2. Epigenetics
    Stem Cell/Wnt
    Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  3. JAK
  4. Ritlecitinib

Ritlecitinib  (Synonyms: PF-06651600)

Cat. No.: HY-100754 Purity: 99.98% ee.: 99.98%
COA Handling Instructions

PF-06651600 est un inhibiteur oralement actif et sélectif de JAK3 avec un IC50 de 33,1 nM.

Ritlecitinib (PF-06651600) is an orally active and selective JAK3 inhibitor with an IC50 of 33.1 nM.

For research use only. We do not sell to patients.

Ritlecitinib Chemical Structure

Ritlecitinib Chemical Structure

CAS No. : 1792180-81-4

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Customer Review

Based on 3 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Ritlecitinib (PF-06651600) is an orally active and selective JAK3 inhibitor with an IC50 of 33.1 nM[1].

IC50 & Target[1]

JAK3

33.1 nM (IC50)

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

285.34

Appearance

Solid

Formula

C15H19N5O
CAS No.
SMILES

C=CC(N1[[email protected]@H](C)CC[[email protected]@H](NC2=C3C(NC=C3)=NC=N2)C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (438.07 mM; Need ultrasonic)

H2O : 6.67 mg/mL (23.38 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5046 mL 17.5230 mL 35.0459 mL
5 mM 0.7009 mL 3.5046 mL 7.0092 mL
10 mM 0.3505 mL 1.7523 mL 3.5046 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  0.5% MC  0.5% Tween-80

    Solubility: 6.67 mg/mL (23.38 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

  • 4.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.98% ee.: 99.98%

COA (252 KB) NP-HPLC (231 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

To study the effect of PF-06651600 on Th17 cells post differentiation, skewed Th17 cells are washed, rested with medium for overnight and resuspended in medium containing the same concentrations of cytokines as during skewing but without anti-CD3 or anti-CD28 antibodies, in the presence of PF-06651600 at 10 different concentrations for 2 additional days. On Day 9, supernatant is harvested from each well and IL-17A is determined[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

The effect of JAK3 inhibition by PF-06651600 is evaluated in vivo using a therapeutic dosing paradigm in a rat adjuvant-induced arthritis. When individual hind paw volume measurements indicate an increase of 0.2 mL (or greater) in a single hind paw, animals are randomly assigned to a treatment group. Daily treatment with PF-06651600 is administered via oral gavage. Treatment groups for Experiment 1 are: 80, 15, or 6 mg/kg of PF-06651600 or vehicle (2% Tween 80/0.5% methylcellulose/deionized water). Treatment groups for Experiment 2 are: 30, 10, and 3 mg/kg of PF-06651600 or vehicle (0.5% methylcellulose/de-ionized water/1 mEQ hydrochloric acid). Treatment groups for Experiment 3 are: 10, 1, 0.3 and 0.1 mg/kg of PF-06651600 or vehicle (0.5% methylcellulose/de-ionized water/1 mEQ hydrochloric acid). Treatment continues for 7 days[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Ritlecitinib1792180-81-4PF-06651600PF06651600PF 06651600JAKJanus kinaseInhibitorinhibitorinhibit

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