TargetMol

Bisantrene HCl

Product Code:
 
TAR-T4047L
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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Further Information

Bioactivity:
Bisantrene (CL-216942; NSC 337766) is a topoisomerase II poison and DNA intercalator. It can be used as a Rac1 inhibitor or model compound to study P-glycoprotein-mediated multi-drug resistance (MDR1). Bisantrene inserts and disrupts the configuration of DNA, leading to DNA single-strand breaks, DNA-protein cross-links, and DNA replication inhibition.
CAS:
71439-68-4
Formula:
C22H24Cl2N8
Molecular Weight:
471.39
Purity:
0.98
SMILES:
Cl.Cl.C1CN=C(NN=C/c2c3ccccc3c(C=N/NC3=NCCN3)c3ccccc23)N1

References

Zagotto G, Oliva A, Guano F, Menta E, Capranico G, Palumbo M. Synthesis, DNA-damaging and cytotoxic properties of novel topoisomerase II-directed bisantrene analogues. Bioorg Med Chem Lett. 1998 Jan 20;8(2):121-6. PubMed PMID: 9871638. Folini M, Pivetta C, Zagotto G, De Marco C, Palumbo M, Zaffaroni N, Sissi C. Remarkable interference with telomeric function by a G-quadruplex selective bisantrene regioisomer. Biochem Pharmacol. 2010 Jun 15;79(12):1781-90. doi: 10.1016/j.bcp.2010.02.018. Epub 2010 Mar 3. PubMed PMID: 20206144. Capranico G, Guano F, Moro S, Zagotto G, Sissi C, Gatto B, Zunino F, Menta E, Palumbo M. Mapping drug interactions at the covalent topoisomerase II-DNA complex by bisantrene/amsacrine congeners. J Biol Chem. 1998 May 22;273(21):12732-9. PubMed PMID: 9582297. Sissi C, Bolgan L, Moro S, Zagotto G, Bailly C, Menta E, Capranico G, Palumbo M. DNA-binding preferences of bisantrene analogues: relevance to the sequence specificity of drug-mediated topoisomerase II poisoning. Mol Pharmacol. 1998 Dec;54(6):1036-45. PubMed PMID: 9855632.