Referencia número: HY-156961

Cadefrecitinib

(Synonyms: GLPG3667)

Revisión del cliente

Based on 1 Customer Validation

Cadefrecitinib (GLPG3667) is a reversible, ATP-competitive and orally active TYK2 inhibitor with an IC₅₀ of 2.3 nM. Cadefrecitinib inhibits IFNα/pSTAT1, and the IC₅₀ values in human peripheral blood mononuclear cell (PBMC) and whole blood assays are 70 nM and 623 nM, respectively. Cadefrecitinib has the potential for the study of inflammatory and autoimmune diseases.

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Pureza: 99.81%
No. CAS: 2308520-97-8
Fòrmula: C₂₂H₂₁N₉O₂
Peso molecular:443.46

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Cadefrecitinib Chemical Structure

No. CAS: 2308520-97-8

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Precio

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Amount: USD 0.00

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
- Ensayo clínico
Chemical Information
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

Tyk2

2.3 nM (IC₅₀)

JAK1

38 nM (IC₅₀)

JAK2

7.3 nM (IC₅₀)

JAK3

374 nM (IC₅₀)

Ver todos los productos específicos de isoformas JAK :

In Vitro

Cadefrecitinib (GLPG3667) shows dose-dependent inhibition of IFNα-induced STAT1 phosphorylation, demonstrating its selectivity and potency against TYK2 in relevant assays (PBMC and whole blood). In human peripheral blood mononuclear cells (PBMCs), the IC₅₀ values for JAK1/TYK2, JAK1/JAK3, and JAK2 are 70 nM, 1113 nM, and 1022 nM, respectively. Its potency is notably higher in the TYK2-dependent pathway compared to JAK1 and JAK2 pathways, confirming its selective TYK2 inhibition profile^[1].

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

Parmacokinetics

Species	Dose	Route	Clearance (CL)	V_d	T_1/2	Bioavailability	AUC	Plasma Concentration	T_max
Mice^[1]	1 mg/kg	i.v.	0.82 (9.9) L/h/kg	1.9 L/kg	1.6 h	/	/	/	/
Mice^[1]	5 mg/kg	p.o.	/	/	/	45 %	2744 ng·h/mL	1570 ng/mL	1.5 h

In Vivo

Cadefrecitinib (GLPG3667) (3-30 mg/kg; oral administration, once daily (q.d.); for 5 days) reduces dermal ear inflammation in an IL-23-induced in vivo mouse model of psoriasis^[1].

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

Animal Model:

Female BALB/c mice (IL-23-induced psoriasis model)^[1]
Dosage:

3, 10, and 30 mg/kg (Solutol HS15/methyl cellulose 0.5% (2/98; v/v))
Administration:

Oral administration, once daily (q.d.); for 5 days
Result:

Successfully reduced ear pinna thickening and STAT3 phosphorylation in the epidermis and dermis. Additionally, reduced neutrophil infiltration in the dermis. However, there was no clear dose-response relationship observed, likely due to other pathways not impacted by TYK2 inhibition.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 2308520-97-8
Appearance Solid
Peso molecular 443.46
Fòrmula C₂₂H₂₁N₉O₂
Color Off-white to light yellow
SMILES

N#CC1=NC=C(C(C)=C1)OC2=CC(NC3=NN=C(N4CCOCC4)C=C3)=C(N=CN5C)C5=N2
Synonyms

GLPG3667
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvente y solubilidad

In Vitro:

DMSO : 50 mg/mL (112.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.2550 mL

11.2750 mL

22.5499 mL

5 mM

0.4510 mL

2.2550 mL

4.5100 mL

10 mM

0.2255 mL

1.1275 mL

2.2550 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (274 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Mammoliti O, et al. Discovery of GLPG3667, a Selective ATP Competitive Tyrosine Kinase 2 Inhibitor for the Treatment of Autoimmune Diseases. J Med Chem. 2024 Jun 13;67(11):8545-8568. [Content Brief]

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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2550 mL	11.2750 mL	22.5499 mL	56.3749 mL
	5 mM	0.4510 mL	2.2550 mL	4.5100 mL	11.2750 mL
	10 mM	0.2255 mL	1.1275 mL	2.2550 mL	5.6375 mL
	15 mM	0.1503 mL	0.7517 mL	1.5033 mL	3.7583 mL
	20 mM	0.1127 mL	0.5637 mL	1.1275 mL	2.8187 mL
	25 mM	0.0902 mL	0.4510 mL	0.9020 mL	2.2550 mL
	30 mM	0.0752 mL	0.3758 mL	0.7517 mL	1.8792 mL
	40 mM	0.0564 mL	0.2819 mL	0.5637 mL	1.4094 mL
	50 mM	0.0451 mL	0.2255 mL	0.4510 mL	1.1275 mL
	60 mM	0.0376 mL	0.1879 mL	0.3758 mL	0.9396 mL
	80 mM	0.0282 mL	0.1409 mL	0.2819 mL	0.7047 mL
	100 mM	0.0225 mL	0.1127 mL	0.2255 mL	0.5637 mL

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Cadefrecitinib

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High-Throughput Bioactive Compound Library

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Posttranslational Modification Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Ver todos los productos específicos de isoformas JAK

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Cadefrecitinib Related Classifications

HY-156961 Related Classifications