Home Cart Sign in  
Chemical Structure| 612487-72-6 Chemical Structure| 612487-72-6

Structure of AZD1080
CAS No.: 612487-72-6

Chemical Structure| 612487-72-6

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor of GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively, shows > 14-fold selectivity against CDK2, CDK5, CDK1 and Erk2.

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

Product Details of AZD1080

CAS No. :612487-72-6
Formula : C19H18N4O2
M.W : 334.37
SMILES Code : N#CC1=CC2=C(NC(O)=C2C3=NC=C(CN4CCOCC4)C=C3)C=C1
MDL No. :MFCD12031593
InChI Key :BLTVBQXJFVRPFK-UHFFFAOYSA-N
Pubchem ID :135564570

Safety of AZD1080

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of AZD1080

PI3K-AKT
Hedgehog

Isoform Comparison

Biological Activity

Target
  • GSK-3α

    GSK-3α, IC50:6.9 nM

  • GSK-3β

    GSK-3β, IC50:31 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Splenic T-cells 100, 10, 1, 0.1, 0.01 μg/mL 24 hours To assess the impact of AZD1080 on splenic T-cell viability, results showed decreased viability at 100 μg/mL, but a slight increase in cell viability over the dose range 0.01 to 1 μg/mL. PMC7870571
KPC cells 100, 10, 1, 0.1, 0.01 μg/mL 24 hours To assess the impact of AZD1080 on KPC cell viability, results showed no significant changes. PMC7870571
LLC cells 100, 10, 1, 0.1, 0.01 μg/mL 24 hours To assess the impact of AZD1080 on LLC cell viability, results showed decreased viability at a high dose (100 μg/mL). PMC7870571
CT26 cells 100, 10, 1, 0.1, 0.01 μg/mL 24 hours To assess the impact of AZD1080 on CT26 cell viability, results showed slightly enhancing the viability at 10 and 100 μg/mL. PMC7870571
MC38 cells 100, 10, 1, 0.1, 0.01 μg/mL 24 hours To assess the impact of AZD1080 on MC38 cell viability, results showed that only the LLC cell line showed decreased viability at a high dose (100 μg/mL) of AZD1080, while slightly enhancing the viability of MC38 and CT26 cells at 10 and 100 μg/mL. PMC7870571
OVCAR3 0.5 μM, 1.0 μM, 2.0 μM, 4.0 μM different time points AZD1080 suppressed OVCAR3 cell proliferation in a concentration-dependent manner. PMC4807899
A2780 0.5 μM, 1.0 μM, 2.0 μM, 4.0 μM different time points AZD1080 suppressed A2780 cell proliferation in a concentration-dependent manner. PMC4807899

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice MC38 colon cancer model Intravenous injection 5 mg/kg Every three days for a total of three times To assess the therapeutic effect of AZD1080 on the MC38 colon cancer model, results showed that sAZD1080 significantly inhibited tumor growth, with 6 out of 15 mice becoming tumor-free. PMC7870571
Nude mice KRAS-driven lung cancer mouse models Oral gavage 25 mg/kg Once daily for 4 weeks To evaluate the antitumor effect of the combination therapy of PP2A activator DT-061 and MEK inhibitor AZD6244 PMC8335581

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.99mL

0.60mL

0.30mL

14.95mL

2.99mL

1.50mL

29.91mL

5.98mL

2.99mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

Historical Records

Categories