[CAS NO. 125974-72-3] Intoplicine

Name: Intoplicine
Brand: Arctom Scientific
SKU: AS458418

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PRODUCTS SPECIFICATIONS [125974-72-3]

Fulfillment

Catalog

AS458418

Brand

Arctom Scientific

CAS

125974-72-3

DESCRIPTION [125974-72-3]

Overview

MDL	MFCD00866361
Molecular Weight	348.44
Molecular Formula	C21H24N4O
SMILES	OC1=CC=C2C3=C(NC4=C3C(NCCCN(C)C)=NC=C4C)C=CC2=C1

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

Summary

Intoplicine (RP 60475), an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine strongly binds DNA (K _A = 2 x 10 ⁵ /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 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 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 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 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

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00003713	Genzyme, a Sanofi Company\|Sanofi	Unspecified Adult Solid Tumor, Protocol Specific	August 1997	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : 80 mg/mL ( 229.59 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8699 mL	14.3497 mL	28.6993 mL
5 mM	0.5740 mL	2.8699 mL	5.7399 mL
10 mM	0.2870 mL	1.4350 mL	2.8699 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2 mg/mL (5.74 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2 mg/mL (5.74 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2 mg/mL (5.74 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

7H-Benzo[e]pyrido[4,3-b]indol-3-ol, 11-[[3-(dimethylamino)propyl]amino]-8-methyl-

11-[[3-(Dimethylamino)propyl]amino]-8-methyl-7H-benzo[e]pyrido[4,3-b]indol-3-ol

Intoplicine