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Submit ReviewGSK 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.
Sold for research purposes under agreement from GlaxoSmithKline
GSK 2250665A is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
M. Wt | 459.61 |
Formula | C26H29N5OS |
Storage | Store at +4°C |
Purity | ≥97% (HPLC) |
CAS Number | 1246030-96-5 |
PubChem ID | 73352604 |
InChI Key | DPRNXTSMYVCYLJ-XUTJKUGGNA-N |
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 45.96 | 100 | |
1eq. HCl | 9.19 | 20 |
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.
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 |
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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Keywords: GSK 2250665A, GSK 2250665A supplier, GSK2250665A, Itk, inducible, T, cell, kinase, inhibitors, inhibits, ITK, 5401, Tocris Bioscience
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