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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.
| 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.
| Molecular Weight | 477.57 |
| Formula | C27H32FN5O2 |
| CAS Number | 2089288-03-7 |
| Purity | >99% |
| Solubility | DMSO ≥ 15 mg/mL (May need warming) |
| Storage | at -20°C |
| Related ATM/ATR Products |
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| Gartisertib
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. |
| AZD0156
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. |
| AZ31
AZ31 is a potent and highly selective ATM inhibitor. |
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