2. PROTAC PI3K/Akt/mTOR
  3. PROTACs PI3K
  4. 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.

PROTAC PI3Kα/δ degrader-1

PROTAC PI3Kα/δ degrader-1 Chemical Structure

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PROTAC PI3Kα/δ degrader-1 Related Antibodies

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Description

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[1]. (Pink: PI3Kα and PI3Kδ ligand (HY-182086); Blue: Cereblon ligand (HY-A0003); Black: linker (HY-W105727)).

IC50 & Target[1]

PI3Kα

0.34 nM (IC50)

PI3Kβ

7.02 nM (IC50)

PI3Kδ

1.85 nM (IC50)

PI3Kγ

1.95 nM (IC50)

Cereblon

 

In Vitro

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.

PROTAC PI3Kα/δ degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: T47D cells
Concentration: 0.002-100 nM
Incubation Time: 8 h
Result: Induced dose-dependent degradation of PI3Kα in T47D cells, with a DC50 of 0.05 nM.

Cell Migration Assay[1]

Cell Line: MCF7 breast cancer cells
Concentration: 10, 50 nM
Incubation Time: 12-24 h
Result: Significantly inhibited MCF7 cell migration into the wound area.

Cell Cycle Analysis[1]

Cell Line: T47D breast cancer cells
Concentration: 0.1, 1, 10 nM
Incubation Time: 24 h
Result: Induced G1 phase cell cycle arrest in a dose-dependent manner, with 10 nM increasing G1 phase cells to 80.1%.
In Vivo

PROTAC PI3Kα/δ degrader-1 (20-40 mg/kg; i.p./p.o.; once daily; 21 days) significantly inhibits the growth of T47D and MCF7 breast cancer xenografts in BALB/c nude mice[1].

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

Animal Model: BALB/c nude mice (female, tumor-bearing, n=5 per group)[1]
Dosage: 20 mg/kg; 40 mg/kg
Administration: i.p.; once daily; 21 days; p.o.; once daily; 21 days
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.
Molecular Weight

877.00

Formula

C45H56N12O7
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
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 PI3Kα/δ degrader-1 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.

Keywords:

PROTAC PI3Kα/δ degrader-1PROTACsPI3KPhosphoinositide 3-kinasePI3Kα/δ PROTAC degraderT47D cellsMCF7 cellsBALB/c nude micebreast cancerInhibitorinhibitorinhibit

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