GSK 2250665A

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Description: Itk inhibitor
Chemical Name: trans-4-[[4-[(6-Ethyl-2-benzothiazolyl)amino]-6-(phenylmethyl)-2-pyrimidinyl]amino]cyclohexanol
Purity: ≥97% (HPLC)

Biological Activity for GSK 2250665A

GSK 2250665A is an Itk inhibitor (pKi = 9.2). Exhibits selectivity for Itk over Aurora B kinase and Btk (pIC50 values are 6.4 and 6.5, respectively) and a panel of other kinases. Inhibits IFNγ production in PBMCs.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Compound Libraries for GSK 2250665A

GSK 2250665A is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for GSK 2250665A

M. Wt 459.61
Formula C26H29N5OS
Storage Store at +4°C
Purity ≥97% (HPLC)
CAS Number 1246030-96-5
PubChem ID 73352604
Smiles CCC1=CC=C(N=C(NC3=NC(N[C@H]5CC[C@H](O)CC5)=NC(CC4=CC=CC=C4)=C3)S2)C2=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for GSK 2250665A

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 45.96 100
1eq. HCl 9.19 20

Preparing Stock Solutions for GSK 2250665A

The following data is based on the product molecular weight 459.61. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.18 mL 10.88 mL 21.76 mL
5 mM 0.44 mL 2.18 mL 4.35 mL
10 mM 0.22 mL 1.09 mL 2.18 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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References for GSK 2250665A

References are publications that support the biological activity of the product.

Alder et al (2013) Identification of a novel and selective series of Itk inhibitors via a template-hopping strategy. ACS Med.Chem.Lett. 12 948 PMID: 24900590

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Citations for GSK 2250665A

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