1. Cell Cycle/DNA Damage
  2. Topoisomerase
  3. Intoplicine dimesylate

Intoplicine dimesylate (Synonyms: RP 60475 dimesylate)

Cat. No.: HY-101647A
Handling Instructions

Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 105 /M) and thereby increases the length of linear DNA.

For research use only. We do not sell to patients.

Intoplicine dimesylate Chemical Structure

Intoplicine dimesylate Chemical Structure

CAS No. : 133711-99-6

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Description

Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 105 /M) and thereby increases the length of linear DNA[1][2].

IC50 & Target

Topoisomerase I

 

Topoisomerase II

 

In Vitro

With 1-hour exposure to Intoplicine dimesylate at final concentrations of 2.5 micrograms/mL and 10.0 micrograms/mL, 26% and 54% of the assessable specimens shows positive in vitro responses, respectively[2].
With continuous exposure to Intoplicine dimesylate at concentrations of 0.25 micrograms/mL and 2.5 micrograms/mL, 16% and 71% of the assessable specimens showed positive responses, respectively[2].
Activity is seen against breast (71%), non-small-cell lung (69%), and ovarian (45%) cancer colony-forming units at a Intoplicine dimesylate concentration of 10.0 micrograms/mL after 1-hour exposure[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

At the highest non-toxic dose (HNTD) (6 mg/kg/injection, total dose, 36 mg/kg), intoplicine dimesylate shows highly active with a T/C of 0% and a corresponding total log cell kill of 3[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

540.65

Formula

C₂₃H₃₂N₄O₇S₂

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Product Name:
Intoplicine dimesylate
Cat. No.:
HY-101647A
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