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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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P120184-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $88.90 | |
P120184-25mg | 25mg | In stock | $400.90 |
Selective Chk1 inhibitor
Synonyms | (2R)-2-amino-2-cyclohexyl-N-[2-(1-methyl-1H-pyrazol-4-yl)-9-oxo-3,10,11-triazatricyclo[6.4.1.0,4,13]trideca-1,4(13),5,7,11-pentaen-6-yl]acetamide | SCHEMBL13599879 | DTXSID401025875 | H11453 | NSC800848 | NSC-800848 | PF 00477736 | PF-736,PF-00477736 | DB |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Selective checkpoint kinase 1 (Chk1) inhibitor (Kivalues are 0.49 and 47 nM for Chk1 and Chk2 respectively). Abrogates cell cycle arrest at S and G2-M checkpoints; sensitizes cells to DNA damage. Enhancesdocetaxel efficacy in tumor cells and xenografts. |
Storage Temp | Store at 2-8°C |
Shipped In | Wet ice |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of checkpoint kinase 1;Inhibitor of checkpoint kinase 2 |
Product Description | PF-00477736 is a potent, selective ATP-competitive small-molecule inhibitor that inhibits Chk1 with a Ki of 0.49 nM. The compound abrogates cell cycle arrest induced by DNA damage and enhances cytotoxicity of clinically important chemotherapeutic agents, including gemcitabine and carboplatin. |
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IUPAC Name | (2R)-2-amino-2-cyclohexyl-N-[2-(1-methylpyrazol-4-yl)-9-oxo-3,10,11-triazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13),11-pentaen-6-yl]acetamide |
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INCHI | InChI=1S/C22H25N7O2/c1-29-11-13(9-25-29)20-16-10-24-28-21(30)15-7-14(8-17(27-20)18(15)16)26-22(31)19(23)12-5-3-2-4-6-12/h7-12,19,27H,2-6,23H2,1H3,(H,26,31)(H,28,30)/t19-/m1/s1 |
InChi Key | NDEXUOWTGYUVGA-LJQANCHMSA-N |
Canonical SMILES | CN1C=C(C=N1)C2=C3C=NNC(=O)C4=C3C(=CC(=C4)NC(=O)C(C5CCCCC5)N)N2 |
Isomeric SMILES | CN1C=C(C=N1)C2=C3C=NNC(=O)C4=C3C(=CC(=C4)NC(=O)[C@@H](C5CCCCC5)N)N2 |
WGK Germany | 3 |
PubChem CID | 135565545 |
Molecular Weight | 419.48 |
PubChem CID | 91623356 |
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CAS Registry No. | 952021-60-2 |
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Solubility | Solvent:DMSO, Max Conc. mg/mL: 31.46, Max Conc. mM: 75 |
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WGK Germany | 3 |
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1. Blasina A, Hallin J, Chen E, Arango ME, Kraynov E, Register J, Grant S, Ninkovic S, Chen P, Nichols T et al.. (2008) Breaching the DNA damage checkpoint via PF-00477736, a novel small-molecule inhibitor of checkpoint kinase 1.. Mol Cancer Ther, 7 (8): (2394-404). [PMID:18723486] |