[CAS NO. 315702-40-0] Ceefourin 1
PRODUCTS SPECIFICATIONS [315702-40-0]
DESCRIPTION [315702-40-0]
Overview
| MDL | MFCD03984494 |
|---|---|
| Molecular Weight | 294.42 |
| Molecular Formula | C11H10N4S3 |
| SMILES | S=C1NN=C(CSC2=NC3=CC=CC=C3S2)N1C |
Summary
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 [1] [2] .
IC50 & Target
MRP4 [1]
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
[1]
.
Ceefourin 1 (100 nM-100 μM) has low cellular toxicity (IC
50
>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)
[1]
.
Ceefourin 1 has an IC
50
of 2.5 μM in HEK293 cell. Ceefourin 1 blocks D-luciferin efflux with an IC
50
of 1.5 μM
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 125 mg/mL ( 424.56 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.3965 mL | 16.9825 mL | 33.9651 mL |
| 5 mM | 0.6793 mL | 3.3965 mL | 6.7930 mL |
| 10 mM | 0.3397 mL | 1.6983 mL | 3.3965 mL |
References
- [1] Leanna Cheung, et al. High-throughput screening identifies Ceefourin 1 and Ceefourin 2 as highly selective inhibitors of multidrug resistance protein 4 (MRP4). Biochem Pharmacol. 2014 Sep 1;91(1):97-108.
- [2] Tony Huynh, et al. CCI52 sensitizes tumors to 6-mercaptopurine and inhibits MYCN-amplified tumor growth. Biochem Pharmacol. 2020 Feb;172:113770.
