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)).
For research use only. We do not sell to patients.
- CAS No.: 3049086-75-8
- Formula: C52H57ClFN9O6
- Molecular Weight:958.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
86 nM
Compound: 3e
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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
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[PMID: 37119666] |
| JeKo-1 | IC50 |
38.1 nM
Compound: 3e
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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
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[PMID: 37119666] |
| OCI-Ly10 | IC50 |
2.3 nM
Compound: 3e
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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
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[PMID: 37119666] |
| TMD8 | IC50 |
4.5 nM
Compound: 3e
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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
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[PMID: 37119666] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:The male Balb/c mice[1]
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Dosage:a single dose 2 mg/kg or 100 mg/kg, 5% DMSO, 10% Solutol, 85% saline
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Administration:Intravenous injection (i.v.); Oral gavage (p.o.)
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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.
Chemical Information
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CAS No. 3049086-75-8
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Molecular Weight 958.52
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Formula C52H57ClFN9O6
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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