Ritlecitinib (PF-06651600)
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 250mg | $1450 | Check With Us |
| 500mg | $2150 | Check With Us |
| 1g | $3225 | Check With Us |
: Cat #: V3111 CAS #: 1792180-81-4 Purity ≥ 98%
Description: Ritlecitinib (PF-06651600) is a novel, potent, selective and irreversible/covalent JAK3 inhibitor with the potential to treat autoimmune diseases such as arthritis and Alopecia areata.
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| Molecular Weight (MW) | 285.34 |
|---|---|
| Molecular Formula | C15H19N5O |
| CAS No. | 1792180-81-4 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 150 mg/mLr |
| Water: NAr | |
| Ethanol: NA | |
| SMILES Code | C=CC(N1[C@@H](C)CC[C@@H](NC2=C3C(NC=C3)=NC=N2)C1)=O |
| Synonyms | PF-06651600; Ritlecitinib; PF06651600; PF 06651600 |
| Protocol | In Vitro | Ritlecitinib is a potent JAK3-selective inhibitor which can inhibit the JAK3 kinase activity with an IC50 of 33.1 nM but without activity (IC50>10 000 nM) against JAK1, JAK2, and TYK2. Ritlecitinib inhibits the phosphorylation of STAT5 elicited by IL-2, IL-4, IL-7, and IL-15 with IC50 values of 244, 340, 407, and 266 nM, respectively. Ritlecitinib also inhibits the phosphorylation of STAT3 elicited by IL-21 with an IC50 of 355 nM. Functional assessment in T-cell differentiation assays demonstrate that Ritlecitinib suppresses Th1 and Th17 differentiation as measured by IFNγ, after 5 days under Th1 conditions, and IL-17 production, after 6 days under Th17 conditions, with IC50 values of 30 nM and 167 nM, respectively. Ritlecitinib also suppresses Th1 and Th17 function as measured by the inhibition of IFNγ production (IC50=48 nM) and IL-17 production (IC50=269 nM) in cells that have been previously differentiated and rested before being treated with PF-06651600. |
|---|---|---|
| In Vivo | In the rat adjuvant-induced arthritis (AIA) model, Ritlecitinib reduces paw swelling with an unbound EC50 of 169 nM. Similarly, Ritlecitinib significantly reduces disease severity in the experimental autoimmune encephalomyelitis (EAE) mouse model when dosed either therapeutically at 30 or 100 mg/kg or prophylactically at 20 and 60 mg/kg. The efficacy of Ritlecitinib in these two rodent models of inflammatory and autoimmune diseases illustrates that JAK3-selective inhibition can be sufficient to have disease modifying effects in human diseases. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 3.5046 mL | 17.5230 mL | 35.0459 mL | 70.0918 mL |
| 5mM | 0.7009 mL | 3.5046 mL | 7.0092 mL | 14.0184 mL |
| 10mM | 0.3505 mL | 1.7523 mL | 3.5046 mL | 7.0092 mL |
| 20mM | 0.1752 mL | 0.8761 mL | 1.7523 mL | 3.5046 mL |
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Step Two: Enter the in vivo formulation
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Method for preparing DMSO master liquid:
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Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.