(rel)-PRT062607
(rel)-PRT062607 ((rel)-P505-15) is the relative configuration of PRT062607 (HY-15322). PRT062607 is a highly selective inhibitor of Syk kinase, with an IC50 value of 1-2 nM, and is more than 80 times less potent against Fgr, Lyn, FAK, Pyk2, and Zap70.
For research use only. We do not sell to patients.
- CAS No.: 1194954-52-3
- Formula: C19H23N9O
- Molecular Weight:393.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Bone marrow cell | IC50 |
5853 nM
Compound: 1, BIB-057
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Cytotoxicity against C57BL/6 mouse bone marrow cells assessed as growth inhibition preincubated for 4 days followed by [3H]-thymidine addition measured after 5 hrs by betaplate counting analysis
Cytotoxicity against C57BL/6 mouse bone marrow cells assessed as growth inhibition preincubated for 4 days followed by [3H]-thymidine addition measured after 5 hrs by betaplate counting analysis
|
[PMID: 25633741] |
Chemical Information
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CAS No. 1194954-52-3
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Molecular Weight 393.45
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Formula C19H23N9O
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SMILES
NC(C(C(NC1=CC(N2N=CC=N2)=CC=C1)=N3)=CN=C3N[C@H]4[C@H](CCCC4)N)=O
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Synonyms
(rel)-P505-15; (rel)-PRT-2607; (rel)-BIIB-057
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Coffey G, et al. Specific inhibition of spleen tyrosine kinase suppresses leukocyte immune function and inflammation in animal models of rheumatoid arthritis. J Pharmacol Exp Ther. 2012 Feb;340(2):350-9. [Content Brief]
[2]. Spurgeon SE, et al. The selective SYK inhibitor P505-15 (PRT062607) inhibits B cell signaling and function in vitro and in vivo and augments the activity of fludarabine in chronic lymphocytic leukemia. J Pharmacol Exp Ther. 2013 Feb;344(2):378-87. [Content Brief]
[3]. Hoellenriegel J, et al. Selective, novel spleen tyrosine kinase (Syk) inhibitors suppress chronic lymphocytic leukemia B-cell activation and migration. Leukemia. 2012 Jul;26(7):1576-83. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)