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Fm-479 was a negative control of FM-381 and showed no activity against JAK3 or other kinases. Fm-381 is a potent covalent reversible inhibitor of JAK3 targeting unique Cys909. For JAK3, FM-381 was 410, 2700 and 3600 times more selective than JAK1, JAK2 and TYK2 with IC50 of 127 pM.
| Molecular Weight | 442.51 |
| Formula | C25H26N6O2 |
| CAS Number | 2226521-64-6 |
| Solubility (25°C) | N/A |
| 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 JAK Products |
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| Zasocitinib
Zasocitinib (NDI-034858) is a highly selective, orally active TYK2 inhibitor, target TYK2 JH2 domain with binding constant Kd of <200 pM. |
| BMS-986202
BMS-986202 is a potent, selective, orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 of 0.19 nM and a Ki of 0.02 nM. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC50 of 14 μM. BMS-986202 can be used in IL-23-driven echinococcosis BMS-986202 can be used in studies of IL-23-driven echinococcosis, anti-CD40-induced colitis and spontaneous lupus. |
| GDC046
GDC046 (Compound 3) is a potent, selective, and orally bioavailable inhibitor of TYK2 with Ki of 4.8 nM, 83.8 nM, 27.6 nM and 253 nM for TYK2, JAK1, JAK2, and JAK3, respectively. |
| RO495
RO495 (CS-2667) is a potent inhibitor of Non-receptor tyrosine-protein kinase 2 (TYK2). |
| TG-89
TG-89 is a JAK inhibitor that inhibits JAK2, FLT3, RET and JAK3. |
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