Art. -Nr.: HY-100694

GS-9901

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GS-9901 is a highly selective and orally active PI3Kδ inhibitor with an IC₅₀ of 1 nM. GS-9901 has ≥100 fold selectivity for PI3Kα (IC₅₀ of 750 nM), PI3Kβ (IC₅₀ of 100 nM) and PI3Kγ (IC₅₀ of 190 nM). GS-9901 can be used for the study of rheumatoid arthritis.

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Reinheit: 99.97%
CAS. Nr.: 1640247-87-5
Formel: C₂₂H₁₇ClFN₉O
Molecular Weight:477.88

Speicherung:

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

GS-9901 Chemical Structure

CAS. Nr.: 1640247-87-5

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

PI3Kδ

1 nM (IC₅₀)

PI3Kβ

100 nM (IC₅₀)

PI3Kγ

190 nM (IC₅₀)

PI3Kα

750 nM (IC₅₀)

Alle PI3K Isoform-spezifische Produkte anzeigen :

In Vivo

GS-9901 (0.3-3 mg/kg, orally, twice daily for 7 days) demonstrates efficacy in a rat model of arthritis^[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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1640247-87-5
Appearance Solid
Molecular Weight 477.88
Formel C₂₂H₁₇ClFN₉O
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

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.

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

2.0926 mL

10.4629 mL

20.9258 mL

5 mM

0.4185 mL

2.0926 mL

4.1852 mL

10 mM

0.2093 mL

1.0463 mL

2.0926 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.

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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Patel L, et al. Discovery of Orally Efficacious Phosphoinositide 3-Kinase δ Inhibitors with Improved Metabolic Stability. J Med Chem. 2016 Oct 13;59(19):9228-9242. [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	2.0926 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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Alle PI3K Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GS-9901 Related Classifications

HY-100694 Related Classifications