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%
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  • COA
  • NMR
  • HPLC
  • SDS
  • Datasheet
99.78

Solubility

In vitro
Batch:

DMSO : 15 mg/mL (33.83 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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

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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

Mechanism of Action

Targets/IC50/Ki
Bcr-Abl
1 nM-2 nM
Src
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. 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.
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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