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Cat. No.: HY-161373

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PI3Kα-IN-22

PI3Kα-IN-22 (Compound 17) is an orally active, potent and selective inhibitor of PI3Kα^H1047R, with an IC₅₀ of 1 nM for pAKT T47D AlphaLISA. PI3Kα-IN-22 can induce tumor regressions in the HCC1954 tumor model in mice.

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

CAS No.: 2925030-26-6
Formula: C₂₄H₂₃F₂N₅O₃
Molecular Weight:467.47

Storage:

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

Data Sheet (269 KB)

PI3Kα-IN-22 Chemical Structure

CAS No.: 2925030-26-6

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

Biological Activity
- Description
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

All PI3K Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
SK-BR-3	IC₅₀	8972 nM Compound: 17	Cytotoxicity against human SK-BR-3 cells harboring wildtype PI3Kalpha assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo 2.0 luminescent cell viability assay Cytotoxicity against human SK-BR-3 cells harboring wildtype PI3Kalpha assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo 2.0 luminescent cell viability assay	[PMID: 38477582]
T47D	IC₅₀	48 nM Compound: 17	Cytotoxicity against human T47D cells harboring PI3Kalpha H1047R mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo 2.0 luminescent cell viability assay Cytotoxicity against human T47D cells harboring PI3Kalpha H1047R mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo 2.0 luminescent cell viability assay	[PMID: 38477582]

Chemical Information

CAS No. 2925030-26-6
Molecular Weight 467.47
Formula C₂₄H₂₃F₂N₅O₃
SMILES

CC(C=C([C@H](NC1=CC=CC=C1C(O)=O)C)C2=NC(N3CCC(F)(F)CC3)=C4C#N)=CN2C4=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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Ketcham JM, et al. Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein. J Med Chem. 2024 Mar 28;67(6):4936-4949. [Content Brief]

Calculators

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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.

Keywords

100 mg

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