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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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R127351-1mg | 1mg | In stock | $29.90 | |
R127351-5mg | 5mg | In stock | $123.90 | |
R127351-10mg | 10mg | In stock | $205.90 | |
R127351-25mg | 25mg | Available within 1-2 weeks(?) Item is derived from our semi-finished stock and is processed in 1-2 weeks. | $463.90 | |
R127351-50mg | 50mg | In stock | $761.90 | |
R127351-100mg | 100mg | In stock | $1,371.90 |
Potent and selective cdk inhibitor
Synonyms | (4-amino-2-(1-(methylsulfonyl)piperidin-4-ylamino)pyrimidin-5-yl)(2,3-difluoro-6-methoxyphenyl)methanone | (4-Amino-2-{[1-(Methylsulfonyl)piperidin-4-Yl]amino}pyrimidin-5-Yl)(2,3-Difluoro-6-Methoxyphenyl)methanone | R 547 | Ro 4584820 | SMR004701352 | NSC |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Potent and selective CDK inhibitor (Kivalues are 1, 2, 3, 46, 171 and 260 nM for CDK4/cyclin D1, CDK1/cyclin B, CDK2/cyclin E, GSK3α, CDK7/cyclin H and GSK3β). Exhibits no effect against a panel of >120 other kinases (Ki> 5,000 nM). Inhibits the prolifera |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Cyclin-dependent kinase 4 inhibitor |
Product Description | R547 is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1. |
ALogP | 2.1 |
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Pubchem Sid | 488195888 |
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Pubchem Sid Url | https://pubchem.ncbi.nlm.nih.gov/substance/488195888 |
IUPAC Name | [4-amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl]-(2,3-difluoro-6-methoxyphenyl)methanone |
INCHI | InChI=1S/C18H21F2N5O4S/c1-29-13-4-3-12(19)15(20)14(13)16(26)11-9-22-18(24-17(11)21)23-10-5-7-25(8-6-10)30(2,27)28/h3-4,9-10H,5-8H2,1-2H3,(H3,21,22,23,24) |
InChi Key | JRNJNYBQQYBCLE-UHFFFAOYSA-N |
Canonical SMILES | COC1=C(C(=C(C=C1)F)F)C(=O)C2=CN=C(N=C2N)NC3CCN(CC3)S(=O)(=O)C |
Isomeric SMILES | COC1=C(C(=C(C=C1)F)F)C(=O)C2=CN=C(N=C2N)NC3CCN(CC3)S(=O)(=O)C |
PubChem CID | 6918852 |
Molecular Weight | 441.45 |
CAS Registry No. | 741713-40-6 |
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DiscoveRx TREEspot | R547| |
PubChem CID | 6918852 |
ChEMBL Ligand | CHEMBL384304 |
RCSB PDB Ligand | LIA |
PubChem SID | 488195888 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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C2329033 | Certificate of Analysis | Jan 03, 2023 | R127351 |
C2329034 | Certificate of Analysis | Jan 03, 2023 | R127351 |
C2329035 | Certificate of Analysis | Jan 03, 2023 | R127351 |
C2329037 | Certificate of Analysis | Jan 03, 2023 | R127351 |
C2329038 | Certificate of Analysis | Jan 03, 2023 | R127351 |
C2329039 | Certificate of Analysis | Jan 03, 2023 | R127351 |
C2329041 | Certificate of Analysis | Jan 03, 2023 | R127351 |
C2329042 | Certificate of Analysis | Jan 03, 2023 | R127351 |
C2329043 | Certificate of Analysis | Jan 03, 2023 | R127351 |
C2329047 | Certificate of Analysis | Jan 03, 2023 | R127351 |
C2329493 | Certificate of Analysis | Jan 03, 2023 | R127351 |
Solubility | Solvent:DMSO, Max Conc. mg/mL: 44.15, Max Conc. mM: 100 |
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1. DePinto W, Chu XJ, Yin X, Smith M, Packman K, Goelzer P, Lovey A, Chen Y, Qian H, Hamid R et al.. (2006) In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials.. Mol Cancer Ther, 5 (11): (2644-58). [PMID:17121911] |