1. Protein Tyrosine Kinase/RTK
    Apoptosis
  2. Bcr-Abl
    Src
    c-Kit
    Apoptosis
  3. PD180970

PD180970 

Cat. No.: HY-103274
Handling Instructions

PD180970 is a highly potent and ATP-competitive p210Bcr-Abl kinase inhibitor, with an IC50 of 5 nM for inhibiting the autophosphorylation of p210Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC50s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research.

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

PD180970 Chemical Structure

PD180970 Chemical Structure

CAS No. : 287204-45-9

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PD180970 is a highly potent and ATP-competitive p210Bcr-Abl kinase inhibitor, with an IC50 of 5 nM for inhibiting the autophosphorylation of p210Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC50s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research[1][2][3].

IC50 & Target[1][2]

Bcr-Abl

5 nM (IC50, p210Bcr-Abl kinase)

Src

0.8 nM (IC50)

KIT

50 nM (IC50)

In Vitro

PD180970 (0.5 μM; 24-96 hours) treatment causes cell death K562 cells[1].
PD180970 (0.5 μM; 24-48 hours) treatment induces apoptosis of K562 cells. The result shows increase in annexin V-PI double-positive cells[1].
PD180970 inhibits tyrosine phosphorylation of p210Bcr-Abl, Gab2, and CrkL in K562 cells with IC50 values of 170 nM, 80 nM, and 80 nM, respectively. In vitro, PD180970 potently inhibits autophosphorylation of p210Bcr-Abl (IC50 of 5 nM) and the kinase activity of purified recombinant Abl tyrosine kinase (IC50 of 2.2 nM)[1].
The blocking Bcr-Abl kinase activity using PD180970 in the human K562 CML cell line resulted in inhibition of Stat5 DNA-binding activity with an IC50 of 5 nM[2].

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

Cell Viability Assay[1]

Cell Line: K562 cells
Concentration: 0.5 μM
Incubation Time: 24 hours, 48 hours, 72 hours, 96 hours
Result: Resulted in cell death.

Apoptosis Analysis[1]

Cell Line: K562 cells
Concentration: 0.5 μM
Incubation Time: 24 hours, 48 hours
Result: Increased annexin V-positive/PI-negative cells.
In Vivo

PD180970 (5 mg/kg; intraperitonial injection; daily; for 7 days) mitigates MPTP-induced neuronal loss in mice. PD180970 has the neuroprotective ability in a preclinical mouse model of Parkinson's disease (PD)[4].

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

Animal Model: Male C57BL/6J mice (3-4 months old) injected with MPTP[4]
Dosage: 5 mg/kg
Administration: Intraperitonial injection; daily; for 7 days
Result: Decreased number of activated microglia on activation by MPTP in mice brains. And showed significant reduction in intensity of Iba1 expression in activated microglia.
Molecular Weight

429.27

Formula

C₂₁H₁₅Cl₂FN₄O

CAS No.
SMILES

O=C1C(C2=C(Cl)C=CC=C2Cl)=CC3=CN=C(NC4=CC=C(F)C(C)=C4)N=C3N1C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

PD180970PD 180970PD-180970Bcr-AblSrcc-KitApoptosisSCFRCD117p210Bcr-AblCMLapoptosisStat5neuroprotectiveInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PD180970
Cat. No.:
HY-103274
Quantity:
MCE Japan Authorized Agent: