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Art. -Nr.: HY-155072

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PROTAC BTK Degrader-5

PROTAC BTK degraders-5(compound 3e) is a selective BTK PROTAC degrader with a DC₅₀ value of 7.0 nM in JeKo-1 cells. PROTAC BTK degraders-5 has no off-target effect on degrading CRBN neosubstates. PROTAC BTK degraders-5 has anti-proliferation effect on various lymphoma tumor cells and can be used in chronic lymphoid malignancies research.
(Pink: Btk ligand (HY-150898); Blue: Cereblon ligand (HY-W440230); Black: linker (HY-168297)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 3049086-75-8
Formel: C₅₂H₅₇ClFN₉O₆
Molecular Weight:958.52

Speicherung:

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

Data Sheet (268 KB)

PROTAC BTK Degrader-5 Chemical Structure

CAS. Nr.: 3049086-75-8

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Use of MCE Products

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

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

Biologische Aktivität

Beschreibung

PROTAC BTK degraders-5(compound 3e) is a selective BTK PROTAC degrader with a DC₅₀ value of 7.0 nM in JeKo-1 cells. PROTAC BTK degraders-5 has no off-target effect on degrading CRBN neosubstates. PROTAC BTK degraders-5 has anti-proliferation effect on various lymphoma tumor cells and can be used in chronic lymphoid malignancies research^[1]. (Pink: Btk ligand (HY-150898); Blue: Cereblon ligand (HY-W440230); Black: linker (HY-168297)).

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	86 nM Compound: 3e	Antiproliferative activity against mouse BaF3 cells expressing BTK C481S mutant assessed as inhibition of cell growth measured after 3 days by CCK-8 assay Antiproliferative activity against mouse BaF3 cells expressing BTK C481S mutant assessed as inhibition of cell growth measured after 3 days by CCK-8 assay	[PMID: 37119666]
JeKo-1	IC₅₀	38.1 nM Compound: 3e	Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth measured after 3 days by CCK-8 assay Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth measured after 3 days by CCK-8 assay	[PMID: 37119666]
OCI-Ly10	IC₅₀	2.3 nM Compound: 3e	Antiproliferative activity against human OCILY10 cells assessed as inhibition of cell growth measured after 3 days by CCK-8 assay Antiproliferative activity against human OCILY10 cells assessed as inhibition of cell growth measured after 3 days by CCK-8 assay	[PMID: 37119666]
TMD8	IC₅₀	4.5 nM Compound: 3e	Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth measured after 3 days by CCK-8 assay Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth measured after 3 days by CCK-8 assay	[PMID: 37119666]

In Vitro

PROTAC BTK Degrader-5 (Compound 3e) (1.6~1000 nM; 24 h) induces BTK degradation with DC₅₀ value of 7.0 nM in JeKo-1 cells^[1].
PROTAC BTK Degrader-5 (100 and 1000 nM) possesses the metabolic stability with the T_1/2 of 145 min^[1].
PROTAC BTK Degrader-5 (100 nM;12 h) induced - BTK degradation blocks by proteasome inhibitor MG - 132 (HY-13259) (5 μM)^[1].
PROTAC BTK Degrader-5 (1.6~1000 nM; 24 h) has no effect on the levels of IKZF1 and GSPT1 and mild effect on the level of IKZF3^[1].
PROTAC BTK Degrader-5 (72 h) has anti- proliferation effect in OCI-ly10, TMD8, JeKo-1 and BTK ^C481S Ba/F3 cells with the IC₅₀ values of 2.3, 4.5, 38.1 and 86.0 nM, which were higher than Ibrutinib (HY-10997)(IC₅₀ value of 4.5, 4.7, 79.8, and 1546.0 nM, respectively)^[1].

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

In Vivo

PROTAC BTK Degrader-5 (2 mg/kg for i.v, sigle dose) is metabolically stable in mice^[1].

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

Animal Model:

The male Balb/c mice^[1]
Dosage:

a single dose 2 mg/kg or 100 mg/kg, 5% DMSO, 10% Solutol, 85% saline
Administration:

Intravenous injection (i.v.); Oral gavage (p.o.)
Result:

Maintained above 10 nM for at least 4 h after administration of PROTAC BTK Degrader-5 at a single dose of 2 mg/kg via intravenous (IV) injection in the plasma (the effective BTK degradation DC₅₀50 = 7.0nM).
Had poor oral bioavailability at a dose of 100 mg/kg.

Related Protocols :

Cell Viability Determination by MTT Colorimetric Assay

Chemical Information

CAS. Nr. 3049086-75-8
Molecular Weight 958.52
Formel C₅₂H₅₇ClFN₉O₆
SMILES

O=C(C1=C(Cl)C=C(OC2=CC=CC=C2)C=C1)C3=CNC4=NC=NC(N[C@@H]5CC[C@H](NC(CC6CCN(CCC7CCN(C8=C(F)C=C(C(N(C9CCC(NC9=O)=O)C%10)=O)C%10=C8)CC7)CC6)=O)CC5)=C43
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 (268 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]. Song Chen, et al. Discovery of novel BTK PROTACs with improved metabolic stability via linker rigidification strategy. European Journal of Medicinal Chemistry.Volume 255, 5 July 2023, 115403.

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

Keywords

MOQ

Minimum order quantity

100 mg

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