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Alternative_name
2-(4-methyl-1,4-diazepan-1-yl)-N-((5-methylpyrazin-2-yl)methyl)-5-oxo-5H-benzo[4,5]thiazolo[3,2-a][1,8]naphthyridine-6-carboxamide
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Description
CX-5461 is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis, with IC₅₀s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II (IC₅₀ ≥25 μM). At 50 mg/kg, CX-5461 demonstrates in vivo antitumor activity against human solid tumors in mouse xenograft models.
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CAS Number
1138549-36-6
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Structure Available
Yes
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Salt Form
No
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Molecular Formula
C₂₇H₂₇N₇O₂S
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Molecular Weight
513.61
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Cell Permeable
Yes
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Purity
≥98% by HPLC
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Solubilities
DMSO
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Handling
Protect from air and light
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Tag Line
A potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis
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Storage Condition
-20°C
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Shipping Condition
gel pack
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Shelf Life
36 months
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PubChem CID
25257557
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SMILES
CC1=CN=C(C=N1)CNC(=O)C2=C3N(C4=CC=CC=C4S3)C5=C(C2=O)C=CC(=N5)N6CCCN(CC6)C
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InChi
InChI=1S/C27H27N7O2S/c1-17-14-29-18(15-28-17)16-30-26(36)23-24(35)19-8-9-22(33-11-5-10-32(2)12-13-33)31-25(19)34-20-6-3-4-7-21(20)37-27(23)34/h3-4,6-9,14-15H,5,10-13,16H2,1-2H3,(H,30,36)
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InChi Key
XGPBJCHFROADCK-UHFFFAOYSA-N
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MSDS Available
Yes