Cat. No.: HY-150618

PI3Kα-IN-9

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

PI3Kα-IN-9 (compound 27) is a selective, long-acting and oral active PI3Kα inhibitor with IC₅₀ values of 4.4, 128, 146 and 153 nM for PI3Kα, PI3Kγ, PI3Kδ and PI3Kβ, respectively. PI3Kα-IN-9 has antiproliferative activity and induces apoptosis. PI3Kα-IN-9 can be used for cancer research.

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

CAS No.: 2715287-67-3
Formula: C₁₈H₂₁N₇O₃
Molecular Weight:383.40

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PI3Kα-IN-9 Chemical Structure

CAS No.: 2715287-67-3

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

PI3Kα

4.4 nM (IC₅₀)

PI3Kγ

128 nM (IC₅₀)

PI3Kδ

146 nM (IC₅₀)

PI3Kβ

153 nM (IC₅₀)

All PI3K Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	0.43 μM Compound: 27	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35834807]
K562	IC₅₀	0.43 μM Compound: 27	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35834807]
MCF7	IC₅₀	0.43 μM Compound: 27	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35834807]
MDA-MB-231	IC₅₀	0.43 μM Compound: 27	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35834807]
MGC-803	IC₅₀	0.43 μM Compound: 27	Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35834807]
MOLT-4	IC₅₀	0.43 μM Compound: 27	Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35834807]
PC-3	IC₅₀	0.43 μM Compound: 27	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35834807]
RPMI-8226	IC₅₀	0.43 μM Compound: 27	Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35834807]
SK-OV-3	IC₅₀	0.43 μM Compound: 27	Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35834807]
U-251	IC₅₀	0.43 μM Compound: 27	Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35834807]

In Vitro

PI3Kα-IN-9 (compound 27) (0-8 μM; 72 hours; cancer cell lines) has antiproliferative activity and induces apoptosis^[1].
PI3Kα-IN-9 (compound 27) (0-8 μM; MGC-803 cells) down-regulates the expression of PI3Kα protein, the proteins of PI3K downstream, p-AKT and p-P70S6 K^[1].

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

Cell Viability Assay^[1]

Cell Line:

MGC-803 (gastric cancer), SKOV-3 (ovarian cancer), PC-3(prostate cancer), MCF-7 (breast cancer), MDA-MB-231 (triple-negative breast cancer), HepG2 (liver cancer), RPMI8226 (multiple myeloma), K562 (chronic myeloid leukemia), U251 (glioma) and MOLT-4 (acute lymphoblastic leukemia) cell lines
Concentration:

0-2 μM
Incubation Time:

72 hours
Result:

Inhibited the growth of a variety of cancer cells with IC₅₀ values ranging from 0.43 to 1.33 μM.

Apoptosis Analysis^[1]

Cell Line:

MGC-803 cells
Concentration:

0, 2, 4 and 8 μM
Incubation Time:

36 hours
Result:

Increased the percentage of apoptotic cells from 12.07 to 61.69% in a dose-dependent manner.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	Clearance (CL)	F
Rat1	1 mg/kg	i.v.	6.29 h	0.03 h	454.7 ng/mL	2237 ng·h/mL	2922.4 ng·h/mL	343 mL/h/kg	/
Rat1	10 mg/kg	p.o.	﹥10 h	9.33 h	2256.7 ng/mL	36697 ng·h/mL	38114.3 ng·h/mL	/	130.4 %

In Vivo

PI3Kα-IN-9 (compound 27) (1-10 mg/kg; p.o. and i.v.; for 24 hours; male Sprague-Dawley rat) has favorable stability (T_1/2>10 h) and high bioavailability (130%)^[1].
PI3Kα-IN-9 (compound 27) (30 mg/kg; p.o.; daily, for 3 weeks; male BALB/c nude mice) has antitumor activity and low cytotoxicity^[1].

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

Animal Model:

Male BALB/c nude mice^[1]
Dosage:

30 mg/kg
Administration:

Oral administration; daily, for 3 weeks
Result:

Inhibited tumor growth with a tumor growth inhibition (TGI) rate of 41.5%.

Chemical Information

CAS No. 2715287-67-3
Appearance Solid
Molecular Weight 383.40
Formula C₁₈H₂₁N₇O₃
Color White to off-white
SMILES

NC1=NC2=CC(C3=NC(N4CCOCC4)=NC(N5CCOCC5)=N3)=CC=C2O1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Phytomedicine

Hypocrellin A against intrahepatic Cholangiocarcinoma via multi-target inhibition of the PI3K-AKT-mTOR, MAPK, and STAT3 signaling pathways. [Abstract]

2024 Sep 7:135:156022. PMID: 39284270

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (260.82 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6082 mL

13.0412 mL

26.0824 mL

5 mM

0.5216 mL

2.6082 mL

5.2165 mL

10 mM

0.2608 mL

1.3041 mL

2.6082 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (6.52 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (6.52 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.5 mg/mL (6.52 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Hou Y, et, al. Discovery of Novel Phosphoinositide-3-Kinase α Inhibitors with High Selectivity, Excellent Bioavailability, and Long-Acting Efficacy for Gastric Cancer. J Med Chem. 2022 Jul 14. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6082 mL	13.0412 mL	26.0824 mL	65.2061 mL
	5 mM	0.5216 mL	2.6082 mL	5.2165 mL	13.0412 mL
	10 mM	0.2608 mL	1.3041 mL	2.6082 mL	6.5206 mL
	15 mM	0.1739 mL	0.8694 mL	1.7388 mL	4.3471 mL
	20 mM	0.1304 mL	0.6521 mL	1.3041 mL	3.2603 mL
	25 mM	0.1043 mL	0.5216 mL	1.0433 mL	2.6082 mL
	30 mM	0.0869 mL	0.4347 mL	0.8694 mL	2.1735 mL
	40 mM	0.0652 mL	0.3260 mL	0.6521 mL	1.6302 mL
	50 mM	0.0522 mL	0.2608 mL	0.5216 mL	1.3041 mL
	60 mM	0.0435 mL	0.2174 mL	0.4347 mL	1.0868 mL
	80 mM	0.0326 mL	0.1630 mL	0.3260 mL	0.8151 mL
	100 mM	0.0261 mL	0.1304 mL	0.2608 mL	0.6521 mL

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PI3Kα-IN-9

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) PI3Kα-IN-9

All PI3K Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PI3Kα-IN-9

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) PI3Kα-IN-9

All PI3K Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PI3Kα-IN-9 Related Classifications

Cat. No.: HY-150618