PROTAC PI3Kα/δ degrader-1
PROTAC PI3Kα/δ degrader-1 is an orally active PI3Kα/δ PROTAC degrader, with an IC50 of 0.34 nM for PI3Kα and 1.85 nM for PI3Kδ. PROTAC PI3Kα/δ degrader-1 inhibits the proliferation and migration of cancer cells, induces G1-phase cell cycle arrest and PI3Kα degradation. PROTAC PI3Kα/δ degrader-1 suppresses tumor growth in breast cancer xenograft mouse models. PROTAC PI3Kα/δ degrader-1 can be used for the research of breast cancer.
(Pink: PI3Kα and PI3Kδ ligand (HY-182086); Blue: Cereblon ligand (HY-A0003); Black: linker (HY-W105727)).
For research use only. We do not sell to patients.
- Formula: C45H56N12O7
- Molecular Weight:877.00
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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PI3Kα 0.34 nM (IC50) |
PI3Kβ 7.02 nM (IC50) |
PI3Kδ 1.85 nM (IC50) |
PI3Kγ 1.95 nM (IC50) |
Cereblon |
PROTAC PI3Kα/δ degrader-1 (Compound D5) inhibits the enzymatic activities of PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, with IC50 values of 0.34, 7.02, 1.85, and 1.95 nM, respectively[1].
PROTAC PI3Kα/δ degrader-1 (72 h) potently inhibits the proliferation of T47D cells (IC50 = 0.06 nM) and MCF7 cells (IC50 = 2.65 nM)[1].
PROTAC PI3Kα/δ degrader-1 (0.002-100 nM; 8 h) induces potent, dose-dependent degradation of PI3Kα in T47D cells, with a DC50 of 0.05 nM[1].
PROTAC PI3Kα/δ degrader-1 (1-10 nM; 2 weeks) inhibits colony formation of MCF7 breast cancer cells[1].
PROTAC PI3Kα/δ degrader-1 (10-50 nM; 12-24 h) inhibits the migration of MCF7 breast cancer cells, as detected by scratch wound healing assay[1].
PROTAC PI3Kα/δ degrader-1 (0.1-10 nM; 24 h) induces dose-dependent G1-phase cell cycle arrest in T47D breast cancer cells, with the arrest effect peaking at 10 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:T47D cells
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Concentration:0.002-100 nM
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Incubation Time:8 h
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Result:Induced dose-dependent degradation of PI3Kα in T47D cells, with a DC50 of 0.05 nM.
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Cell Line:MCF7 breast cancer cells
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Concentration:10, 50 nM
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Incubation Time:12-24 h
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Result:Significantly inhibited MCF7 cell migration into the wound area.
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Cell Line:T47D breast cancer cells
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Concentration:0.1, 1, 10 nM
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Incubation Time:24 h
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Result:Induced G1 phase cell cycle arrest in a dose-dependent manner, with 10 nM increasing G1 phase cells to 80.1%.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (female, tumor-bearing, n=5 per group)[1]
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Dosage:20 mg/kg; 40 mg/kg
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Administration:i.p.; once daily; 21 days; p.o.; once daily; 21 days
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Result:Significantly reduced tumor volume compared to the control group.
Showed no significant body weight loss in any treated group.
Significantly inhibited the growth of MCF7 breast cancer xenografts.
Chemical Information
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Molecular Weight 877.00
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Formula C45H56N12O7
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SMILES
NC(N=C1)=NC=C1C(NC(N2C3=NCC2)=NC4=C3C=CC(OCCCN5CCN(CCCCCCCCC(NC6=C(CN(C7CCC(NC7=O)=O)C8=O)C8=CC=C6)=O)CC5)=C4OC)=O
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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)
PROTAC PI3Kα/δ degrader-1 Related Classifications
HY-182083 Related Classifications
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