GSK2292767
featured

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 522376

CAS#: 1254036-66-2 (free base)

Description: GSK2292767 is a potent and selective PI3Kδ inhibitor. GSK2292767 is is currently in clinical trials for the treatment of respiratory diseases such as asthma and COPD. GSK2292767 is highly selective for PI3Kδ over the closely related isoforms and are active in a disease relevant brown Norway rat acute OVA model of Th2-driven lung inflammation. PI3Kδ is highly enriched in leukocytes, making it an attractive target for the treatment of inflammatory conditions, such as asthma,6 chronic obstructive pulmonary disease (COPD), and autoimmune diseases.


Chemical Structure

img
GSK2292767
CAS# 1254036-66-2 (free base)

Theoretical Analysis

MedKoo Cat#: 522376
Name: GSK2292767
CAS#: 1254036-66-2 (free base)
Chemical Formula: C24H28N6O5S
Exact Mass: 512.18
Molecular Weight: 512.585
Elemental Analysis: C, 56.24; H, 5.51; N, 16.40; O, 15.61; S, 6.25

Price and Availability

Size Price Availability Quantity
5mg USD 380 2 Weeks
10mg USD 650 2 Weeks
25mg USD 1250 2 Weeks
Bulk inquiry

Synonym: GSK2292767; GSK-2292767; GSK 2292767.

IUPAC/Chemical Name: N-(5-(4-(5-(((2R,6S)-2,6-dimethylmorpholino)methyl)oxazol-2-yl)-1H-indazol-6-yl)-2-methoxypyridin-3-yl)methanesulfonamide

InChi Key: NLUPPCTVKHDVIQ-GASCZTMLSA-N

InChi Code: InChI=1S/C24H28N6O5S/c1-14-11-30(12-15(2)34-14)13-18-9-26-23(35-18)19-5-16(6-21-20(19)10-27-28-21)17-7-22(29-36(4,31)32)24(33-3)25-8-17/h5-10,14-15,29H,11-13H2,1-4H3,(H,27,28)/t14-,15+

SMILES Code: CS(=O)(NC1=CC(C2=CC3=C(C(C4=NC=C(CN5C[C@@H](C)O[C@@H](C)C5)O4)=C2)C=NN3)=CN=C1OC)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: GSK2292767 is an analogue of GSK2269557

Product Data:
Safety Data Sheet (SDS):
Biological target: GSK2292767 is a potent and selective inhibitor of PI3Kδ, with a pIC50 of 10.1.
In vitro activity: TBD
In vivo activity: Compounds 2 and 3 (GSK2292767) are both highly selective for PI3Kδ over the closely related isoforms and are active in a disease relevant brown Norway rat acute OVA model of Th2-driven lung inflammation.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
dmf 16.0 31.21
DMF:PBS (pH 7.2) (1:2) 0.3 0.59
DMSO 57.0 111.20

Preparing Stock Solutions

The following data is based on the product molecular weight 512.59 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Down K, Amour A, Baldwin IR, Cooper AW, Deakin AM, Felton LM, Guntrip SB, Hardy C, Harrison ZA, Jones KL, Jones P, Keeling SE, Le J, Livia S, Lucas F, Lunniss CJ, Parr NJ, Robinson E, Rowland P, Smith S, Thomas DA, Vitulli G, Washio Y, Hamblin JN. Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease. J Med Chem. 2015 Sep 24;58(18):7381-99. doi: 10.1021/acs.jmedchem.5b00767. Epub 2015 Sep 3. PMID: 26301626.
In vitro protocol: TBD
In vivo protocol: 1. Down K, Amour A, Baldwin IR, Cooper AW, Deakin AM, Felton LM, Guntrip SB, Hardy C, Harrison ZA, Jones KL, Jones P, Keeling SE, Le J, Livia S, Lucas F, Lunniss CJ, Parr NJ, Robinson E, Rowland P, Smith S, Thomas DA, Vitulli G, Washio Y, Hamblin JN. Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease. J Med Chem. 2015 Sep 24;58(18):7381-99. doi: 10.1021/acs.jmedchem.5b00767. Epub 2015 Sep 3. PMID: 26301626.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

1: Down KD, Amour A, Baldwin IR, Cooper AW, Deakin AM, Felton LM, Guntrip SB,
Hardy C, Harrison ZA, Jones KL, Jones P, Keeling SE, Le J, Livia S, Lucas F,
Lunniss CJ, Parr NJ, Robinson E, Rowland P, Smith S, Thomas DA, Vitulli G, Washio
Y, Hamblin N. Optimization of Novel Indazoles as Highly Potent and Selective
Inhibitors of Phosphoinostide-3-Kinase Delta for the Treatment of Respiratory
Disease. J Med Chem. 2015 Aug 24. [Epub ahead of print] PubMed PMID: 26301626.