PF-06700841 (Brepocitinib) is a dual inhibitor of JAK1 and TYK2, with IC50 values of 17 nM and 23 nM, respectively. PF-06700841 (Brepocitinib) inhibits EPO/pSTAT5 (JAK2 homodimer) in HWB spiked with CD34+ progenitor cells (IC50 of 577 nM). PF-06700841 also inhibits the JAK1/JAK3 driven γ-common chain cytokines, represented by IL-15/pStat5 and IL-21/pSTAT3 with reasonable potency (HWB IC50s of 238 and 204 nM, respectively).
| Molecular Weight | 561.60 |
| Formula | C25H29F2N7O4S |
| CAS Number | 2140301-96-6 |
| Solubility (25°C) | DMSO 57 mg/mL |
| 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 |
|---|
| SDC-1802
SDC-1802 is a JAK1/TYK2 inhibitor that can be used in studies related to systemic lupus erythematosus. |
| OST-246
OST-246 is an inhibitor of JAK3, MAP3K11, and TYK2 for studies related to autoimmune diseases and inflammation. |
| NDI-031232
NDI-031232 is a TYK2 inhibitor. |
| NDI-031301
NDI-031301 is a TYK2 inhibitor. |
| NDI-031407
NDI-031407 is a TYK2 inhibitor for studies related to endocrine metabolic diseases and psoriasis. |
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