9-氨基喜树碱

9-Aminocamptothecin

	产品编号	CFN90309
	CAS编号	91421-43-1
	分子式 = 分子量	C₂₀H₁₇N₃O₄ = 363.37
	产品纯度	>=98%
	物理属性	Powder
	化合物类型	Alkaloids
	植物来源	The barks of Camptotheca acuminata Decne
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产品名称	产品编号	CAS编号	包装	QQ客服
9-氨基喜树碱	CFN90309	91421-43-1	10mg	QQ客服：2159513211
9-氨基喜树碱	CFN90309	91421-43-1	20mg	QQ客服：2159513211
9-氨基喜树碱	CFN90309	91421-43-1	50mg	QQ客服：2159513211
9-氨基喜树碱	CFN90309	91421-43-1	100mg	QQ客服：2159513211

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Description:

9-Aminocamptothecin is a topoisomerase I inhibitor with potent anticancer activity.In combination with 9-Aminocamptothecin, one 15-mer peptide (SAYAATVRGPLSSAS) has synergistic cytotoxic effects with 9-Aminocamptothecin both in the cytotoxicity assay and in nude mouse xenograft human tumor models.

Targets:

P450 (e.g. CYP17)

In vitro:

Int J Oncol. 2014 Aug;45(2):877-86.

Cytochrome P450 3A-mediated metabolism of the topoisomerase I inhibitor 9-aminocamptothecin: impact on cancer therapy.[Pubmed: 24889073]

The metabolism of 9-Aminocamptothecin (9-AC) was investigated in human and rat liver microsomes.
METHODS AND RESULTS:
In both species 9-Aminocamptothecin was almost exclusively biotransformed to dihydroxy-9-Aminocamptothecin (M1) and monohydroxy-9-Aminocamptothecin (M2). The enzymatic efficiencies of the formation of M1 and M2 (V(max)/K(m)) were 1.7- and 2.7‑fold higher in rat than in human liver microsomes indicating species-related differences in 9-Aminocamptothecin hydroxylation. Incubation in the presence of human recombinant cytochrome P450 (CYP) enzymes demonstrated that the formation of M1 and M2 is mainly catalyzed by CYP3A4 and only to a minor extent by extrahepatic CYP1A1. The predominant role of CYP3A4 was further supported by a dramatic inhibition of metabolite formation in the presence of the CYP3A4 substrates troleandomycin and ketoconazole. Experiments conducted in isolated perfused rat livers further demonstrated that biliary excretion of 9-Aminocamptothecin, M1 and M2 during 60 min of perfusion was pronounced and accounted for 17.7±2.59, 0.05±0.01 and 2.75±0.14% of total 9-Aminocamptothecin applied to the liver, respectively.
CONCLUSIONS:
In summary, this study established that CYP3A-dependent hydroxylation is the main metabolic pathway for 9-Aminocamptothecin in rat and human liver, which have to be taken into consideration during cancer therapy of patients.

In vivo:

Macromol Biosci. 2009 Nov 10;9(11):1135-42.

Antitumor efficacy of colon-specific HPMA copolymer/9-aminocamptothecin conjugates in mice bearing human-colon carcinoma xenografts.[Pubmed: 19685500 ]

The antitumor activity of a colon-specific N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer - 9-aminocamptothecin (9-AC) conjugate (P-9-AC) was assessed in orthotopic and subcutaneous animal (HT29 xenograft) tumor models.
METHODS AND RESULTS:
P-9-AC treatment of mice bearing orthotopic colon tumors, with a dose of 3 mg/kg of 9-AC equivalent every other day for 6 weeks, resulted in regression of tumors in 9 of 10 mice. A lower dose of P-9-AC (1.25 mg/kg of 9-AC equivalent) every other day for 8 weeks inhibited subcutaneous tumor growth in all mice. No liver metastases were observed.
CONCLUSIONS:
Colon-specific release of 9-AC from polymer conjugates enhanced antitumor activity and minimized the systemic toxicity.

Cancer Chemother Pharmacol. 2009 Apr;63(5):793-8.

