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AZD8186

Cat. No. M14845
AZD8186 Structure
Size Price Availability Quantity
5mg USD 150  USD150 In stock
10mg USD 250  USD250 In stock
50mg USD 740  USD740 In stock
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Quality Control & Documentation
Biological Activity

AZD8186 is a PI3K inhibitor, which potently inhibits PI3Kβ (IC50=4 nM) and PI3Kδ (IC5050=12 nM) with selectivity over PI3Kα (IC50=35 nM) and PI3Kγ (IC50=675 nM).

Chemical Information
Molecular Weight 457.47
CAS Number 1627494-13-6
Solubility (25°C) DMSO ≥ 35 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] Atish D Choudhury, et al. A Phase I Study Investigating AZD8186, a Potent and Selective Inhibitor of PI3Kβ/δ, in Patients with Advanced Solid Tumors

[2] Nicci Owusu-Brackett, et al. Targeting PI3Kβ alone and in combination with chemotherapy or immunotherapy in tumors with PTEN loss

[3] Esteban A Terzo, et al. SETD2 loss sensitizes cells to PI3Kβ and AKT inhibition

[4] James T Lynch, et al. Inhibiting PI3Kβ with AZD8186 Regulates Key Metabolic Pathways in PTEN-Null Tumors

[5] Urs Hancox, et al. Inhibition of PI3Kβ signaling with AZD8186 inhibits growth of PTEN-deficient breast and prostate tumors alone and in combination with docetaxel

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  Catalog
Abmole Inhibitor Catalog




Keywords: AZD8186 supplier, PI3K, inhibitors, activators


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