IRE1α kinase-IN-8, a benzoheterocyclecarboxaldehyde derivative, is a potent IRE-1α inhibitor.
| Molecular Weight | 406.43 |
| Formula | C23H22N2O5 |
| CAS Number | 1338933-29-1 |
| 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.
[4] Diana Pelizzari Raymundo et al. Trends Cancer. Pharmacological Targeting of IRE1 in Cancer
| Related IRE1 Products |
|---|
| Z4P
Z4P is a BBB-permeable IRE1 inhibitor (IC50: 1.11 μM). |
| IRE1α kinase-IN-9
IRE1α kinase-IN-9 is a potent IRE-1α inhibitor, exhibits an average IC50 value of <0.1 μM. |
| Kira8 Hydrochloride
Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM. |
| KIRA-7
KIRA-7, an imidazopyrazine compound, binds the IRE1α kinase (IC50 of 110 nM) to allosterically inhibit its RNase activity. KIRA-7 has an anti-fibrotic effect. |
| B I09
B I09 is an IRE-1 RNase inhibitor, with an IC50 of 1230 nM. |
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