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Brepocitinib
Brepocitinib (PF-06700841) is a potent dual JAK1/TYK2 inhibitor with IC50 values of 17 nM and 23 nM, respectively, and also inhibits JAK2 and JAK3 with IC50 values of 77 nM and 6.49 μM.
Catalog No. TQ0010Cas No. 1883299-62-4
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Brepocitinib
Catalog No. TQ0010Cas No. 1883299-62-4
Brepocitinib (PF-06700841) is a potent dual JAK1/TYK2 inhibitor with IC50 values of 17 nM and 23 nM, respectively, and also inhibits JAK2 and JAK3 with IC50 values of 77 nM and 6.49 μM.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $30 | In Stock | |
| 5 mg | $64 | In Stock | |
| 10 mg | $106 | In Stock | |
| 25 mg | $228 | In Stock | |
| 50 mg | $413 | In Stock | |
| 100 mg | $662 | In Stock | |
| 200 mg | $926 | In Stock | |
| 500 mg | $1,370 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $119 | In Stock |
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CitedProduct Introduction
Bioactivity
Chemical Properties
| Description | Brepocitinib (PF-06700841) is a potent dual JAK1/TYK2 inhibitor with IC50 values of 17 nM and 23 nM, respectively, and also inhibits JAK2 and JAK3 with IC50 values of 77 nM and 6.49 μM. |
| Targets&IC50 | JAK3:6.9 μM, JAK2:77 nM (cell free), TYK2:23 nM (cell free), JAK1:17 nM (cell free) |
| In vitro | PF-06700841 inhibits TYK2/JAK2 mediated IL-12/pSTAT4 and IL-23/pSTAT3 (human whole blood IC50s: 65/120 nM). PF-06700841 inhibits the JAK1/JAK3 driven γ-common chain cytokines, represented by IL-15/pStat5 and IL-21/pSTAT3 with reasonable potency (IC50s: 238/204 nM). PF-06700841 also has good potency against IL6/pStat1 in the CD3+ cellular subset (IC50: 81 nM), but lower inhibition of IL6/pSTAT3, again in the CD3+ cellular subset (IC50: 641 nM). PF-06700841 inhibits EPO/pSTAT5 (JAK2 homodimer) in HWB spiked with CD34+ progenitor cells (IC50: 577 nM). IL10/pSTAT3 (TYK2/JAK1) and IL27/pSTAT3 (JAK1/JAK2/TYK2) are also inhibited by PF-06700841 (IC50s: 305 nM/86 nM). |
| In vivo | PF-06700841 (3-30 mg/kg; p.o; for 7 consecutive days; female Lewis rats) treatment significantly reduces paw volume increase in a dose-dependent manner. The plasma concentrations in animals dosed with PF-06700841 at peak (30 min) and trough (24 h) time intervals post final dose respectively are as follows: 3 mg/kg, 3.54 μM, 0.0221 μM; 10 mg/kg, 10.95 μM, 0.06 μM; and 30 mg/kg, 23.89 μM, 0.06 μM. |
| Alias | PF-06700841 |
| Molecular Weight | 389.4 |
| Formula | C18H21F2N7O |
| Cas No. | 1883299-62-4 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: Insoluble DMSO: 75 mg/mL (192.60 mM) Ethanol: 75 mg/mL (192.60 mM) | |||||||||||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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