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.
Product information
CAS Number: 133711-99-6
Molecular Weight: 540.65
Formula: C23H32N4O7S2
Chemical Name: 16-{[3-(dimethylamino)propyl]amino}-13-methyl-11,15-diazatetracyclo[8.7.0.0²,⁷.0¹²,¹⁷]heptadeca-1,3,5,7,9,12(17),13,15-octaen-5-ol; bis(methanesulfonic acid)
Smiles: CC1=CN=C(NCCCN(C)C)C2=C1NC1=CC=C3C=C(O)C=CC3=C12.CS(O)(=O)=O.CS(O)(=O)=O
InChiKey: JAUYMMJDKJISLX-UHFFFAOYSA-N
InChi: InChI=1S/C21H24N4O.2CH4O3S/c1-13-12-23-21(22-9-4-10-25(2)3)19-18-16-7-6-15(26)11-14(16)5-8-17(18)24-20(13)19;2*1-5(2,3)4/h5-8,11-12,24,26H,4,9-10H2,1-3H3,(H,22,23);2*1H3,(H,2,3,4)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. 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. 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.
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.
Products are for research use only. Not for human use.
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