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Indisulam

Indisulam

  • CAT Number: I007331
  • CAS Number: 165668-41-7
  • Molecular Formula: C14H12ClN3O4S2
  • Molecular Weight: 385.84
  • Purity: ≥95%
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Indisulam (Cat No.:I007331) is a powerful inhibitor of carbonic anhydrase (CA), targeting cytosolic isozymes I and II as well as the tumor-associated transmembrane isozyme IX. By inhibiting these CA enzymes, Indisulam interferes with various cellular processes. It effectively suppresses the expression of cyclin E and the phosphorylation of CDK2, crucial steps in the transition from the G1 phase to the S phase of the cell cycle. The inhibition of these key factors by Indisulam offers potential therapeutic benefits in the treatment of cancer and other diseases involving dysregulated cell cycle progression.

Catalog Number I007331
CAS Number 165668-41-7
Molecular Formula

C14H12ClN3O4S2

Purity 95%
Solubility Soluble in DMSO, not in water
Storage -20°C
IUPAC Name 4-N-(3-chloro-1H-indol-7-yl)benzene-1,4-disulfonamide
InChI InChI=1S/C14H12ClN3O4S2/c15-12-8-17-14-11(12)2-1-3-13(14)18-24(21,22)10-6-4-9(5-7-10)23(16,19)20/h1-8,17-18H,(H2,16,19,20)
InChIKey SETFNECMODOHTO-UHFFFAOYSA-N
SMILES C1=CC2=C(C(=C1)NS(=O)(=O)C3=CC=C(C=C3)S(=O)(=O)N)NC=C2Cl
Reference

</br>1:Therapeutic potential and molecular mechanism of a novel sulfonamide anticancer drug, indisulam (E7070) in combination with CPT-11 for cancer treatment. Ozawa Y, Kusano K, Owa T, Yokoi A, Asada M, Yoshimatsu K.Cancer Chemother Pharmacol. 2012 May;69(5):1353-62. doi: 10.1007/s00280-012-1844-8. Epub 2012 Feb 17. PMID: 22349812 </br>2:Covariate-based dose individualization of the cytotoxic drug indisulam to reduce the risk of severe myelosuppression. Zandvliet AS, Schellens JH, Copalu W, Beijnen JH, Huitema AD.J Pharmacokinet Pharmacodyn. 2009 Feb;36(1):39-62. doi: 10.1007/s10928-009-9111-2. Epub 2009 Feb 7. PMID: 19199010 </br>3:Self-associated indisulam in phospholipid-based nanomicelles: a potential nanomedicine for cancer. Cesur H, Rubinstein I, Pai A, Onyüksel H.Nanomedicine. 2009 Jun;5(2):178-83. doi: 10.1016/j.nano.2008.09.001. Epub 2008 Dec 13. PMID: 19071064 Free PMC Article</br>4:Population pharmacokinetic and pharmacodynamic analysis to support treatment optimization of combination chemotherapy with indisulam and carboplatin. Zandvliet AS, Schellens JH, Dittrich C, Wanders J, Beijnen JH, Huitema AD.Br J Clin Pharmacol. 2008 Oct;66(4):485-97. doi: 10.1111/j.1365-2125.2008.03230.x. Epub 2008 May 29. PMID: 18637887 Free PMC Article</br>5:A dose-escalation study of indisulam in combination with capecitabine (Xeloda) in patients with solid tumours. Siegel-Lakhai WS, Zandvliet AS, Huitema AD, Tibben MM, Milano G, Girre V, Diéras V, King A, Richmond E, Wanders J, Beijnen JH, Schellens JH.Br J Cancer. 2008 Apr 22;98(8):1320-6. doi: 10.1038/sj.bjc.6604300. Epub 2008 Apr 15. PMID: 18414469 Free PMC Article</br>6:Clinical complete long-term remission of a patient with metastatic malignant melanoma under therapy with indisulam (E7070). Baur M, Gneist M, Owa T, Dittrich C.Melanoma Res. 2007 Oct;17(5):329-31. PMID: 17885589 </br>7:PK/PD model of indisulam and capecitabine: interaction causes excessive myelosuppression. Zandvliet AS, Siegel-Lakhai WS, Beijnen JH, Copalu W, Etienne-Grimaldi MC, Milano G, Schellens JH, Huitema AD.Clin Pharmacol Ther. 2008 Jun;83(6):829-39. Epub 2007 Sep 12. PMID: 17851564 </br>8:CYP2C9 and CYP2C19 polymorphic forms are related to increased indisulam exposure and higher risk of severe hematologic toxicity. Zandvliet AS, Huitema AD, Copalu W, Yamada Y, Tamura T, Beijnen JH, Schellens JH.Clin Cancer Res. 2007 May 15;13(10):2970-6. PMID: 17504998 Free Article</br>9:A randomized phase II pharmacokinetic and pharmacodynamic study of indisulam as second-line therapy in patients with advanced non-small cell lung cancer. Talbot DC, von Pawel J, Cattell E, Yule SM, Johnston C, Zandvliet AS, Huitema AD, Norbury CJ, Ellis P, Bosquee L, Reck M.Clin Cancer Res. 2007 Mar 15;13(6):1816-22. PMID: 17363538 Free Article</br>10:A phase I and pharmacokinetic study of indisulam in combination with carboplatin. Dittrich C, Zandvliet AS, Gneist M, Huitema AD, King AA, Wanders J.Br J Cancer. 2007 Feb 26;96(4):559-66. Epub 2007 Feb 6. PMID: 17285128 Free PMC Article

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