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

Ritlecitinib  (Synonyms: リトレシチニブ; PF-06651600)

製品番号: HY-100754 純度: 99.43%
COA 取扱説明書 Technical Support

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

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Ritlecitinib 構造式

Ritlecitinib 構造式

CAS 番号 : 1792180-81-4

容量 価格（税別） 在庫状況 数量
無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 88 在庫あり
Solution
10 mM * 1 mL in DMSO USD 88 在庫あり
Solid
5 mg USD 64 在庫あり
10 mg USD 119 在庫あり
25 mg USD 280 在庫あり
50 mg USD 392 在庫あり
100 mg USD 548 在庫あり
500 mg USD 1250 在庫あり
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5 g   お問い合わせ  

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カスタマーレビュー

Based on 7 publication(s) in Google Scholar

Other Forms of Ritlecitinib:

Ritlecitinib 関連抗体

Top Publications Citing Use of Products

JAK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
JAK1 JAK2 JAK3 Tyk2 JAK

  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

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)

Cellular Effect
Cell Line Type Value Description References
BaF3 IC50
> 10000 nM
Compound: 11; PF-06651600
Antiproliferative activity against mouse BaF3 parent cell measured after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 parent cell measured after 72 hrs by CCK-8 assay
[PMID: 35860875]
BaF3 IC50
> 10000 nM
Compound: 11; PF-06651600
Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK1 fusion protein assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK1 fusion protein assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
[PMID: 35860875]
BaF3 IC50
> 10000 nM
Compound: 11; PF-06651600
Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK2 fusion protein assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK2 fusion protein assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
[PMID: 35860875]
BaF3 IC50
28.1 nM
Compound: 11; PF-06651600
Antiproliferative activity against mouse BaF3 cells harboring JAK3 M5111 mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells harboring JAK3 M5111 mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
[PMID: 35860875]
CD4+ve Th IC50
48 nM
Compound: PF-06651600
Inhibition of Th1 cell differentiation in human peripheral blood CD4+ve Th cells assessed as decrease in IFNgamma production measured after 5 days
Inhibition of Th1 cell differentiation in human peripheral blood CD4+ve Th cells assessed as decrease in IFNgamma production measured after 5 days
[PMID: 36561076]
U-937 IC50
0.04 μM
Compound: 5; PF-06651600
Antiproliferative activity against human U-937 cells harbouring JAK3 M511 mutation assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human U-937 cells harbouring JAK3 M511 mutation assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
[PMID: 35306167]
U-937 IC50
19.5 nM
Compound: 11; PF-06651600
Antiproliferative activity against human U-937 cells harboring JAK3 M511135 mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against human U-937 cells harboring JAK3 M511135 mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
[PMID: 35860875]
体外実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ritlecitinib 関連抗体
体内実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

285.35

分子式

C15H19N5O
CAS 番号
Appearance

Solid

Color

White to yellow

SMILES

C=CC(N1[C@@H](C)CC[C@@H](NC2=C3C(NC=C3)=NC=N2)C1)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 125 mg/mL (438.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5045 mL 17.5223 mL 35.0446 mL
5 mM 0.7009 mL 3.5045 mL 7.0089 mL
10 mM 0.3504 mL 1.7522 mL 3.5045 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  0.5% Methyl cellulose/0.5% Tween-80 in Saline water

    Solubility: 6.67 mg/mL (23.37 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.80% ee.: 99.93%

COA (253 KB) HNMR (226 KB) NP-HPLC (103 KB) LCMS (110 KB)

取扱説明書 (2659 KB)
参考文献
細胞実験
[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
動物実験
[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.5045 mL 17.5223 mL 35.0446 mL 87.6114 mL
5 mM 0.7009 mL 3.5045 mL 7.0089 mL 17.5223 mL
10 mM 0.3504 mL 1.7522 mL 3.5045 mL 8.7611 mL
15 mM 0.2336 mL 1.1682 mL 2.3363 mL 5.8408 mL
20 mM 0.1752 mL 0.8761 mL 1.7522 mL 4.3806 mL
25 mM 0.1402 mL 0.7009 mL 1.4018 mL 3.5045 mL
30 mM 0.1168 mL 0.5841 mL 1.1682 mL 2.9204 mL
40 mM 0.0876 mL 0.4381 mL 0.8761 mL 2.1903 mL
50 mM 0.0701 mL 0.3504 mL 0.7009 mL 1.7522 mL
60 mM 0.0584 mL 0.2920 mL 0.5841 mL 1.4602 mL
80 mM 0.0438 mL 0.2190 mL 0.4381 mL 1.0951 mL
100 mM 0.0350 mL 0.1752 mL 0.3504 mL 0.8761 mL
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Ritlecitinib Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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.

Keywords:

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

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