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| 10mg |
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| 25mg |
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| 100mg |
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Purity: ≥98%
Indotecan (LMP400; NSC724998) is a novel, potent and selective topoisomerase I inhibitor with IC50 values of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. It is undergoing Phase I trials and may have anticancer activity. Inhibitors of human nuclear type IB topoisomerase (Top1) are potent and commonly used anticancer drugs.
| Targets |
Topoisomerase I
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|---|---|
| ln Vitro |
The Indotecan IC50 values for L. inhibition (48 hours). It was 0.10 μM, 0.10 μM, and 57.16 μM for fantum promastigotes, isolated infected splenocytes, and uninfected splenocytes, respectively [2]. 30 minutes) inhibits L. DNA synthesis and creates covalent complexes of TopI-DNA. infantum cultures [2].
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| ln Vivo |
The livers of mice with visceral leishmaniasis and their own livers are less parasitized when indocean (2.5 mg/kg; intraperitoneally every 2 days for 15 days) is administered [2].
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| Animal Protocol |
Animal/Disease Models: Female balb/c (Bagg ALBino) mouse (4-6 weeks) were injected intravenously (iv) (iv)(iv) with posterior circulating parasites through the tail vein [2]
Doses: 2.5 mg/kg per injection Body weight Route of Administration: intraperitoneal (ip) injection once every 2 days for a total of 15 days (8 doses total) Experimental Results: A dramatic reduction in the number of transformed amastigotes recovered from target organs of drug-treated animals was observed. |
| References |
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| Molecular Formula |
C26H26N2O7
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|---|---|
| Molecular Weight |
478.493847370148
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| Exact Mass |
478.174
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| Elemental Analysis |
C, 65.26; H, 5.48; N, 5.85; O, 23.41
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| CAS # |
915303-09-2
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| Related CAS # |
915303-09-2 (Indotecan; LMP-400); 915360-05-3 ( Indimitecan, LMP776)
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| PubChem CID |
11533060
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| Appearance |
White to gray solid powder
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| LogP |
2.619
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
35
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| Complexity |
872
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1C2C3C(C(N(C=2C2C1=CC1=C(C=2)OCO1)CCCN1CCOCC1)=O)=CC(OC)=C(OC)C=3
|
| InChi Key |
FMFIFGLHVOZDEL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H26N2O7/c1-31-19-10-15-18(13-20(19)32-2)26(30)28(5-3-4-27-6-8-33-9-7-27)24-16-11-21-22(35-14-34-21)12-17(16)25(29)23(15)24/h10-13H,3-9,14H2,1-2H3
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| Chemical Name |
15,16-dimethoxy-20-(3-morpholin-4-ylpropyl)-5,7-dioxa-20-azapentacyclo[10.8.0.02,10.04,8.013,18]icosa-1(12),2,4(8),9,13,15,17-heptaene-11,19-dione
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| Synonyms |
NSC-724998; NSC724998; NSC 724998; LMP-400; LMP400; LMP 400; Indotecan
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: < 1 mg/mL
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0899 mL | 10.4495 mL | 20.8991 mL | |
| 5 mM | 0.4180 mL | 2.0899 mL | 4.1798 mL | |
| 10 mM | 0.2090 mL | 1.0450 mL | 2.0899 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01051635 | Completed | Drug: LMP400 Drug: LMP776 |
Neoplasms Lymphoma |
National Cancer Institute (NCI) |
January 25, 2010 | Phase 1 |
| NCT01794104 | Completed | Drug: LMP400 | Neoplasm Lymphoma |
National Cancer Institute (NCI) |
May 19, 2016 | Phase 1 |
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