Cat. No.: HY-10812

GNE-490

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GNE-490, a (thienopyrimidin-2-yl)aminopyrimidine, is a potent pan-PI3K inhibitor with IC₅₀s of 3.5 nM, 25 nM, 5.2 nM, 15 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. GNE-490 has >200 fold selectivity for mTOR (IC₅₀=750 nM). GNE-490 shows potent suppression efficacy profile against MCF7.1 breast cancer xenograft model.

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Pureté: 96.79%
CAS No.: 1033739-92-2
Formule: C₁₈H₂₂N₆O₂S
Masse moléculaire:386.47

Stockage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

GNE-490 Chemical Structure

CAS No.: 1033739-92-2

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Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

PI3Kα

3.5 nM (IC₅₀)

PI3Kβ

25 nM (IC₅₀)

PI3Kδ

5.2 nM (IC₅₀)

PI3Kγ

15 nM (IC₅₀)

mTOR

750 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform PI3K :

Voir tous les produits spécifiques à Isoform mTOR :

Cellular Effect

Cell Line	Type	Value	Description	References
PC-3	IC₅₀	0.49 nM Compound: 21, GNE-490	Antiproliferative activity against human PC3 cells deficient in PTEN in after 3 to 4 days Antiproliferative activity against human PC3 cells deficient in PTEN in after 3 to 4 days	[PMID: 20050669]

Chemical Information

CAS No. 1033739-92-2
Appearance Solid
Masse moléculaire 386.47
Formule C₁₈H₂₂N₆O₂S
Color White to off-white
SMILES

OC(C)(C)C1=CC(N=C(C2=CN=C(N)N=C2C)N=C3N4CCOCC4)=C3S1
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (1)

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Molecules

Anticancer Potential of Thieno[2,3-d]pyrimidine Derivatives in Oral Carcinoma Models. [Abstract]

2026 Jan 23;31(3):397. PMID: 41683377

Solvant et solubilité

In Vitro:

DMSO : ≥ 100 mg/mL (258.75 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

2.5875 mL

12.9376 mL

25.8752 mL

5 mM

0.5175 mL

2.5875 mL

5.1750 mL

10 mM

0.2588 mL

1.2938 mL

2.5875 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (272 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)
Instruction de manipulation (2659 KB)

Références

[1]. Daniel P Sutherlin, et al. Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer. J Med Chem. 2010 Feb 11;53(3):1086-97. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5875 mL	12.9376 mL	25.8752 mL	64.6881 mL
	5 mM	0.5175 mL	2.5875 mL	5.1750 mL	12.9376 mL
	10 mM	0.2588 mL	1.2938 mL	2.5875 mL	6.4688 mL
	15 mM	0.1725 mL	0.8625 mL	1.7250 mL	4.3125 mL
	20 mM	0.1294 mL	0.6469 mL	1.2938 mL	3.2344 mL
	25 mM	0.1035 mL	0.5175 mL	1.0350 mL	2.5875 mL
	30 mM	0.0863 mL	0.4313 mL	0.8625 mL	2.1563 mL
	40 mM	0.0647 mL	0.3234 mL	0.6469 mL	1.6172 mL
	50 mM	0.0518 mL	0.2588 mL	0.5175 mL	1.2938 mL
	60 mM	0.0431 mL	0.2156 mL	0.4313 mL	1.0781 mL
	80 mM	0.0323 mL	0.1617 mL	0.3234 mL	0.8086 mL
	100 mM	0.0259 mL	0.1294 mL	0.2588 mL	0.6469 mL

Keywords

GNE-490

1 Cited Publications

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GNE-490

Kinase Inhibitor Library

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Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) GNE-490

Voir tous les produits spécifiques à Isoform PI3K

Voir tous les produits spécifiques à Isoform mTOR

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

GNE-490 Related Classifications

HY-10812 Related Classifications