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Nemiralisib (Synonyms: GSK2269557 (free base))

Cat. No.: HY-19535A Purity: 99.50%
Handling Instructions

Nemiralisib (GSK2269557 free base) is a potent and highly selective PI3Kδ inhibitor with a pKi of 9.9.

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

Nemiralisib Chemical Structure

Nemiralisib Chemical Structure

CAS No. : 1254036-71-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 140 In-stock
Estimated Time of Arrival: December 31
1 mg USD 84 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 228 In-stock
Estimated Time of Arrival: December 31
25 mg USD 492 In-stock
Estimated Time of Arrival: December 31
50 mg USD 852 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1440 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Nemiralisib (GSK2269557 free base) is a potent and highly selective PI3Kδ inhibitor with a pKi of 9.9.

IC50 & Target

PI3Kδ

9.9 (pKi)

PI3Kγ

5.2 (pIC50)

PI3Kα

5.3 (pIC50)

PI3Kβ

5.8 (pIC50)

In Vitro

Nemiralisib (GSK2269557 free base) is highly selective for PI3Kδ, with >1000-fold selectivity over the closely related isoforms PI3Kα (pIC50=5.3), PI3Kβ (pIC50=5.8) and PI3Kγ (pIC50=5.2). Nemiralisib inhibits IFNγ in the peripheral blood mononuclear (PBMC) assay with an pIC50 of 9.7[1].

In Vivo

To assess the suitability of the series for inhaled delivery clearance data in rat microsomes and subsequently in vivo pharmacokinetic data from Sprague Dawley male rats is obtained. Compounds (e.g., Nemiralisib) are administered by the oral or intravenous routes, at a dose level of 3 and 1mg/kg respectively (n=2 rats/route). Nemiralisib free base is active in a disease relevant brown norway rat acute OVA model of Type 2 helper T-cells (Th2)-driven lung inflammation[1].

Clinical Trial
Molecular Weight

440.54

Formula

C₂₆H₂₈N₆O

CAS No.

1254036-71-9

SMILES

CC(N1CCN(CC2=CN=C(C3=CC(C4=CC=CC5=C4C=CN5)=CC6=C3C=NN6)O2)CC1)C

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 31 mg/mL (70.37 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2699 mL 11.3497 mL 22.6994 mL
5 mM 0.4540 mL 2.2699 mL 4.5399 mL
10 mM 0.2270 mL 1.1350 mL 2.2699 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Rats[1]
In vivo pharmacokinetics is tested in Sprague Dawley male rats. Compounds (e.g., Nemiralisib) are administered discretely by the oral or intravenous routes, at a dose level of 3 and 1 mg/kg respectively (n=2 rats/route). Compounds (e.g., Nemiralisib) are formulated as a solution in DMSO:PEG200:water (5:45:50 v/v/v) at a dose volume of 6 (oral) and 2 (intravenous) mL/kg. All animals are serially bled from the tail vein and blood samples collected over a time-course of 0-7 h are submitted to LC-MS/MS analysis for the quantification of the parent compound. The main pharmacokinetic parameters are estimated by non-compartmental analysis.

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

References

Purity: 99.50%

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Nemiralisib
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HY-19535A
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