WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H402502
CAS#: 915303-09-2
Description: Indotecan, also known as LMP400, is a novel selective and potent topoisomerase I inhibitor with potential anticancer activitity. Indotecan is currently in Phase I trials.
Hodoodo Cat#: H402502
Name: Indotecan
CAS#: 915303-09-2
Chemical Formula: C26H26N2O7
Exact Mass: 478.17
Molecular Weight: 478.501
Elemental Analysis: C, 65.26; H, 5.48; N, 5.85; O, 23.41
Synonym: LMP400; LMP-400; LMP 400; Indotecan.
IUPAC/Chemical Name: 2,3-dimethoxy-6-(3-morpholinopropyl)-5H-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
InChi Key: FMFIFGLHVOZDEL-UHFFFAOYSA-N
InChi Code: InChI=1S/C26H26N2O7/c1-31-19-10-15-18(13-20(19)32-2)26(30)28(5-3-4-27-6-8-33-9-7-27)24-16-11-21-22(35-14-34-21)12-17(16)25(29)23(15)24/h10-13H,3-9,14H2,1-2H3
SMILES Code: O=C1N(CCCN2CCOCC2)C3=C(C(C4=C3C=C(OCO5)C5=C4)=O)C6=C1C=C(OC)C(OC)=C6
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 478.50 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Jossé R, Martin SE, Guha R, Ormanoglu P, Pfister TD, Reaper PM, Barnes CS, Jones J, Charlton P, Pollard JR, Morris J, Doroshow JH, Pommier Y. ATR inhibitors VE-821 and VX-970 sensitize cancer cells to topoisomerase i inhibitors by disabling DNA replication initiation and fork elongation responses. Cancer Res. 2014 Dec 1;74(23):6968-79. doi: 10.1158/0008-5472.CAN-13-3369. Epub 2014 Sep 30. PubMed PMID: 25269479; PubMed Central PMCID: PMC4252598.
2: Beck DE, Agama K, Marchand C, Chergui A, Pommier Y, Cushman M. Synthesis and biological evaluation of new carbohydrate-substituted indenoisoquinoline topoisomerase I inhibitors and improved syntheses of the experimental anticancer agents indotecan (LMP400) and indimitecan (LMP776). J Med Chem. 2014 Feb 27;57(4):1495-512. doi: 10.1021/jm401814y. Epub 2014 Feb 11. PubMed PMID: 24517248; PubMed Central PMCID: PMC3983348.
3: Pfister TD, Hollingshead M, Kinders RJ, Zhang Y, Evrard YA, Ji J, Khin SA, Borgel S, Stotler H, Carter J, Divelbiss R, Kummar S, Pommier Y, Parchment RE, Tomaszewski JE, Doroshow JH. Development and validation of an immunoassay for quantification of topoisomerase I in solid tumor tissues. PLoS One. 2012;7(12):e50494. doi: 10.1371/journal.pone.0050494. Epub 2012 Dec 28. PubMed PMID: 23284638; PubMed Central PMCID: PMC3532478.
4: Cinelli MA, Reddy PV, Lv PC, Liang JH, Chen L, Agama K, Pommier Y, van Breemen RB, Cushman M. Identification, synthesis, and biological evaluation of metabolites of the experimental cancer treatment drugs indotecan (LMP400) and indimitecan (LMP776) and investigation of isomerically hydroxylated indenoisoquinoline analogues as topoisomerase I poisons. J Med Chem. 2012 Dec 27;55(24):10844-62. doi: 10.1021/jm300519w. Epub 2012 Dec 7. PubMed PMID: 23215354; PubMed Central PMCID: PMC3542640.
5: Balaña-Fouce R, Prada CF, Requena JM, Cushman M, Pommier Y, Ã