2. PI3K/Akt/mTOR
  3. PI3K mTOR
  4. GNE-490

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.

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

GNE-490 Chemical Structure

GNE-490 Chemical Structure

CAS No. : 1033739-92-2

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1 mg USD 160 In-stock
5 mg USD 420 In-stock
10 mg USD 680 In-stock
25 mg USD 1350 In-stock
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Based on 1 publication(s) in Google Scholar

GNE-490 Related Antibodies

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mTOR mTORC1 mTORC2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

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)

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]
Molecular Weight

386.47

Formula

C18H22N6O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

Solvent & Solubility
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5875 mL 12.9376 mL 25.8752 mL
5 mM 0.5175 mL 2.5875 mL 5.1750 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
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GNE-490 Related Classifications

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:

GNE-4901033739-92-2GNE490GNE 490PI3KmTORPhosphoinositide 3-kinaseMammalian target of Rapamycin(thienopyrimidin-2-yl)aminopyrimidinePI3KαPI3KβPI3KδPI3KγMCF7.1breast cancerInhibitorinhibitorinhibit

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