2. PI3K/Akt/mTOR
  3. PI3K Akt
  4. PI3Kα-IN-32

PI3Kα-IN-32 (Compound 11f) is a selective, orally active PI3Kα inhibitor, with an IC50 of 26.3 nM against PI3KαH1047R. PI3Kα-IN-32 inhibits AKT phosphorylation. PI3Kα-IN-32 exhibits anticancer activity against breast cancer. PI3Kα-IN-32 can be used in the research of HR+/HER2- breast cancer.

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

PI3Kα-IN-32

PI3Kα-IN-32 Chemical Structure

CAS No. : 3057582-20-1

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PI3Kα-IN-32 Related Antibodies

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Description

PI3Kα-IN-32 (Compound 11f) is a selective, orally active PI3Kα inhibitor, with an IC50 of 26.3 nM against PI3KαH1047R. PI3Kα-IN-32 inhibits AKT phosphorylation. PI3Kα-IN-32 exhibits anticancer activity against breast cancer. PI3Kα-IN-32 can be used in the research of HR+/HER2- breast cancer[1].

IC50 & Target[1]

PI3Kα-H1047R

26.3 nM (IC50)

PI3Kα

94.6 nM (IC50)

In Vitro

PI3Kα-IN-32 potently and selectively inhibits the enzymatic activity of the PI3KαH1047R mutant, with an IC50 of 26.3 nM[1].
PI3Kα-IN-32 (maximum 10 μM; 144 h) potently inhibits the proliferation of T47D HR+/HER2- breast cancer cells with an IC50 of 88.8 nM, and is 14.7-fold more selective for SK-BR-3 breast cancer cells expressing wild-type PI3Kα than for the former[1].
PI3Kα-IN-32 inhibits AKT phosphorylation in T47D HR+/HER2- breast cancer cells with an IC50 of 29.0 nM, and shows 5.8-fold selectivity for SK-BR-3 breast cancer cells expressing wild-type PI3Kα over the former[1].
PI3Kα-IN-32 (10 μM) exhibits high selectivity for PI3Kα, shows only weak activity against PI3Kδ and PIK3C3, and has no significant activity against the other 108 tested kinases[1].

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

PI3Kα-IN-32 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: T47D HR+/HER2- breast cancer cells, SK-BR-3 wild-type PI3Kα breast cancer cells
Concentration: 10 μM (max, serial 4-fold dilutions)
Incubation Time: 144 h
Result: Inhibited T47D cell proliferation with an IC50 of 88.8 nM.
Inhibited SK-BR-3 cell proliferation with an IC50 of 1307.5 nM, giving a T47D/SK-BR-3 selectivity ratio of 14.7.
Parmacokinetics
Species Dose Route Cmax AUC T1/2
Mice[1] 100 mg/kg p.o. 8830 ng/mL 61400 ng·h/mL 4.13 h
Rat[1] 100 mg/kg p.o. 25948 ng/mL 284091 ng·h/mL 5.04 h
In Vivo

PI3Kα-IN-32 (50-150 mg/kg; p.o.; once daily; 21 days) exhibits potent, dose-dependent antitumor activity in T47D xenograft mice[1].

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

Animal Model: BALB/c Nude (female, 6-8 weeks old, subcutaneous inoculation of T47D cells with 17β-estradiol tablet implantation)[1]
Dosage: 50 mg/kg; 100 mg/kg; 150 mg/kg
Administration: p.o.; QD; 21 days
Result: Produced 77% tumor growth inhibition (TGI = 0.77) at 50 mg/kg.
Attained complete tumor regression at 100 mg/kg (TGI = 1.06) and 150 mg/kg (TGI = 1.19).
Showed no significant body weight loss at all tested dosages.
Caused no significant changes in plasma insulin levels at 4 h and 24 h post-dose.
Decreased tumor p-AKT (Ser473) levels by over 90% within 4 h of oral administration.
Confirmed dose-dependent inhibition of AKT phosphorylation in tumor tissue after treatment.
Molecular Weight

487.45

Formula

C20H18F5N5O2S
CAS No.
SMILES

OC(C1)(C)CN1C(N=C2)=NC=C2NC(N[C@H](C3=C(C)C4=C(C(F)=CC(F)=C4)S3)C(F)(F)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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PI3Kα-IN-32 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:

PI3Kα-IN-323057582-20-1PI3KAktPhosphoinositide 3-kinasePKBProtein kinase BT47D HR+/HER2- breast cancer cellsPIK3CA H1047R mutant PI3KαT47D xenograft miceHEK 293 cellshERG channelsSD ratsSK-BR-3 breast cancer cellsCYP enzymesAKT phosphorylationHR+/HER2- breast cancerInhibitorinhibitorinhibit

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