TAS-103 HCl salt (BMS-247615)
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MedKoo CAT#: 202834

CAS#: 174634-09-4

Description: TAS-103, also known as BMS-247615, is a quinoline derivative that displays antitumor activity in murine and human tumor models. TAS-103 has been reported to be a potent topoisomerase II poison. TAS-103 showed the strongest antitumor activity among the conventional anticancer agents for colorectal cancer (p<0.05). The combination with CDDP augmented the antitumor activity of TAS-103 (p<0.05), indicating that CDDP is one of the most potent candidates to be used in combination with TAS-103 . TAS-103 may be useful in the chemotherapy of colorectal cancer.


Price and Availability

Size Price Shipping out time Quantity
5mg USD 120 Same day
10mg USD 190 Same day
25mg USD 330 Same day
50mg USD 550 Same day
100mg USD 950 Same day
200mg USD 1450 Same day
500mg USD 1950 Same day
1g USD 3450 Same day
Inquire bulk and customized quantity

Pricing updated 2020-10-22. Prices are subject to change without notice.

TAS-103 ( BMS-247615 ), purity > 98%, is in stock. The same day shipping out after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 202834
Name: TAS-103 HCl salt (BMS-247615)
CAS#: 174634-09-4
Chemical Formula: C20H21Cl2N3O2
Exact Mass:
Molecular Weight: 406.31
Elemental Analysis: C, 59.12; H, 5.21; Cl, 17.45; N, 10.34; O, 7.88


Related CAS #: 174634-09-4 (HCl salt)   174634-08-3 (free base)  

Synonym: TAS103; TAS-103; TAS 103; BMS247615; BMS 247615; BMS-247615.

IUPAC/Chemical Name: .6-((2-(dimethylamino)ethyl)amino)-3-hydroxy-7H-indeno[2,1-c]quinolin-7-one dihydrochloride

InChi Key: HAYAYGFVSIWSGQ-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H19N3O2.2ClH/c1-23(2)10-9-21-20-18-17(13-5-3-4-6-14(13)19(18)25)15-8-7-12(24)11-16(15)22-20;;/h3-8,11,24H,9-10H2,1-2H3,(H,21,22);2*1H

SMILES Code: O=C(C1=C2C3=CC=C(O)C=C3N=C1NCCN(C)C)C4=C2C=CC=C4.[H]Cl.[H]Cl


Technical Data

Appearance:
Red solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (SDS):

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 water, not soluble in DMSO, not soluble in chloroform.

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in water.

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


References

1: Yoshida M, Kabe Y, Wada T, Asai A, Handa H. A new mechanism of 6-((2-(dimethylamino)ethyl)amino)-3-hydroxy-7H-indeno(2,1-c)quinolin-7-one dihydrochloride (TAS-103) action discovered by target screening with drug-immobilized affinity beads. Mol Pharmacol. 2008 Mar;73(3):987-94. Epub 2007 Dec 18. PubMed PMID: 18089836.

2: Fujimoto S. Promising antitumor activity of a novel quinoline derivative, TAS-103, against fresh clinical specimens of eight types of tumors measured by flow cytometric DNA analysis. Biol Pharm Bull. 2007 Oct;30(10):1923-9. PubMed PMID: 17917263.

3: Torigoe T, Izumi H, Wakasugi T, Niina I, Igarashi T, Yoshida T, Shibuya I, Chijiiwa K, Matsuo K, Itoh H, Kohno K. DNA topoisomerase II poison TAS-103 transactivates GC-box-dependent transcription via acetylation of Sp1. J Biol Chem. 2005 Jan 14;280(2):1179-85. Epub 2004 Nov 8. PubMed PMID: 15533934.

4: Shimizu K, Takada M, Asai T, Kuromi K, Baba K, Oku N. Cancer chemotherapy by liposomal 6-[12-(dimethylamino)ethyl]aminol-3-hydroxy-7H-indeno[2,1-clquinolin-7-one dihydrochloride (TAS-103), a novel anti-cancer agent. Biol Pharm Bull. 2002 Oct;25(10):1385-7. PubMed PMID: 12392102.

5: Ishida K, Asao T. Self-association and unique DNA binding properties of the anti-cancer agent TAS-103, a dual inhibitor of topoisomerases I and II. Biochim Biophys Acta. 2002 Jul 18;1587(2-3):155-63. Review. PubMed PMID: 12084457.

6: Tsunoda T, Tanimura H, Yamaue H, Ishimoto K, Kobunai T, Yamada Y. In vitro antitumor activity of TAS-103 against freshly-isolated human colorectal cancer. Anticancer Res. 2001 Nov-Dec;21(6A):3897-902. PubMed PMID: 11911266.

