1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. PROTAC BTK Degrader-5

PROTAC BTK degraders-5(compound 3e) is a selective BTK 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 research1.

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

PROTAC BTK Degrader-5 Chemical Structure

PROTAC BTK Degrader-5 Chemical Structure

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Description

PROTAC BTK degraders-5(compound 3e) is a selective BTK 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 research1.

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 T1/2 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.
Molecular Weight

958.52

Formula

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

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
References
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PROTAC BTK Degrader-5 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
PROTAC BTK Degrader-5
Cat. No.:
HY-155072
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