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经验公式(希尔记法):
C27H35N5
化学文摘社编号:
分子量:
429.60
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
InChI
1S/C27H35N5/c1-29(2)25-12-7-5-10-23(25)20-31-18-9-19-32(27(31)22-14-16-28-17-15-22)21-24-11-6-8-13-26(24)30(3)4/h5-8,10-17,27H,9,18-21H2,1-4H3
SMILES string
CN(C)C1=CC=CC=C1CN2CCCN(CC3=CC=CC=C3N(C)C)C2C4=CC=NC=C4
InChI key
KVQOGDQTWWCZFX-UHFFFAOYSA-N
assay
≥95% (HPLC)
form
liquid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light
shipped in
dry ice
storage temp.
−20°C
Quality Level
General description
A cell-permeable hexahydropyrimidine compound that displays similar pharmacological property as, but is structurally disctinct from, GANT58 (Cat. No. 373400). While both compounds act as downstream Hedgehog (Hh) pathway-selective blockers and target Gli-mediated gene transactivation with similar potency (IC50 ~5 µM) in SAG-stimulated Shh-L2 cells, GANT61 does exhibit better in vivo antitumor efficacy, presumably due to its superior pharmacokinetics, and only GANT61, but not GANT58, is shown to inhibit Gli DNA binding in HEK293 cells.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Gli1 and Gli2
Gli1 and Gli2
Packaging
Packaged under inert gas
Physical form
A 25 mM (2 mg/186 µL) solution of Hh/Gli Antagonist, GANT61 (Cat. No. 373401) in DMSO.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)
存储类别
10 - Combustible liquids
wgk
WGK 2
flash_point_f
188.6 °F - closed cup - (refers to pure substance)
flash_point_c
87 °C - closed cup - (refers to pure substance)
Matthias Lauth et al.
Proceedings of the National Academy of Sciences of the United States of America, 104(20), 8455-8460 (2007-05-15)
The developmentally important Hedgehog (Hh) signaling pathway has recently been implicated in several forms of solid cancer. Current drug development programs focus on targeting the protooncogene Smoothened, a key transmembrane pathway member. These drug candidates, albeit promising, do not address
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