7: Azuma R, Saeki M, Yamamoto Y, Hagiwara Y, Grochow LB, Donehower RC. Metabolism and urinary excretion of a new quinoline anticancer drug, TAS-103, in humans. Xenobiotica. 2002 Jan;32(1):63-72. PubMed PMID: 11820510.

8: Okamoto R, Takano H, Sekikawa T, Tanaka T, Toyada M, Ukon K, Tanimoto K, Kumazaki T, Nishiyama M. Unique action determinants of double acting topoisomerase inhibitor, TAS-103. Int J Oncol. 2001 Nov;19(5):921-7. PubMed PMID: 11604989.

9: Ewesuedo RB, Iyer L, Das S, Koenig A, Mani S, Vogelzang NJ, Schilsky RL, Brenckman W, Ratain MJ. Phase I clinical and pharmacogenetic study of weekly TAS-103 in patients with advanced cancer. J Clin Oncol. 2001 Apr 1;19(7):2084-90. PubMed PMID: 11283142.

10: Etiévant C, Kruczynski A, Barret JM, Perrin D, van Hille B, Guminski Y, Hill BT. F 11782, a dual inhibitor of topoisomerases I and II with an original mechanism of action in vitro, and markedly superior in vivo antitumour activity, relative to three other dual topoisomerase inhibitors, intoplicin, aclarubicin and TAS-103. Cancer Chemother Pharmacol. 2000;46(2):101-13. PubMed PMID: 10972479.

11: Kluza J, Lansiaux A, Wattez N, Mahieu C, Osheroff N, Bailly C. Apoptotic response of HL-60 human leukemia cells to the antitumor drug TAS-103. Cancer Res. 2000 Aug 1;60(15):4077-84. PubMed PMID: 10945613.

12: Padget K, Stewart A, Charlton P, Tilby MJ, Austin CA. An investigation into the formation of N- [2-(dimethylamino)ethyl]acridine-4-carboxamide (DACA) and 6-[2-(dimethylamino)ethylamino]- 3-hydroxy-7H-indeno[2, 1-C]quinolin-7-one dihydrochloride (TAS-103) stabilised DNA topoisomerase I and II cleavable complexes in human leukaemia cells. Biochem Pharmacol. 2000 Sep 15;60(6):817-21. PubMed PMID: 10930536.

13: Aoyagi Y, Kobunai T, Utsugi T, Wierzba K, Yamada Y. Establishment and characterization of 6-[[2-(Dimethylamino)ethyl]amino]-3-hydroxy-7H-indeno[2,1-c]quinolin-7-one dihydrochloride (TAS-103)-resistant cell lines. Jpn J Cancer Res. 2000 May;91(5):543-50. PubMed PMID: 10835500.

14: Ishida K, Asao T. Interaction of a novel antitumor agent TAS-103 with DNA. Nucleic Acids Symp Ser. 1999;(42):129-30. PubMed PMID: 10780413.

15: Minderman H, Wrzosek C, Cao S, Utsugi T, Kobunai T, Yamada Y, Rustum YM. Mechanism of action of the dual topoisomerase-I and -II inhibitor TAS-103 and activity against (multi)drug resistant cells. Cancer Chemother Pharmacol. 2000;45(1):78-84. PubMed PMID: 10647506.

16: Parajuli P, Yano S, Nishioka Y, Nokihara H, Hanibuchi M, Nishimura N, Utsugi T, Sone S. Therapeutic efficacy of a new topoisomerase I and II inhibitor TAS-103, against both P-glycoprotein-expressing and -nonexpressing drug-resistant human small-cell lung cancer. Oncol Res. 1999;11(5):219-24. PubMed PMID: 10608616.

17: Fortune JM, Velea L, Graves DE, Utsugi T, Yamada Y, Osheroff N. DNA topoisomerases as targets for the anticancer drug TAS-103: DNA interactions and topoisomerase catalytic inhibition. Biochemistry. 1999 Nov 23;38(47):15580-6. PubMed PMID: 10569942.

18: Byl JA, Fortune JM, Burden DA, Nitiss JL, Utsugi T, Yamada Y, Osheroff N. DNA topoisomerases as targets for the anticancer drug TAS-103: primary cellular target and DNA cleavage enhancement. Biochemistry. 1999 Nov 23;38(47):15573-9. PubMed PMID: 10569941.

19: Ohyama T, Li Y, Utsugi T, Irie S, Yamada Y, Sato T. A dual topoisomerase inhibitor, TAS-103, induces apoptosis in human cancer cells. Jpn J Cancer Res. 1999 Jun;90(6):691-8. PubMed PMID: 10429663.

20: Aoyagi Y, Kobunai T, Utsugi T, Oh-hara T, Yamada Y. In vitro antitumor activity of TAS-103, a novel quinoline derivative that targets topoisomerases I and II. Jpn J Cancer Res. 1999 May;90(5):578-87. PubMed PMID: 10391099.