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Indimitecan

Cat. No. M30893
Indimitecan Structure
Synonym:

LMP776

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Biological Activity

Indimitecan (LMP776) is a topoisomerase I (Top1) inhibitor with anticancer activities.

Chemical Information
Molecular Weight 459.45
Formula C25H21N3O6
CAS Number 915360-05-3
Form Solid
Solubility (25°C) DMSO 8.33 mg/mL (ultrasonic and warming and adjust pH to 3 with HCl and heat to 60°C)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Florence Coussy, et al. Sci Transl Med. BRCAness, SLFN11, and RB1 loss predict response to topoisomerase I inhibitors in triple-negative breast cancers

[2] Anish Thomas, et al. Clin Cancer Res. Targeting Topoisomerase I in the Era of Precision Medicine

[3] Jenna H Burton, et al. Clin Cancer Res. NCI Comparative Oncology Program Testing of Non-Camptothecin Indenoisoquinoline Topoisomerase I Inhibitors in Naturally Occurring Canine Lymphoma

[4] Daniel E Beck, et al. J Med Chem. 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)

[5] Maris A Cinelli, et al. J Med Chem. 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 poiso䲧

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Keywords: Indimitecan, LMP776 supplier, Topoisomerase, inhibitors, activators


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