| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 50mg |
|
||
| Other Sizes |
|
| ln Vitro |
Treatment with echinomycin (0-10 nM; 16 hours; U251 cells) markedly and dose-dependently reduced the production of VEGF mRNA produced by hypoxia. With an EC50 of 1.2 nM, echinomycin highly potently and dose-dependently suppresses the hypoxic stimulation of luciferase expression in U251-HRE [1].
|
|---|---|
| ln Vivo |
Through selective depletion of cancer stem cells (CSCs), treatment with Echinomycin (10 μg/kg; i.v.; for 40 days) efficiently eradicates human acute myeloid malignancies and murine lymphoma in xenogeneic models. AML, or leukemia. HIF1α prevents the negative feedback loop in the Notch pathway, which keeps mice lymphoma CSCs alive [2].
|
| Cell Assay |
RT-PCR[1]
Cell Types: U251 Cell Tested Concentrations: 0 nM, 0.625 nM, 1.25 nM, 5 nM, 10 nM Incubation Duration: 16 hrs (hours) Experimental Results: Dramatically inhibited hypoxia-induced VEGF mRNA expression in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: NOD-SCID (severe combined immunodeficient) mouse received 1.8Gy irradiation and intravenous (iv) (iv)injection of peripheral blood cells from AML-71 and AML-150 patients [2]
Doses: 10 μg/kg Route of Administration: intravenous (iv) (iv)injection; intravenous (iv) (iv)injection. Results lasting 40 days: Effective eradication of mouse lymphoma and serially transplantable human AML in xenogeneic models by preferential elimination of CSCs. |
| References | |
| Additional Infomation |
Quinomycin C is a cyclodepsipeptide.
Echinomycin is a cytotoxic polypeptide quinoxaline antibiotic isolated from Streptomyces echinatus that binds to DNA and inhibits RNA synthesis. Echinomycin has been reported in Streptomyces triostinicus, Streptomycetaceae, and Streptomyces echinatus with data available. Echinomycin is a polypeptide quinoxaline antineoplastic antibiotic isolated from the bacterium Streptomyces echinatus. Echinomycin intercalates into DNA at two locations simultaneously in a sequence-specific fashion, thereby inhibiting DNA replication and RNA synthesis. (NCI04) A cytotoxic polypeptide quinoxaline antibiotic isolated from Streptomyces echinatus that binds to DNA and inhibits RNA synthesis. See also: Echinomycin (annotation moved to). |
| Molecular Formula |
C51H64N12O12S2
|
|---|---|
| Molecular Weight |
1101.265
|
| Exact Mass |
1100.42
|
| CAS # |
512-64-1
|
| PubChem CID |
3197
|
| Appearance |
White to off-white solid powder
|
| Density |
1.41 g/cm3
|
| Boiling Point |
1427.2ºC at 760 mmHg
|
| Flash Point |
817ºC
|
| Index of Refraction |
1.536
|
| LogP |
1.826
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
18
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
77
|
| Complexity |
2200
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
AUJXLBOHYWTPFV-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C51H64N12O12S2/c1-25(2)38-49(72)74-22-36(59-42(65)34-21-53-30-17-13-15-19-32(30)57-34)44(67)55-28(6)46(69)63(10)40-48(71)62(9)39(26(3)4)50(73)75-23-35(58-41(64)33-20-52-29-16-12-14-18-31(29)56-33)43(66)54-27(5)45(68)60(7)37(47(70)61(38)8)24-77-51(40)76-11/h12-21,25-28,35-40,51H,22-24H2,1-11H3,(H,54,66)(H,55,67)(H,58,64)(H,59,65)
|
| Chemical Name |
N,N'-((1R,4S,7R,11S,14R,17S,20R,24S)-11,24-diisopropyl-2,4,12,15,17,25-hexamethyl-27-(methylthio)-3,6,10,13,16,19,23,26-octaoxo-9,22-dioxa-28-thia-2,5,12,15,18,25-hexaazabicyclo[12.12.3]nonacosane-7,20-diyl)bis(quinoxaline-2-carboxamide)
|
| Synonyms |
Quinomycin A Antibiotic A 654ISK 302BEchinomycin NSC 526417NSC 13502
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~5.3 mg/mL (~4.81 mM)
|
|---|---|
| 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 | 0.9080 mL | 4.5402 mL | 9.0804 mL | |
| 5 mM | 0.1816 mL | 0.9080 mL | 1.8161 mL | |
| 10 mM | 0.0908 mL | 0.4540 mL | 0.9080 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.
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
