Cat. No.: HY-100754B

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(2R,5S)-Ritlecitinib

(Synonyms: (2R,5S)-PF-06651600)

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(2R,5S)-Ritlecitinib (2R,5S)-PF-06651600) is a JAK3 inhibitor (IC50=144.8 nM).

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

Purity: 99.77%
CAS No.: 1792180-79-0
Formula: C₁₅H₁₉N₅O
Molecular Weight:285.35

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

(2R,5S)-Ritlecitinib Chemical Structure

CAS No.: 1792180-79-0

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

(2R,5S)-Ritlecitinib (2R,5S)-PF-06651600) is a JAK3 inhibitor (IC50=144.8 nM)^[1]^[2].

IC₅₀ & Target^[1]

JAK3

144.8 nM (IC₅₀)

All JAK Isoforms :

In Vitro

(2R,5S)-Ritlecitinib (example 68) has different IC₅₀s for inhibiting JAK3 at different ATP concentrations. At 4 μM ATP, IC₅₀=144.8 nM; at 1 mM ATP, IC₅₀ >2477.8 nM^[1].
The stable half-life of (2R,5S)-Ritlecitinib in human blood shows T_1/2 >360 min^[1].
(2R,5S)-Ritlecitinib (compound 13) targets JAK3 (1 mM ATP) with an IC₅₀ >2478 nM, and its isomer Ritlecitinib (HY-100754) has an IC₅₀ of 33 nM^[2].

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

Chemical Information

CAS No. 1792180-79-0
Appearance Solid
Molecular Weight 285.35
Formula C₁₅H₁₉N₅O
Color White to light yellow
SMILES

C[C@@H]1CC[C@@H](CN1C(C=C)=O)NC2=C3C=CNC3=NC=N2
Synonyms

(2R,5S)-PF-06651600
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (350.45 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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Volume _(start) Volume _(start)

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In Vivo:

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

Stock Solution Working Solution

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: ≥ 5.5 mg/mL (19.27 mM); Clear solution

This protocol yields a clear solution of ≥ 5.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 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.

Protocol 2

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

Solubility: ≥ 5.5 mg/mL (19.27 mM); Clear solution

This protocol yields a clear solution of ≥ 5.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5.5 mg/mL (19.27 mM); Clear solution

This protocol yields a clear solution of ≥ 5.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Matthew Frank, et al. Pyrrolo[2,3-d]pyrimidinyl-, pyrrolo[2,3-b]pyrazinyl-and pyrrolo[2,3-d]pyridinylacrylamides as JAK inhibitor and their preparation. World Intellectual Property Organization, WO2015083028 A1 2015-06-11.

[2]. Thorarensen A, et al. Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2 S, 5 R)-5-((7 H-Pyrrolo [2, 3-d] pyrimidin-4-yl) amino)-2-methylpiperidin-1-yl) prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans. Journal of medicinal chemistry, 2017, 60(5): 1971-1993.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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(2R,5S)-Ritlecitinib

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Cysteine Targeted Covalent Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

3D Diverse Fragment Library

All JAK Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

(2R,5S)-Ritlecitinib Related Classifications

Cat. No.: HY-100754B