In vitro: LTURM34 shows potent inhibition of DNA-PK with excellent selectivity over the Class I PI3K isoforms. The IC50s are 5.8 and 8.5 μM for PI3K β and δ, respectively. LTURM34 shows potent and broad ranging antiproliferative activity. LTURM34 is more consistently active against the selected cell lines (11 of 16), but at best shows 54% inhibition against the HOP-92 non-small cell lung cancer line.
| Molecular Weight | 414.48 |
| Formula | C24H18N2O3S |
| CAS Number | 1879887-96-3 |
| Solubility (25°C) | 82 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
| Related DNA-PK Products |
|---|
| ZL-2201
ZL-2201 is a potent DNA-PK inhibitor with an IC50 of 1 nM. |
| AMA-37
AMA-37, an Arylmorpholine analog, is ATP-competitive DNA-PK inhibitor, with IC50 values of 0.27 μM (DNA-PK), 32 μM (p110α), 3.7 μM (p110β), and 22 μM (p110γ), respectively. |
| PIK-75
PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 induces apoptosis. |
| BAY-8400
The DNA-PK inhibitor BAY-8400 is an orally active and selective inhibitor of DNA-PK kinase that synergistically enhances the efficacy of radiotherapeutic agents in xenograft models. |
| STL127705
STL127705 (Compound L) is a Ku 70/80 heterodimer protein inhibitor, inhibits Ku70/80-DNA interaction, with an IC50 of 3.5 μM. STL127705 also inhibits Ku-dependent activation of DNA-PKCS kinase (IC50, 2.5 μM). |
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