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この商品について
実験式(ヒル表記法):
C18H22N6O3S
CAS番号:
分子量:
402.47
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Quality Segment
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 20 mg/mL
shipped in
ambient
storage temp.
2-8°C
SMILES string
[S](=O)(=O)(N)c1ccc(cc1)Nc2nc3[nH]cnc3c(n2)OCC4CCCCC4
InChI
1S/C18H22N6O3S/c19-28(25,26)14-8-6-13(7-9-14)22-18-23-16-15(20-11-21-16)17(24-18)27-10-12-4-2-1-3-5-12/h6-9,11-12H,1-5,10H2,(H2,19,25,26)(H2,20,21,22,23,24)
InChI key
OWXORKPNCHJYOF-UHFFFAOYSA-N
General description
A cell-permeable 2,6-disubstituted purine compound that displays antiproliferative properties. Acts as a potent and ATP-competitive inhibitor of Cdk1/cyclin B and Cdk2/cyclin A3 (IC50 = 9.5 nM and 5.4 nM). Displays greater selectivity for Cdk1/2 over other kinases tested (IC50 = 600 nM, 800 nM, 900 nM and 1.6 µM for ROCKII, PDK1, DYRK1A and Cdk4/D1, respectively). Shown to inhibit human MCF-7 breast carcinoma cell growth with a GI50 of 8 µM.
A cell-permeable purine analog that displays anti-proliferative properties and acts as a potent and ATP-competitive inhibitor of Cdk1/cyclin B and Cdk2/cyclin A3 (IC50 = 9.5 nM and 5.4 nM, respectively). Displays greater selectivity for Cdk′s over other kinases tested (IC50 = 30 nM, 600 nM, 800 nM, 900 nM, and 1.6 µM for Cdk2/A, ROCKII, PDK1, DYRK1A, and Cdk4/D1, respectively). Shown to inhibit human MCF-7 breast carcinoma cell growth (GI50 of 8 µM).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Cdk1/cyclin B, Cdk2/cyclin A3
Cdk1/cyclin B, Cdk2/cyclin A3
Product competes with ATP.
Reversible: no
Target IC50: 9.5 nM, 5.4 nM against Cdk1/cyclin B, Cdk2/cyclin A3, respectively
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Hardcastle, I.R., et al. 2004. J. Med. Chem.47, 3710.
Sayle, K.L., et al. 2003. Bioorg. Med. Chem. Lett.13, 3079.
Davies, T.G., et al. 2002. Nat. Struct. Biol.9, 745.
Sayle, K.L., et al. 2003. Bioorg. Med. Chem. Lett.13, 3079.
Davies, T.G., et al. 2002. Nat. Struct. Biol.9, 745.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Carcinogenic / Teratogenic (D)
保管分類
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
試験成績書(COA)
製品のロット番号・バッチ番号を入力して、試験成績書(COA) を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。