Pazelliptine

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 585036

CAS#: 65222-35-7

Description: Pazelliptine is a DNA topoisomerase inhibitor and antitumor drug.


Chemical Structure

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Pazelliptine
CAS# 65222-35-7

Theoretical Analysis

MedKoo Cat#: 585036
Name: Pazelliptine
CAS#: 65222-35-7
Chemical Formula: C22H27N5
Exact Mass: 361.23
Molecular Weight: 361.493
Elemental Analysis: C, 73.10; H, 7.53; N, 19.37

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: Pazelliptine

IUPAC/Chemical Name: 1,3-Propanediamine, N,N-diethyl-N'-(6-methyl-5H-pyrido(3',4':4,5)pyrrolo(2,3-g)isoquinolin-10-yl)-

InChi Key: LPHSYQSMAGVYNT-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H27N5/c1-4-27(5-2)12-6-9-24-22-18-13-17-19-14-23-10-8-20(19)26-21(17)15(3)16(18)7-11-25-22/h7-8,10-11,13-14,26H,4-6,9,12H2,1-3H3,(H,24,25)

SMILES Code: CC1=C(NC2=CC=NC=C23)C3=CC4=C1C=CN=C4NCCCN(CC)CC

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

Shelf Life: >3 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:

Preparing Stock Solutions

The following data is based on the product molecular weight 361.49 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.

Recalculate based on batch purity %
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:

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1: Balosso J, Giocanti N, Favaudon V. Additive and supraadditive interaction between ionizing radiation and pazelliptine, a DNA topoisomerase inhibitor, in Chinese hamster V-79 fibroblasts. Cancer Res. 1991 Jun 15;51(12):3204-11. PubMed PMID: 1645614.

2: Fontaine-Aupart MP, Frejacques M, Renault E, Ferradini C, Gardes-Albert M, Hickel B, Rivalle C, Bisagni E. Two-photon ionisation of the antitumor drug pazelliptine (BD40) by 355 nm laser photolysis. J Photochem Photobiol B. 1993 Dec;21(2-3):203-9. PubMed PMID: 8301416.

3: Renault E, Fontaine-Aupart MP, Tfibel F, Gardes-Albert M, Bisagni E. Spectroscopic study of the interaction of pazelliptine with nucleic acids. J Photochem Photobiol B. 1997 Oct;40(3):218-27. PubMed PMID: 9463113.

4: Langdon SP, Hendriks HR, Braakhuis BJ, Pratesi G, Berger DP, Fodstad O, Fiebig HH, Boven E. Preclinical phase II studies in human tumor xenografts: a European multicenter follow-up study. Ann Oncol. 1994 May;5(5):415-22. PubMed PMID: 8075048.

5: Guerquin-Kern JL, Coppey M, Carrez D, Brunet AC, Nguyen CH, Rivalle C, Slodzian G, Croisy A. Complementary advantages of fluorescence and SIMS microscopies in the study of cellular localization of two new antitumor drugs. Microsc Res Tech. 1997 Feb 15;36(4):287-95. PubMed PMID: 9140928.

6: Rosselli F, Duchaud E, Averbeck D, Moustacchi E. Comparison of the effects of DNA topoisomerase inhibitors on lymphoblasts from normal and Fanconi anemia donors. Mutat Res. 1994 Dec;325(4):137-44. PubMed PMID: 7527905.

7: Pierson V, Pierre A, Pommier Y, Gros P. Production of protein-associated DNA breaks by 10-[diethylaminopropylamino]-6-methyl-5H-pyrido[3',4':4,5]pyrrolo [2,3-g]isoquinoline in cultured L1210 cells and in isolated nuclei: comparison with other topoisomerase II inhibitors. Cancer Res. 1988 Mar 15;48(6):1404-9. PubMed PMID: 2830964.

8: Vilarem MJ, Charcosset JY, Primaux F, Gras MP, Calvo F, Larsen CJ. Differential effects of ellipticine and aza-analogue derivatives on cell cycle progression and survival of BALB/c 3T3 cells released from serum starvation or thymidine double block. Cancer Res. 1985 Aug;45(8):3906-11. PubMed PMID: 4016757.

9: Ono K, Nakane H, Barre-Sinoussi F, Chermann JC. Differential inhibition by an antitumoral drug 10-[gamma-diethylaminopropylamino]-6-methyl-5H-pyrido[3',4': 4,5]pyrrolo [2,3-G]isoquinoline (BD-40), a pyrido-pyrrolo-isoquinoline derivative, of in vitro DNA synthesis catalyzed by various DNA polymerases. Cancer Lett. 1990 May 15;51(1):59-65. PubMed PMID: 1692511.

10: Moustacchi E, Favaudon V, Bisagni E. Likelihood of the new antitumoral drug 10-[gamma-diethylaminopropylamino]-6-methyl-5H-pyrido[3',4':4,5]pyrrolo [2,3-g]isoquinoline (BD-40), a pyridopyrroloisoquinoline derivative, to induce DNA strand breaks in vivo and its nonmutagenicity in yeast. Cancer Res. 1983 Aug;43(8):3700-6. PubMed PMID: 6344990.

11: Vilarem MJ, Gras MP, Primaux F, Larsen CJ. Effects of BD-40, an ellipticine analogue (aza-ellipticine) on cell cycle traverse and DNA synthesis in cultures of synchronized mouse fibroblasts. Biochimie. 1984 Sep-Oct;66(9-10):591-9. PubMed PMID: 6525354.

12: Vilarem MJ, Riou JF, Multon E, Gras MP, Larsen CJ. The in vitro involvement of topoisomerase II in the activity of aza-ellipticine analogues is not correlated with drug activity on isolated nuclei. Biochem Pharmacol. 1986 Jul 1;35(13):2087-95. PubMed PMID: 3015146.

13: Vilarem MJ, Riou JF, Riou G, Larsen CJ. [Study, at the gene level, of the activation of topoisomerase II by antitumor agents]. Pathol Biol (Paris). 1987 Nov;35(9):1263-9. French. PubMed PMID: 2827094.

14: Sekaki A, Gardes-Albert M, Houee-Levin C, Ferradini C, Rivalle C, Bisagni E, Croisy A, Hickel B. Role of the superoxide anion in the oxidative activation of the new antitumor drug BD40: a radiolysis study. Int J Radiat Biol. 1989 Jun;55(6):901-11. PubMed PMID: 2567329.

15: Vilarem MJ, Gras MP, Rivalle C, Larsen CJ. Possible relationship between pyrido-pyrrolo-isoquinoline derivative (BD-40) cell uptake and cell viability. Biochimie. 1982 Oct;64(10):923-32. PubMed PMID: 6817823.

16: Lidereau R, Chermann JC, Gruest J, Montagnier L, Ducrocq C, Rivalle C, Bisagni E. Antitumoral activity of dipyrido [4,3-b] [3,4-f] indoles on L 1210 leukemia. Bull Cancer. 1980;67(1):1-8. PubMed PMID: 7362880.

17: Vilarem MJ, Gras MP, Larsen CJ. BD-40, an ellipticine-related DNA intercalative agent induces DNA-protein bridges in vivo. Nucleic Acids Res. 1984 Nov 26;12(22):8653-65. PubMed PMID: 6504706; PubMed Central PMCID: PMC320405.

18: Vilarem MJ, Gras MP, Bisagni E, Larsen CJ. [BD-40, intercalating 9-azaellipticine derivative, induces breaks in cellular DNA associated with protein bridges]. C R Acad Sci III. 1984;299(4):69-72. French. PubMed PMID: 6437622.