Description
Ceefourin 1 is a potent and highly selective multidrug resistance protein 4 (MRP4) inhibitor. Ceefourin 1 inhibits transport of a broad range of MRP4 substrates, yet is highly selective for MRP4 over other ABC transporters. Ceefourin 1 is a benzothiazol and primarily as a chemosensitizer for high-risk neuroblastoma.
Product information
CAS Number: 315702-40-0
Molecular Weight: 294.42
Formula: C11H10N4S3
Chemical Name: 3-[(1,3-benzothiazol-2-ylsulfanyl)methyl]-4-methyl-4,5-dihydro-1H-1,2,4-triazole-5-thione
Smiles: CN1C(=S)NN=C1CSC1=NC2=CC=CC=C2S1
InChiKey: KVNBVHCJAUXKPJ-UHFFFAOYSA-N
InChi: InChI=1S/C11H10N4S3/c1-15-9(13-14-10(15)16)6-17-11-12-7-4-2-3-5-8(7)18-11/h2-5H,6H2,1H3,(H,14,16)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 125 mg/mL (424.56 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Ceefourin 1 are highly selective for MRP4 over other ABC transporters, including P-glycoprotein (P-gp), ABCG2 (Breast Cancer Resistance Protein; BCRP) and MRP1 (ABCC1). Ceefourin 1 has limited off-target effects and high stability. Ceefourin 1 (100 nM-100 μM) has low cellular toxicity (IC50>50) in two normal (HSF, MRC5), seven neuroblastoma (BE(2)-C, IMR-32, LAN-1, IMR-32, SK-N-SH, NBL-WN, SHEP) and four other human cancer cell lines (HEPG2, LNCap, SJ-G2, MCF7). Ceefourin 1 has an IC50 of 2.5 μM in HEK293 cell. Ceefourin 1 blocks D-luciferin efflux with an IC50 of 1.5 μM.
Products are for research use only. Not for human use.
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