cell lines. This compound also inhibits kit ligand-dependent proliferation of M07e cells with IC50 of 40 nM, by inhibition of kit ligand-dependent c-kit autophosphorylation. [1] In addition, this chemical, as a Src inhibitor, potently inhibits mitotic progression during early mitosis in cells of all types and induces varying degrees of apoptotic cell death. [2]
Kinase Assay
In Vitro Bcr-Abl Kinase Assays
Bcr-Abl complexed to SHIP2 is immunoprecipitated from cell lysates of K562 cells maintained in log-phase culture conditions. Complexes are collected on protein A-Sepharose, and complexes are washed three times in lysis buffer and then washed twice in abl kinase buffer [50 mM Tris (pH 8.0), 10 mM MgCl2, 1 mM DTT, 2 mM p-nitrophenylphosphate, and 2 μM ATP; New England Biolabs Buffer and protocol]. Kinase assays are performed with 10 μM [γ-32P]ATP/sample for 15–60 min at 30°C in the presence or absence of the indicated concentrations of drug. The reaction is stopped by the addition of SDS-PAGE sample buffer and heated at 100°C for 10 min. Proteins are separated on 7.5% SDS-polyacrylamide gels, gels are dried under vacuum, and phosphorylation is visualized by autoradiography on X-ray film.
References

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