2. PROTAC PI3K/Akt/mTOR
  3. PROTACs PI3K
  4. PROTAC PI3Kα degrader-1

PROTAC PI3Kα degrader-1 is a PI3Kα PROTAC degrader (DC50 = 0.08 μM), demonstrating good selectivity for PI3Kα degradation over PI3Kβ, PI3Kγ, and PI3Kδ. PROTAC PI3Kα degrader-1 effectively degrades PI3Kα in a time- and concentration-dependent, over PI3Kβ, PI3Ky and PI3Kδ, and potently inhibited the phosphorylation of AKT at the Ser473site. PROTAC PI3Kα degrader-1 shows significant in vivo anticancer efficacy in HGC-27 and DOHH2 xenograft models. (Pink: PI3Kα ligand : (HY-174798), Blue: E3 ligase CRBN Ligand (HY-10984), Black: Linker, E3 ligase ligand-linker conjugate (HY-W940885)).

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

PROTAC PI3Kα degrader-1 Chemical Structure

PROTAC PI3Kα degrader-1 Chemical Structure

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PROTAC PI3Kα degrader-1 Related Antibodies

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Description

PROTAC PI3Kα degrader-1 is a PI3Kα PROTAC degrader (DC50 = 0.08 μM), demonstrating good selectivity for PI3Kα degradation over PI3Kβ, PI3Kγ, and PI3Kδ. PROTAC PI3Kα degrader-1 effectively degrades PI3Kα in a time- and concentration-dependent, over PI3Kβ, PI3Ky and PI3Kδ, and potently inhibited the phosphorylation of AKT at the Ser473site. PROTAC PI3Kα degrader-1 shows significant in vivo anticancer efficacy in HGC-27 and DOHH2 xenograft models. (Pink: PI3Kα ligand : (HY-174798), Blue: E3 ligase CRBN Ligand (HY-10984), Black: Linker, E3 ligase ligand-linker conjugate (HY-W940885))[1].

IC50 & Target[1]

Cereblon

 

PI3Kα

62 nM (IC50)

PI3Kβ

293.94 nM (IC50)

PI3Kγ

>10000 nM (IC50)

PI3Kδ

42.10 (IC50)

In Vitro

PROTAC PI3Kα degrader-1 (Compound 12) (1 μM) shows negligible activity against 79 kinases (< 20% inhibition) while exhibits potent inhibition of PIK3CA (＞ 95%) in T47D breast cancer cells[1].

PROTAC PI3Kα degrader-1 (0.1-10 μM) demonstrates good selectivity for PI3Kα degradation over PI3Kβ, PI3Kγ and PI3Kδ in T47D breast cancer cells[1].

PROTAC PI3Kα degrader-1 exhibits excellent selectivity for the degradation of PI3Kα in various cancer cell lines, with IC50s of 0.35 μM (T47D), 1.64 μM (MDA-MB-453), 1.45 μM (HGC-27), 0.37 μM (AGS), 3.38 μM (LNCaP), 1.48 μM (PC3) and 0.69 μM (Pfeiffer)[1].

PROTAC PI3Kα degrader-1 (0.0032-10 μM, 0-24 h) degrades PI3Kα in a concentration- and time-dependent manner in T47D and HGC-27 cells[1].

PROTAC PI3Kα degrader-1 (1 μM, 20 h) degrades PI3Kα via the ubiquitin-proteasome pathway through CRBN recruitment in T47D cells[1].

PROTAC PI3Kα degrader-1 (0.1-10 μM, 24 h) induces cell cycle arrest at the G2/M phase concentration-dependently in T47D cells[1].

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

PROTAC PI3Kα degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: T47D cells
Concentration: 1 μM
Incubation Time: 20h with/without MG132 (HY-13259) (1 μM)
Result: Reduced the level of PI3Kα, while the addition of MG132 restored PI3Kα levels.

RT-PCR[1]

Cell Line: T47D cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Did not decrease the mRNA levels of PIK3CA.

Western Blot Analysis[1]

Cell Line: T47D cells
Concentration: 1 μM
Incubation Time: 8 h after Thalidomide (HY-14658) (10 μM) preincubated 1h and then incubated in fresh medium for an additional 48 hours.
Result: Degraded PI3Kα but preincubation with thalidomide (10 μM, 1 h) reduced this degradation.
Restored PI3Kα expression to normal levels 48 h after an 8h treatment followed by incubation in fresh medium.
In Vivo

PROTAC PI3Kα degrader-1 (Compound 12) (2 μM, 0-60 min) shows superior plasma stability across all of the tested species including mice, rats, dogs, monkeys, and human[1].

PROTAC PI3Kα degrader-1 (2 μM, 0-60 min) exhibits moderate to high clearance rates in each species,with half-life (t1/2) values of 22.6 min (mouse), 45.7 min (rat), 67.6 min (dog), 32.5 min (monkey), and 34.7 min (human), which is heavily dependent on NADPH[1].

PROTAC PI3Kα degrader-1 (30-60 mg/kg, i.p., daily for 14 days) demonstrates significant anticancer efficacy in the HGC-27 xenograft model[1].

PROTAC PI3Kα degrader-1 (30 mg/kg, i.p., daily for 21 days) exhibits potent antitumor activity in the DOHH2 xenograft model[1].

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

Animal Model: Male BALB/c nude mice (20-22 g) bearing HGC-27 xenografts[1]
Dosage: 30, 60 mg/kg
Administration: i.p. daily for 14 days
Result: Showed tumor growth rates (TGI) of 38.3% at 30 mg/kg and 56.8% at 60 mg/kg.
Induced dose-dependent degradation of PI3Kα.
Showed no significant changes in body weight.
Animal Model: Male BALB/c nude mice (20-22 g) bearing DOHH2 xenografts[1]
Dosage: 30 mg/kg
Administration: i.p. daily for 21 days
Result: Demonstrated a strong efficacy with a tumor growth inhibition (TGI) rate of 61.8%, which is more effective than Ibrutinib (HY-10997) administered orally at a dose of 25 mg/kg and Idelalisib (HY-13026) administered orally at a dose of 10 mg/kg.
Showed no significant body weight loss.
Molecular Weight

897.99

Formula

C46H49F2N7O8S
SMILES

O=S(NC1=C(N=CC(C2=CC3=C(N=CN=C3C(OCCCCCCCCCCCCNC4=CC=CC(C(N5C6CCC(NC6=O)=O)=O)=C4C5=O)=C2)C)=C1)OC)(C7=CC=C(C=C7F)F)=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 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 degrader-1PROTACsPI3KPhosphoinositide 3-kinaseCancerHGC-27DOHH2PI3KαInhibitorinhibitorinhibit

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