Art. -Nr.: HY-16596

CNX-1351

Name: CNX-1351
Brand: MedChemExpress
SKU: HY-16596
Price: 120.00 USD
Availability: InStock
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CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC₅₀ of 6.8 nM.

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Reinheit : 98.87%
CAS. Nr.: 1276105-89-5
Formel: C₃₀H₃₅N₇O₃S
Molecular Weight:573.71

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

CNX-1351 Chemical Structure

CAS. Nr.: 1276105-89-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC₅₀ of 6.8 nM.

IC₅₀ & Target

^[1]

PI3Kα

6.8 nM (IC₅₀)

PI3Kβ

166 nM (IC₅₀)

PI3Kδ

240.3 nM (IC₅₀)

PI3Kγ

3020 nM (IC₅₀)

Alle PI3K Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	GI₅₀	54.7 nM Compound: 3, CNX-1351	Growth inhibition of human MCF7 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay Growth inhibition of human MCF7 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay	[PMID: 23360348]
SK-OV-3	EC₅₀	10 nM Compound: 3, CNX-1351	Inhibition of PI3Kalpha in human SKOV3 cells assessed as inhibition of Akt Ser473 phosphorylation at 1 to 1000 nM after 1 hr by immunoblot analysis Inhibition of PI3Kalpha in human SKOV3 cells assessed as inhibition of Akt Ser473 phosphorylation at 1 to 1000 nM after 1 hr by immunoblot analysis	[PMID: 23360348]
SK-OV-3	GI₅₀	77.6 nM Compound: 3, CNX-1351	Growth inhibition of human SKOV3 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay Growth inhibition of human SKOV3 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay	[PMID: 23360348]

In Vitro

CNX-1351 is able to potently (EC₅₀<100 nM) and specifically inhibit signaling in PI3Kα-dependent cancer cell lines, and this leads to a potent antiproliferative effect (GI₅₀<100 nM). CNX-1351 inhibits PI3K signaling in SKOV3 cells, with potency (EC₅₀ of 10-100 nM) similar to that of the pan-PI3K inhibitor. To investigate the functional consequence of inhibiting PI3Kα in cells, two cell lines with different PIK3CA activating mutations, SKOV3 ovarian cancer cells (H1047R) and MCF-7 breast cancer cells (E545K), are treated with CNX-1351 and growth is monitored. Both PIK3CA-driven cell lines are growth inhibited by exposure to CNX-1351 for 96 h (GI₅₀ of 78 and 55 nM, respectively)^[1].

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

In Vivo

CNX-1351 inhibits p-Akt^Ser473 in mouse spleens and bonds to PI3Kα in vivo. CNX-1351 is delivered into the intraperitoneal cavity of nude mice at 100 mg/kg once a day for 5 consecutive days (n=3 mice per group). Spleens are harvested from the mice at the indicated times after the last dose (1-24 h) and interrogated by immunoblot for P-Akt^Ser473 or for PI3Kα occupancy. Inhibition of PI3K signaling is detected as a decrease in P-Akt^Ser473 at 1 and 4 h after last dose^[1].

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

Chemical Information

CAS. Nr. 1276105-89-5
Appearance Solid
Molecular Weight 573.71
Formel C₃₀H₃₅N₇O₃S
Color White to yellow
SMILES

C/C(C)=C/C(CCC(N1CCN(CC2=CC3=NC(C4=CC=CC5=C4C=NN5)=NC(N6CCOCC6)=C3S2)CC1)=O)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (174.30 mM; Need ultrasonic; 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

1.7430 mL

8.7152 mL

17.4304 mL

5 mM

0.3486 mL

1.7430 mL

3.4861 mL

10 mM

0.1743 mL

0.8715 mL

1.7430 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 (4.36 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.36 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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)

Verweise

[1]. Nacht M, et al. Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα. J Med Chem. 2013 Feb 14;56(3):712-21. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7430 mL	8.7152 mL	17.4304 mL	43.5760 mL
	5 mM	0.3486 mL	1.7430 mL	3.4861 mL	8.7152 mL
	10 mM	0.1743 mL	0.8715 mL	1.7430 mL	4.3576 mL
	15 mM	0.1162 mL	0.5810 mL	1.1620 mL	2.9051 mL
	20 mM	0.0872 mL	0.4358 mL	0.8715 mL	2.1788 mL
	25 mM	0.0697 mL	0.3486 mL	0.6972 mL	1.7430 mL
	30 mM	0.0581 mL	0.2905 mL	0.5810 mL	1.4525 mL
	40 mM	0.0436 mL	0.2179 mL	0.4358 mL	1.0894 mL
	50 mM	0.0349 mL	0.1743 mL	0.3486 mL	0.8715 mL
	60 mM	0.0291 mL	0.1453 mL	0.2905 mL	0.7263 mL
	80 mM	0.0218 mL	0.1089 mL	0.2179 mL	0.5447 mL
	100 mM	0.0174 mL	0.0872 mL	0.1743 mL	0.4358 mL

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CNX-1351

Alle PI3K Isoform-spezifische Produkte anzeigen