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Cat. No.: HY-153322

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ITK degrader 2

ITK degrader 2 is an orally active ITK PROTAC degrader with a DC₅₀ < 0.001 nM. ITK degrader 2 degrades ITK via the ubiquitin-proteasome pathway. ITK degrader 2 can be used in the research of cancer, autoimmune diseases and inflammatory diseases.

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

CAS No.: 2858738-65-3
Formula: C₄₁H₄₉F₂N₉O₃
Molecular Weight:753.88

Storage:

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

Data Sheet (266 KB)

ITK degrader 2 Chemical Structure

CAS No.: 2858738-65-3

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Use of MCE Products

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

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

All PROTACs Isoforms :

In Vitro

ITK degrader 2 (compound 30) (1 pM-0.512 μM; 4 h) induces degradation of ITK in C-terminal HiBiT-tagged Molt4 cells with a DC₅₀ < 0.001 nM and a D_max of 85%.^[1].

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

In Vivo

ITK degrader 2 (Compound 30) (6, 24 h) exhibits oral pharmacokinetic properties in mice, with a C_max of 0.87 μM, a T_max of 2 h, and an AUC_Last of 1.25 h·μM^[1].

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

Chemical Information

CAS No. 2858738-65-3
Molecular Weight 753.88
Formula C₄₁H₄₉F₂N₉O₃
SMILES

C[C@@]12[C@@](CC3=C(NN=C3C(NC4=C5)=CC4=CC=C5N(C)C([C@@H](N6CCN(CC6)CC7CCN(C8=CC=C(C9C(NC(CC9)=O)=O)C=N8)CC7)C)=O)C2)([H])C1(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (266 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]. Wegrzyniak, et al. Substituted piperidinedione and dioxotetrahydropyrimidine compounds for inhibiting or degrading target proteins, compositions, comprising the same, methods of their making, and methods of their use. World Intellectual Property Organization, WO2022235698 A1 2022-11-10.

Calculators

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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.

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100 mg

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