2. PI3K/Akt/mTOR Cell Cycle/DNA Damage Cytoskeleton
  3. PI3K mTOR Akt CDK Cadherin
  4. PI3Kα-IN-29

PI3Kα-IN-29 is a potent, orally active and selective PI3Kα with an IC50 of 2.5 nM. PI3Kα-IN-29 exhibits >400-fold selectivity over PI3Kβ/δ/γ/mTOR. PI3Kα-IN-29 selectively degrades the H1047R mutant p110α protein and inhibits PI3Kα kinase activity. PI3Kα-IN-29 suppresses PI3K/AKT/mTOR signaling, induces G1 arrest, and inhibits migration. PI3Kα-IN-29 inhibits tumor growth in a T47 mouse model. PI3Kα-IN-29 can be used for the research of breast cancer.

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

PI3Kα-IN-29

PI3Kα-IN-29 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

PI3Kα-IN-29 Related Antibodies

Top Publications Citing Use of Products

View All PI3K Isoform Specific Products:

View All Isoforms
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

View All mTOR Isoform Specific Products:

View All Isoforms
mTOR mTORC1 mTORC2

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PI3Kα-IN-29 is a potent, orally active and selective PI3Kα with an IC50 of 2.5 nM. PI3Kα-IN-29 exhibits >400-fold selectivity over PI3Kβ/δ/γ/mTOR. PI3Kα-IN-29 selectively degrades the H1047R mutant p110α protein and inhibits PI3Kα kinase activity. PI3Kα-IN-29 suppresses PI3K/AKT/mTOR signaling, induces G1 arrest, and inhibits migration. PI3Kα-IN-29 inhibits tumor growth in a T47 mouse model. PI3Kα-IN-29 can be used for the research of breast cancer[1].

IC50 & TargetHY-179623

PI3Kα

2.5 nM (IC50)

PI3Kβ

>1000 nM (IC50)

PI3Kδ

>1000 nM (IC50)

PI3Kγ

>1000 nM (IC50)

In Vitro

PI3Kα-IN-29 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: T47D, MCF7
Concentration: T47D: 0, 100, 500 nM
MCF7: 0, 1.25, 5 µM
Incubation Time: 24 h
Result: Concentration-dependently induced G1 phase arrest both in T47D and MCF7 celss.
Increased G1 population to 71.8% and 60.2% in T47D at 500 and 100 nM, respectively.
In MCF7 cells, a similar G1 arrest pattern was observed at 1.25 and 5 µM.

Western Blot Analysis[1]

Cell Line: T47D, RKO, HCT116, SKOV3, SKBR3, PC3, MCF10A and MCF7
Concentration: 0, 0.5, 1, 5 μM
Incubation Time: 24 h
Result: Concentration-dependently suppressed phosphorylation of AKT (Ser473) in all tested cell lines.
Selectively induced degradation of mutant PI3Kα protein (H1047R) in a concentration-dependent manner, with the most pronounced effect in T47D cells.\r
Significant degradation was also observed in other PIK3CA-mutant lines: RKO, HCT116 (colorectal cancer), and SKOV3 (ovarian cancer).
No degradation was observed in wild-type (SKBR3, MCF10A) or E545K-mutant (MCF7) cell lines.

Cell Migration Assay [1]

Cell Line: MCF7
Concentration: 125, 250, 500 nM
Incubation Time: 0, 12, 24 h
Result: Significantly suppressed MCF7 cell migration, with minimal wound closure observed even at low concentrations after 24 h.

Western Blot Analysis[1]

Cell Line: T47D, MCF7
Concentration: 0, 0.1, 0.5, 1, 2 μM
Incubation Time: 24 h
Result: Upregulated p27 expression, and downregulated E-cadherin expression.
Demonstrated concentration-dependent suppression of retino-blastoma (RB) protein phosphorylation, with concomitant RB degradation observed at higher concentrations.

Cell Proliferation Assay[1]

Cell Line: MCF7
Concentration: 125, 250, 500 nM, 1 and 2 μM
Incubation Time: 14 days
Result: Concentration-dependently inhibited colony formation in MCF7 cells.
Achieved near‑complete suppression at higher concentrations (≥1 µM).
Parmacokinetics
Species Dose Route Cmax AUC0-t AUC0-∞ T1/2 Vd/F CL/F MRT0-∞ Tmax F
Rat[1] 2 mg/kg i.v. 3030.81 ng/mL 1290.94 ng·h/mL 1296.47 ng·h/mL 4.52 h 10.04 L/kg 1.56 L/h/kg 2.21 h / /
Rat[1] 20 mg/kg i.g. 484.67 ng/mL 2750.11 ng·h/mL 2755.76 ng·h/mL 2.72 h 29.36 L/kg 7.42 L/h/kg 4.30 h 3.00 h 21.30 %
In Vivo

PI3Kα-IN-29 (50 and 100 mg/kg, p.o., once daily for 21 days) demonstrates potent in vivo antitumor efficacy alongside a favorable safety profile in a T47D xenograft mouse model[1].
PI3Kα-IN-29 (500, 1000, and 1500 mg/kg, i.g., single dose) demonstrates a favorable safety profile in ICR mice[1].

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

Animal Model: BALB/c nude mice subcutaneously inoculated with T47D cells[1]
Dosage: 50 and 100 mg/kg
Administration: p.o., once daily for 21 days
Result: Achieved 70.7% and 52.3% tumor growth inhibition (TGI) at 100 and 50 mg/kg, respectively.
Showed a marked tumor regression at 100 mg/kg.
Showed no significant changes in body weight and no apparent histopatho-logical abnormalities.
Dose-dependently reduced Ki67 expression and phosphorylation of AKT.
Animal Model: ICR mice[1]
Dosage: 500, 1000, and 1500 mg/kg
Administration: i.g., single dose
Result: Revealed no significant body weight loss roup throughout the 14-day period.
Showed no inflammatory infiltration or organ-specific lesions in all major organs.
Molecular Weight

391.38

Formula

C20H17N5O4
SMILES

C[C@H](OC1=CC=C2C3=NC(C4=CC5=C(C=C4)OC(N)=N5)=CN3COC2=C1)C(N)=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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

PI3Kα-IN-29 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

PI3Kα-IN-29PI3KmTORAktCDKCadherinPhosphoinositide 3-kinaseMammalian target of RapamycinPKBProtein kinase BCyclin dependent kinaseMCF7migration inhibitionalpelisibH1047R mutant p110αhyperglycemiaPI3Kα IC50tumor growth inhibitionT47DpharmacokineticsPI3KαPI3Kα-selective inhibitorG1 arrestInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PI3Kα-IN-29
Cat. No.:
HY-179623
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.