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

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 Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 121 In-stock
Solution
10 mM * 1 mL in DMSO USD 121 In-stock
Solid
5 mg USD 110 In-stock
10 mg USD 180 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

PD180970 Related Antibodies

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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)

Cellular Effect
Cell Line Type Value Description References
K562 IC50
5 nM
Compound: 2, PD180970
Inhibition of STAT5 DNA binding activity in human K562 cells after 24 hrs by electrophoretic mobility shift assay
Inhibition of STAT5 DNA binding activity in human K562 cells after 24 hrs by electrophoretic mobility shift assay
10.1039/C1MD00175B
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].

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

PD180970 Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

Light yellow to yellow

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (232.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3295 mL 11.6477 mL 23.2954 mL
5 mM 0.4659 mL 2.3295 mL 4.6591 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 1.25 mg/mL (2.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.27%

SDS (251 KB)

COA (248 KB) HNMR (256 KB) LCMS (256 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3295 mL 11.6477 mL 23.2954 mL 58.2384 mL
5 mM 0.4659 mL 2.3295 mL 4.6591 mL 11.6477 mL
10 mM 0.2330 mL 1.1648 mL 2.3295 mL 5.8238 mL
15 mM 0.1553 mL 0.7765 mL 1.5530 mL 3.8826 mL
20 mM 0.1165 mL 0.5824 mL 1.1648 mL 2.9119 mL
25 mM 0.0932 mL 0.4659 mL 0.9318 mL 2.3295 mL
30 mM 0.0777 mL 0.3883 mL 0.7765 mL 1.9413 mL
40 mM 0.0582 mL 0.2912 mL 0.5824 mL 1.4560 mL
50 mM 0.0466 mL 0.2330 mL 0.4659 mL 1.1648 mL
60 mM 0.0388 mL 0.1941 mL 0.3883 mL 0.9706 mL
80 mM 0.0291 mL 0.1456 mL 0.2912 mL 0.7280 mL
100 mM 0.0233 mL 0.1165 mL 0.2330 mL 0.5824 mL
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PD180970 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PD180970287204-45-9PD 180970PD-180970Bcr-AblSrcc-KitApoptosisSCFRCD117p210Bcr-AblCMLapoptosisStat5neuroprotectiveInhibitorinhibitorinhibit

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