(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.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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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
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[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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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)
(rel)-PRT062607 Related Classifications
HY-15322A Related Classifications
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