Phase II study of 9-aminocamptothecin in previously treated lymphomas: results of Cancer and Leukemia Group B 9551.[Pubmed: 18648813]

To evaluate the efficacy and toxicity of the topoisomerase I inhibitor, 9-aminocamptothecin (9-AC), in patients with relapsed lymphoma and to correlate 9-AC plasma concentrations with response and toxicity.
METHODS AND RESULTS:
Eligible patients had relapsed Hodgkin lymphoma (HL) treated with one or two prior regimens, low grade non-Hodgkin's lymphoma (NHL) treated with one or two prior regimens, or aggressive NHL treated with one prior regimen. The first nine patients received 9-AC dimethylacetamide 0.85 mg/m(2) per day intravenously over 72 h every 2 weeks and the remaining 27 patients received 9-AC/colloidal dispersion 1.1 mg/m(2) per day. Patients received a minimum of three cycles unless progression or intolerable toxicity occurred. Responding patients received two cycles past best response with a minimum of six cycles. CALGB 9551 accrued 37 patients from April 1996 through October 2000; one patient with HD, 18 patients with indolent lymphoma, and 17 patients with aggressive lymphoma. The overall response rate was 17%, with response rates of 11% (2 partial responses) in patients with indolent histologies and 23% (1 complete response, 3 partial responses) in patients with aggressive histologies. The patient with HD did not respond. Response rates were similar for both drug formulations. The median remission duration for the six responders was 6.5 months, with one remission lasting longer than 12 months. Significant grade 3 and 4 toxicities included neutropenia (66%), anemia (31%), and thrombocytopenia (36%), with 20% of patients experiencing grade 3 or 4 infection. No treatment related deaths occurred. Steady state serum concentrations did not correlate with patient response or toxicity.
CONCLUSIONS:
Single agent 9-AC has modest activity in aggressive non-Hodgkin's lymphomas.

产品名称	产品编号	CAS编号	分子式 = 分子量	位单	联系QQ
7-乙基-10-羟基喜树碱; 7-Ethyl-10-Hydroxycamptothecin	CFN90335	86639-52-3	C₂₂H₂₀N₂O₅ = 392.4	20mg	QQ客服：2056216494
9-甲氧基喜树碱; 9-Methoxycamptothecine	CFN99729	39026-92-1	C₂₁H₁₈N₂O₅ = 378.38	20mg	QQ客服：215959384
9-氨基喜树碱; 9-Aminocamptothecin	CFN90309	91421-43-1	C₂₀H₁₇N₃O₄ = 363.37	20mg	QQ客服：1457312923
(S)-10-羟基喜树碱; (S)-10-Hydroxycamptothecin	CFN99735	19685-09-7	C₂₀H₁₆N₂O₅ = 364.35	20mg	QQ客服：1457312923
10-甲氧基喜树碱; 10-Methoxycamptothecin	CFN90157	19685-10-0	C₂₁H₁₈N₂O₅ = 378.38	5mg	QQ客服：1457312923
鲁比替康; Rubitecan	CFN93013	91421-42-0	C₂₀H₁₅N₃O₆ = 393.35	5mg	QQ客服：1413575084
10-硝基喜树碱; 10-Nitro-camptothecin	CFN90439	104195-61-1	C₂₀H₁₅N₃O₆ = 393.34	5mg	QQ客服：2056216494
盐酸拓扑替康; Topotecan hydrochloride	CFN90462	119413-54-6	C₂₃H₂₄ClN₃O₅ = 457.9	20mg	QQ客服：2159513211
盐酸依立替康; Irinotecan hydrochloride	CFN90886	100286-90-6	C₃₃H₃₉ClN₄O₆ = 623.2	20mg	QQ客服：1457312923
7-乙基喜树碱; 7-Ethylcamptothecin	CFN90336	78287-27-1	C₂₂H₂₀N₂O₄ = 376.41	20mg	QQ客服：2159513211

	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	2.752 mL	13.7601 mL	27.5202 mL	55.0403 mL	68.8004 mL
5 mM	0.5504 mL	2.752 mL	5.504 mL	11.0081 mL	13.7601 mL
10 mM	0.2752 mL	1.376 mL	2.752 mL	5.504 mL	6.88 mL
50 mM	0.055 mL	0.2752 mL	0.5504 mL	1.1008 mL	1.376 mL
100 mM	0.0275 mL	0.1376 mL	0.2752 mL	0.5504 mL	0.688 mL

9-氨基喜树碱

9-Aminocamptothecin

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