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PD180970

Catalog No. T23128   CAS 287204-45-9
Synonyms: PD 180970

PD180970 is an inhibitor of Bcr-Abl with IC50s of 5 nM, 0.8 nM and 50 nM for the autophosphorylation of p210Bcr-Abl, Src and Kit. PD180970 can be used in studies about chronic myelogenous leukemia.

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PD180970 Chemical Structure
PD180970, CAS 287204-45-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
5 mg In stock $ 89.00
10 mg In stock $ 147.00
25 mg In stock $ 246.00
50 mg In stock $ 369.00
100 mg In stock $ 543.00
1 mL * 10 mM (in DMSO) In stock $ 97.00
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Purity: 98.47%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PD180970 is an inhibitor of Bcr-Abl with IC50s of 5 nM, 0.8 nM and 50 nM for the autophosphorylation of p210Bcr-Abl, Src and Kit. PD180970 can be used in studies about chronic myelogenous leukemia.
Targets&IC50 c-Kit:50 nM, Src:0.8 nM, BCR-ABL:5 nM (Ip210Bcr-Ablkinase)
In vitro In K562 cells, PD180970 (0.5 μM) induces apoptosis and causes cell death. The IC50 values are 170, 80, and 80 nM for the tyrosine phosphorylation of p210Bcr-Abl, Gab2, and CrkL. PD180970 significantly inhibits the purified recombinant Abl tyrosine kinase activity with an IC50 of 2.2 nM[1]. In the human K562 CML cells, PD180970 inhibits the activity of Stat5 DNA-binding with an IC50 of 5 nM[2].
In vivo In Male C57BL/6J mice injected with MPTP, intraperitonial injection of PD180970 (5 mg/kg) decreased number of activated microglia on activation by MPTP and reduces the Iba1 expression intensity in activated microglia[1].
Synonyms PD 180970
Molecular Weight 429.27
Formula C21H15Cl2FN4O
CAS No. 287204-45-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90.0 mg/mL (209.7 mM), Sonication is recommended.

TargetMolReferences and Literature

1. J F Dorsey, et al. The pyrido[2,3-d]pyrimidine derivative PD180970 inhibits p210Bcr-Abl tyrosine kinase and induces apoptosis of K562 leukemic cells. Cancer Res. 2000 Jun 15;60(12):3127-31. 2. Mei Huang, et al. Inhibition of Bcr-Abl kinase activity by PD180970 blocks constitutive activation of Stat5 and growth of CML cells. Oncogene. 2002 Dec 12;21(57):8804-16. 3. Amie S Corbin, et al. Sensitivity of oncogenic KIT mutants to the kinase inhibitors MLN518 and PD180970. Blood. 2004 Dec 1;104(12):3754-7. 4. Suresh Sn, et al. Small molecule modulator of aggrephagy regulates neuroinflammation to curb pathogenesis of neurodegeneration. EBioMedicine. 2019 Dec;50:260-273.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Metabolism Compound Library Kinase Inhibitor Library Cytoskeletal Signaling Pathway Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

PD180970 287204-45-9 Angiogenesis Cytoskeletal Signaling Tyrosine Kinase/Adaptors Bcr-Abl Src c-Kit PD-180970 PD 180970 inhibitor inhibit

 

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