A selective RNA polymerase inhibitor

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Product Type

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Application

CX-5461

Name: CX-5461
Brand: -

Item No. 18392

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)

Technical Information

Formal Name

2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-N-[(5-methyl-2-pyrazinyl)methyl]-5-oxo-5H-benzothiazolo[3,2-a][1,8]naphthyridine-6-carboxamide

CAS Number

1138549-36-6

Molecular Formula

C₂₇H₂₇N₇O₂S

Formula Weight

513.6

Purity

≥98%

Formulation

A crystalline solid

Solubility(Learn about Variance in Solubility)

DMF: 2 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 1 mg/mlEthanol: 0.1 mg/ml

λ_max

242, 292, 299, 339 nm

SMILES

CC1=NC=C(CNC(C2=C3N(C(C=CC=C4)=C4S3)C5=C(C=CC(N6CCCN(C)CC6)=N5)C2=O)=O)N=C1

InChi Code

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)

InChi Key

XGPBJCHFROADCK-UHFFFAOYSA-N

Shipping & Storage Information

Storage

-20°C

Shipping

Room temperature in continental US; may vary elsewhere

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

1 mg

$49

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5 mg

$178

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10 mg

$255

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50 mg

$1,053

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Product Description

CX-5461 is an inhibitor of ribosomal RNA (rRNA) synthesis. It selectively inhibits RNA polymerase I-driven transcription of rRNA in HCT116, A375, and MIA PaCa-2 tumor cells (IC₅₀s = 142, 113, and 54 nM, respectively) without affecting RNA polymerase II (IC₅₀ > 25µM), DNA replication, or protein translation.^1,2 At 50 mg/kg, CX-5461 demonstrates in vivo antitumor activity against human solid tumors in mouse xenograft models.¹

WARNING This product is not for human or veterinary use.

References & Product Citations

Product Description References

1. Drygin, D., Lin, A., Bliesath, J., et al. Targeting RNA polymerase I with an oral small molecule CX-5461 inhibits ribosomal RNA synthesis and solid tumor growth. Cancer Res. 71(4), 1418-1430 (2011).

2. Haddach, M., Schwaebe, M.K., Michaux, J., et al. Discovery of CX-5461, the first direct and selective inhibitor of RNA polymerase I, for cancer therapeutics. ACS Med. Chem. Lett. 3(7), 602-606 (2012).

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