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Submit ReviewBMS 509744
Description: Potent and selective ITK inhibitor
Chemical Name: N-[5-[[5-[(4-Acetyl-1-piperazinyl)carbonyl]-4-methoxy-2-methylphenyl]thio]-2-thiazolyl]-4-[[(1,2,2-trimethylpropyl)amino]methyl]benzamide
Purity: ≥97% (HPLC)
Biological Activity for BMS 509744
BMS 509744 is a potent and selective interleukin-2 inducible T cell kinase (ITK) inhibitor (IC50 = 19 nM). Displays 200-fold selectivity over Tec family kinases and 55-fold selectivity over other kinases tested. Reduces HIV infection of primary CD4+ T cells and attenuates the establishment of HIV infection in vitro. Reduces T cell proliferation and IL-2 production in vitro. Reduces lung inflammation in a mouse model of ovalbumin-induced allergy/asthma.
Compound Libraries for BMS 509744
BMS 509744 is also offered as part of the Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for BMS 509744
| M. Wt | 623.83 |
| Formula | C32H41N5O4S2 |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 439575-02-7 |
| PubChem ID | 11467730 |
| InChI Key | ZHXNIYGJAOPMSO-UHFFFAOYSA-N |
| Smiles | COC1=CC(C)=C(SC3=CN=C(NC(C4=CC=C(CNC(C)C(C)(C)C)C=C4)=O)S3)C=C1C(N2CCN(C(C)=O)CC2)=O |
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.
Product Datasheets for BMS 509744
References for BMS 509744
References are publications that support the biological activity of the product.
Kutach et al (2010) Crystal structures of IL-2-inducible T cell kinase complexed with inhibitors: insights into rational drug design and activity regulation. Chem Biol Drug Des. 76 154 PMID: 20545945
Das et al (2006) Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors. Bioorg.Med.Chem.Lett. 16 3706 PMID: 16682193
Readinger et al (2008) Selective targeting of ITK blocks multiple steps of HIV replication. Proc.Natl.Acad.Sci.U.S.A. 105 6684 PMID: 18443296
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Keywords: BMS 509744, BMS 509744 supplier, BMS509744, lung, inflammation, allergy, asthma, inducible, T, cell, kinase, emt, tsk, HIV, potent, selective, ITK, inhibitors, inhibits, Il2, 5009, Tocris Bioscience
1 Citation for BMS 509744
Citations are publications that use Tocris products. Selected citations for BMS 509744 include:
Mamand et al (2018) Comparison of interleukin-2-inducible kinase (ITK) inhibitors and potential for combination therapies for T-cell lymphoma. Sci Rep 8 14216 PMID: 30242208
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