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AZD0156

Cat. No. M10130
AZD0156 Structure
Synonym:

AZD-0156

Size Price Availability Quantity
10mg USD 135  USD135 In stock
50mg USD 397  USD397 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

AZD0156 is a potent, selective and orally active ATM inhibitor with an IC50 of 0.58 nM. AZD0156 inhibits ATM mediated signal transduction, prevents DNA damage checkpoint activation, damages DNA damage repair, and induces tumor cell apoptosis.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 461.56
Formula C26H31N5O3
CAS Number 1821428-35-6
Purity >99%
Solubility DMSO 2 mg/mL (Need warmed and ultrasonic)
Storage at -20°C
References

[1] Kurt G. Pike. AACR. Identifying high quality, potent and selective inhibitors of ATM kinase: Discovery of AZD0156

Related ATM/ATR Products
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Gartisertib (VX-803) is an ATP-competitive, orally active, selective ATR inhibitor with Ki<150 pM. Gartisertib inhibits atR-driven phosphorylation of checkpoint kinase-1 (Chk1) with an IC50 value of 8 nM. It has antitumor activity.

RP-3500

RP-3500 (ATR inhibitor 4) is an orally potent, selective ATR kinase inhibitor (ATRi) in biochemical assays IC50 1.00 nM. The RP-3500 is 30 times more selective to ATR (IC).50=120 nM), which is 2,000 times > ATM, DNA-PK, and PI3Kα kinase.

AZ32

AZ32 is an orally bioavailable and blood-brain barrier-(BBB)penetrating inhibitor of ATM with IC50 of <6.2 nM and 0.31 μM for ATM enzyme in cell.

AZD1390

AZD1390 is currently the most effective and highly selective ATM inhibitor with an IC50 of 0.78 nM, oral activity and the ability to cross the blood-brain barrier. In vivo, AZD1390 combined with radiotherapy effectively inhibited tumor growth.

AZ31

AZ31 is a potent and highly selective ATM inhibitor.

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Keywords: AZD0156, AZD-0156 supplier, ATM/ATR, inhibitors

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