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Art. -Nr.: HY-149917

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PROTAC ITK degrader 1

Name: PROTAC ITK degrader 1
Brand: MedChemExpress
SKU: HY-149917
Price: 340.00 USD
Availability: InStock
Rating: 5 (1 reviews)

PROTAC ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC₅₀=3.6 nM in vivo in mice), with good plasma exposure levels. PROTAC ITK degrader 1 induces rapid, and prolonged ITK degradation and suppresses IL-2 secretion (EC₅₀=35.2 nM, Jurkat cells) stimulated by anti-CD3 antibodyin vivo.
(Pink: Itk ligand (HY-168387); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-168388)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₄₈H₅₇F₃N₁₀O₇
Molecular Weight:943.02

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (271 KB)

PROTAC ITK degrader 1 Chemical Structure

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

PROTAC ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC₅₀=3.6 nM in vivo in mice), with good plasma exposure levels. PROTAC ITK degrader 1 induces rapid, and prolonged ITK degradation and suppresses IL-2 secretion (EC₅₀=35.2 nM, Jurkat cells) stimulated by anti-CD3 antibodyin vivo^[1]. (Pink: Itk ligand (HY-168387); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-168388)).

Alle PROTACs Isoform-spezifische Produkte anzeigen :

In Vitro

PROTAC ITK degrader 1 (compound 28) (0.001-3 μM; 12 h) dose-dependently decreases the protein levels of ITK in Jurkat cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

Jurkat cells
Concentration:

0.001 μM, 0.003 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM
Incubation Time:

12 h
Result:

Exhibited strong ITK degradation potencies in a dose-dependent manner. Even rapidly led to significant ITK protein downregulation after 1 h incubation.

In Vivo

PROTAC ITK degrader 1 (compound 28) (20 mg/kg; ip; single dose) significantly degrades ITK protein 2 h, 8 h, and 16 h after treatment on mice. PROTAC ITK degrader 1 (25 mg/kg; ip; single dose) also inhibits inhibits IL-2 secretion 6 h after treatment in vivo in anti-CD3 monoclonal antibody (mAb)-induced IL-2 mouse model^[1].

Pharmacokinetic Analysis in Balb/c Mice^[1]

Route	Dose (mg/kg)	AUC_0-t (ng·h/mL)	AUC_0-∞ (ng·h/mL)	T_1/2 (h)	V_z (L/kg)	Cl (mL/min/kg)	C_max (ng/mL)	MRT_last (h)	Bioavailability (%)
i.v.	5	15138	15415	4.39	2057	5.4	4910	4.42	/
ip	10	25931	27261	5.75	3055	6.1	3423	5.84	88.4%

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

Animal Model:

Balb/c mice, and anti-CD3 mAb-induced IL-2 mouse model^[1]
Dosage:

20 mg/kg, 25 mg/kg
Administration:

IP; singel dose
Result:

Successfully delivered to the peripheral blood and spleen tissue, eliciting efficient, rapid, and prolonged ITK degradation starting at 2 h and lasting for at least 16 h with 20 mg/kg dose in Balb/c mice.
Efficiently suppressed the production of cytokine IL-2, resulting in a reduction of over 70% compared to the vehicle group with 25 mg/kg dose.

Chemical Information

Molecular Weight 943.02
Formel C₄₈H₅₇F₃N₁₀O₇
SMILES

O=C(NC1=CN([C@@H](CCN2CCN(CCC3CCN(C4=CC=C(C(N(C5CCC(NC5=O)=O)C6=O)=O)C6=C4)CC3)CC2)C7=CC=CC=C7)N=C1)C8=NNC9=C8CCC(C)(C)C9.OC(C(F)(F)F)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 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)

Verweise

[1]. Zhou D, et al. Discovery of Potent and Highly Selective Interleukin-2-Inducible T-Cell Kinase Degraders with In Vivo Activity. J Med Chem. 2023 Apr 13;66(7):4979-4998. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Bioz

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MOQ

Minimum order quantity

100 mg

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