TAS-103 HCL|BMS-247615; TAS103|Provide by DC CHEM

Cas No.:	174634-08-3
Synonyms:	BMS-247615; TAS103; TAS 103; BMS247615; BMS 247615, BMS-247615; TAS103; TAS 103; BMS247615; BMS 247615
SMILES:	O=C(C1=C2C3=CC=C(O)C=C3N=C1NCCN(C)C)C4=C2C=CC=C4
Formula:	C₂₀H₁₉N₃O₂
M.Wt:	333.38
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

TAS-103(BMS-247615) is a dual inhibitor of topoisomerase-I (topo-I) and topoisomerase-II (topoII). IC50 value: Target: Topoisomerase in vitro: TAS-103 was effective in inhibiting in vitro proliferation of human SCLC (SBC-3 and H69) cells and their drug-resistant variants SBC-3/ADM or SBC-3/CDDP and H-69/VP, respectively. SBC-3/ADM and H-69/VP expressed high P-gp, whereas SBC-3/CDDP did not . TAS-103 disrupts SRP complex formation and reduces the amount of SRP14 and SRP19. TAS-103 treatment and RNAi-mediated knockdown of SRP54 or SRP14 promoted accumulation of the exogenously expressed chimeric protein interleukin-6-FLAG inside cells . In 13 human cancer cell lines, MGMT expression correlated with IC50 for TAS-103, whereas gamma-GCS expression inversely correlated with the IC50 value, suggesting MGMT may work to decrease TAS-103 activity but gamma-GCS may increase it . in vivo: TAS-103 also effectively reduced the tumor growth (more than 50% inhibition) of the parental as well as MDR SCLC cells grown SC in nude mice . Thirty-two patients were treated with escalating doses (50 to 200 mg/m(2)) of TAS-103, administered intravenously over 1 hour each week for 3 weeks. Pharmacokinetic analysis was performed at the 130-, 160-, and 200-mg/m(2) dose levels .For the detailed information of TAS-103 HCL, the solubility of TAS-103 HCL in water, the solubility of TAS-103 HCL in DMSO, the solubility of TAS-103 HCL in PBS buffer, the animal experiment (test) of TAS-103 HCL, the cell expriment (test) of TAS-103 HCL, the in vivo, in vitro and clinical trial test of TAS-103 HCL, the EC50, IC50,and affinity,of TAS-103 HCL, Please contact DC Chemicals.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC47325	Huanglongmycin N	Huanglongmycin N is a DNA topoisomerase I inhibitor (EC50 = 14 μM).
DC46831	T-2513 hydrochloride	T-2513 hydrochloride is a selective topoisomerase I inhibitor. T-2513 hydrochloride binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death.
DC46830	Intoplicine dimesylate	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.
DC45986	Hippeastrine	Hippeastrine, an active alkaloid, exhibits a good dose-dependent inhibitory effect against topoisomerase I (Top I) with an IC50 at 7.25 μg/mL. Antiproliferative and anticancer activities.
DC45556	(±)-Evodiamine	(±)-Evodiamine, a quinazolinocarboline alkaloid, is a Top1 inhibitor. Evodiamine exhibits anti-inflammatory, antiobesity, and antitumor effects. (±)-Evodiamine inhibits the proliferation of a wide variety of tumor cells by inducing their apoptosis.
DC45283	Coralyne chloride	Coralyne chloride is a protoberberine alkaloid with potent anti-cancer activities. Coralyne chloride acts as a potent topoisomerase I poison and induces Top I mediated DNA cleavage. Coralyne chloride can be used for preparing coralyne derivatives as DNA binding fluorescent probes.
DC44139	PluriSIn #2	PluriSIn #2 is a selective transcriptional inhibitor of topoisomerase II α (TOP2A). PluriSIn #2 is a compound that selectively eliminates undifferentiated human pluripotent stem cells (hPSCs).
DC42296	Exatecan D5 Mesylate	Exatecan D5 Mesylate (DX8951f-D5) is deuterium labeled Exatecan Mesylate. Exatecan Mesylate is a DNA topoisomerase I, with an IC50 of 0.975 μg/mL.
DC41162	Gimatecan	Gimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.
DC41116	Merbarone	Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage. Merbarone is an anticancer agent.

TAS-103(BMS247615)