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AZD6482

Cat. No. M2295
AZD6482 Structure
Synonym:

KIN 193

Size Price Availability Quantity
10mg USD 160  USD160 In stock
50mg USD 580  USD580 In stock
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Quality Control & Documentation
Biological Activity

AZD6482 is a PI3Kβ inhibitor (IC50=0.021μM) used in antithrombotic therapy. AZD6482 targets a process that is critical to pathological thrombus formation without interfering with normal haemostasis, which avoids the drawbacks of the existing anti-thrombotic therapy.

Chemical Information
Molecular Weight 408.45
Formula C22H24N4O4
CAS Number 1173900-33-8
Solubility (25°C) DMSO 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Hua-Fu Zhao, et al. Correction to: Synergism between the phosphatidylinositol 3-kinase p110β isoform inhibitor AZD6482 and the mixed lineage kinase 3 inhibitor URMC-099 on the blockade of glioblastoma cell motility and focal adhesion formation

[2] Hua-Fu Zhao, et al. Synergism between the phosphatidylinositol 3-kinase p110β isoform inhibitor AZD6482 and the mixed lineage kinase 3 inhibitor URMC-099 on the blockade of glioblastoma cell motility and focal adhesion formation

[3] Jianbo Tian, et al. N 6-methyladenosine mRNA methylation of PIK3CB regulates AKT signalling to promote PTEN-deficient pancreatic cancer progression

[4] Peng-Fei Xu, et al. PI3Kβ inhibitor AZD6482 exerts antiproliferative activity and induces apoptosis in human glioblastoma cells

[5] S Nylander, et al. Human target validation of phosphoinositide 3-kinase (PI3K)β: effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kβ inhibitor

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Keywords: AZD6482, KIN 193 supplier, PI3K, inhibitors, activators


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