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Cat. No.: HY-189880

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PI3Kα-IN-36

PI3Kα-IN-36 is a selective and orally active PI3Kα^H1047R inhibitor with a pAKT inhibition IC₅₀ of 96 nM in T47D cells. PI3Kα-IN-36 selectively inhibits T47D cell proliferation with an IC₅₀ of 65 nM. PI3Kα-IN-36 achieves 81% tumor growth inhibition in a T47D xenograft mouse model. PI3Kα-IN-36 can be used in research related to PI3Kα^H1047R mutation-driven tumors.

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

Formula: C₂₃H₂₄ClN₅O₃
Molecular Weight:453.92

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

PI3Kα-IN-36 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
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Classifications
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Biological Activity

Description

IC₅₀ & Target

^[1]

PI3Kα-H1047R

96 nM (IC₅₀)

All PI3K Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
T47D	IC50	96 nM	Inhibition of pAKT levels in human T47D cells measured by HTRF assay. Inhibition of pAKT levels in human T47D cells measured by HTRF assay.	acs.jmedchem.6c00269
T47D	IC50	65 nM	Antiproliferative activity against human T47D cells assessed as viability reduction by CTG assay. Antiproliferative activity against human T47D cells assessed as viability reduction by CTG assay.	acs.jmedchem.6c00269
SK-BR-3	IC50	23000 nM	Antiproliferative activity against human SKBR3 cells assessed as viability reduction by CTG assay. Antiproliferative activity against human SKBR3 cells assessed as viability reduction by CTG assay.	acs.jmedchem.6c00269

In Vitro

Anti-cancerOthers

Anti-cancer

PI3Kα-IN-36 inhibits pAKT in T47D cells with an IC₅₀ of 96 nM and shows >60-fold selectivity over SKBR3 cells; it inhibits T47D cell proliferation with an IC₅₀ of 65 nM and shows >100-fold selectivity over SKBR3 cells; it has a high protein binding rate (free fraction of 0.2%) and a high intrinsic clearance in human liver microsomes (17 mL/min/kg)^[1].

Others

PI3Kα-IN-36 (compound 34) (3 μM) produces ≥50% inhibition of only two wild-type kinases in a panel of 197 kinases and shows weak activity against 14 of 78 safety panel targets^[1].
PI3Kα-IN-36 (2-24 h) shows time-dependent pAKT inhibition, with a fivefold increase in potency from 2 h to 20 h, and sustained pAKT inhibition for up to 6 h after washout^[1].

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

In Vivo

Anti-cancerCarbohydrate Metabolism

Anti-cancer

PI3Kα-IN-36 (compound 34) (100-250 mg/kg; p.o.; single administration) produces maximum pAKT target engagement at 4 h after dosing in the T47D xenograft tumor model, with near-complete pAKT reduction at 250 mg/kg^[1].

Anti-cancer

Carbohydrate Metabolism

PI3Kα-IN-36 (100-250 mg/kg; p.o.; BID or QD; 14 days) produces measurable tumor growth inhibition in the T47D xenograft tumor model, with an optimal TGI of 81% at 175/150 mg/kg BID, while showing no elevation of serum insulin or blood glucose^[1].

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

Related Protocols :

Chemical Information

Molecular Weight 453.92
Formula C₂₃H₂₄ClN₅O₃
SMILES

O=C(O)C1=NC(Cl)=CC=C1N[C@@H](C2=CC(C)=CC3=C2N=C(N4C[C@]5([H])C[C@]5([H])C4)N(C)C3=O)C
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

Handling Instructions (2659 KB)

References

[1]. Chen C, et al. Discovery of Tetrasubstituted Quinazolin‑4(3H)‑ones as Wild‑type‑sparing, Highly Selective PI3Kα^H1047R Inhibitors. Journal of Medicinal Chemistry. 2026;69(19):21747‑2176

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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PI3Kα-IN-36

All PI3K Isoforms

Biological Activity

Description

IC50 & Target

Cellular Effect

In Vitro

In Vivo

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PI3Kα-IN-36 Related Classifications

HY-189880 Related Classifications

Bioz

Keywords

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