2. PI3K/Akt/mTOR
  3. PI3K
  4. GS-9901

GS-9901 is a highly selective and orally active PI3Kδ inhibitor, with an IC50 of 1 nM. Has potential to treat rheumatoid arthritis.

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

GS-9901 Chemical Structure

GS-9901 Chemical Structure

CAS No. : 1640247-87-5

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10 mg USD 420 In-stock
25 mg USD 900 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

GS-9901 Related Antibodies

Top Publications Citing Use of Products

View All PI3K Isoform Specific Products:

View All Isoforms
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GS-9901 is a highly selective and orally active PI3Kδ inhibitor, with an IC50 of 1 nM. Has potential to treat rheumatoid arthritis[1].

IC50 & Target[1]

PI3Kδ

1 nM (IC50)

In Vivo

GS-9901 (0.3/1/3 mg/kg, orally, twice daily for 7 days) demonstrates efficacy in a rat model of arthritis and is predicted to be suitable for q.d. dosing in humans[1].

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

Animal Model: Female Lewis rats with established collagen-induced arthritis (CIA)[1].
Dosage: 0.3 mg/kg, 1 mg/kg, and 3 mg/kg.
Administration: Orally, twice-daily for 7 days starting on the 10th day after the second collagen immunization.
Result: Demonstrated significant reduction in ankle swelling in rats treated with 0.3 mg/kg 35 (31% reduction), 1 mg/kg 35 (67%), and 3 mg/kg 35 (65%).
Plasma concentrations measured on day 7 (12 h after last dose) were consistent with maintaining approximately 60%, 80%, and >90% inhibition of PI3Kδ at 0.3, 1.0, and 3 mg/kg doses, respectively, at trough levels.
Molecular Weight

477.88

Formula

C22H17ClFN9O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC1=NC(N)=NC(N[C@H](C2CC2)C(N3C4=CN=CC=C4)=NC5=C(F)C=CC(Cl)=C5C3=O)=C1C#N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 250 mg/mL (523.14 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 2.0926 mL 10.4629 mL 20.9258 mL
5 mM 0.4185 mL 2.0926 mL 4.1852 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • 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

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

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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. 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 2.0926 mL 10.4629 mL 20.9258 mL 52.3144 mL
5 mM 0.4185 mL 2.0926 mL 4.1852 mL 10.4629 mL
10 mM 0.2093 mL 1.0463 mL 2.0926 mL 5.2314 mL
15 mM 0.1395 mL 0.6975 mL 1.3951 mL 3.4876 mL
20 mM 0.1046 mL 0.5231 mL 1.0463 mL 2.6157 mL
25 mM 0.0837 mL 0.4185 mL 0.8370 mL 2.0926 mL
30 mM 0.0698 mL 0.3488 mL 0.6975 mL 1.7438 mL
40 mM 0.0523 mL 0.2616 mL 0.5231 mL 1.3079 mL
50 mM 0.0419 mL 0.2093 mL 0.4185 mL 1.0463 mL
60 mM 0.0349 mL 0.1744 mL 0.3488 mL 0.8719 mL
80 mM 0.0262 mL 0.1308 mL 0.2616 mL 0.6539 mL
100 mM 0.0209 mL 0.1046 mL 0.2093 mL 0.5231 mL
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GS-9901 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:

GS-99011640247-87-5GS9901GS 9901PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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