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Cat. No.: HY-153536

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PROTAC BTK Degrader-3

PROTAC BTK Degrader-3 is an orally active PROTAC degrader targeting BTK, with a DC₅₀ value of 10.9 nM. PROTAC BTK Degrader-3 has an IC₅₀ of 6.3 nM against wild-type BTK and an IC₅₀ of 8 nM against BTK^C481S. PROTAC BTK Degrader-3 can be used in cancer-related research.
(Pink: Btk ligand (HY-150885); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W125996)).

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

CAS No.: 2563861-90-3
Formula: C₄₁H₄₀N₁₀O₅
Molecular Weight:752.82

Storage:

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

Data Sheet (276 KB)

PROTAC BTK Degrader-3 Chemical Structure

CAS No.: 2563861-90-3

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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
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

PROTAC BTK Degrader-3 is an orally active PROTAC degrader targeting BTK, with a DC₅₀ value of 10.9 nM. PROTAC BTK Degrader-3 has an IC₅₀ of 6.3 nM against wild-type BTK and an IC₅₀ of 8 nM against BTK^C481S. PROTAC BTK Degrader-3 can be used in cancer-related research^[1]. (Pink: Btk ligand (HY-150885); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W125996)).

All PROTACs Isoforms :

In Vitro

PROTAC BTK Degrader-3 (cpd 1) (48 h) has significant BTK degradation activity in Mino human mantle cell lymphoma cells, with a DC₅₀ of 10.9 nM^[1].
PROTAC BTK Degrader-3 has significant inhibitory activity against both BTK^wt and BTK^C481S kinases, with IC₅₀ values of 6.3 nM and 8 nM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

In Vivo

PROTAC BTK Degrader-3 (cpd 1) (3.8 mg/kg; administered via oral gavage; once daily for 3 consecutive days) induces significant degradation of BTK protein in the spleen of female ICR mice, with a DD₅₀ of 3.8 mg/kg^[1].
PROTAC BTK Degrader-3 (10 mg/kg; oral administration; single dose) exhibits oral absorption properties in male Beagle dogs, with a corresponding AUC_0-t value of 26900 pg/mL*h.

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

Chemical Information

CAS No. 2563861-90-3
Molecular Weight 752.82
Formula C₄₁H₄₀N₁₀O₅
SMILES

O=C1C2=CC=C(N3CC(C3)N4CC(C4)N5CCC(CC5)N6N=C(C7=C6N=CN=C7N)C8=CC=C(OC9=CC=CC=C9)C=C8)C=C2C(N1C%10C(NC(CC%10)=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 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]. Zhang C, et al. Salt of compound for degrading btk, crystal form thereof, and use thereof in medicine. WO2022052950A1. WIPO. 2022.

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.

Bioz

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100 mg

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