| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
ML230 targets the ATP-binding cassette transporter ABCG2 (BCRP), a protein that pumps various substrates out of cells and contributes to multidrug resistance in cancer. By inhibiting ABCG2, ML230 can reverse drug resistance and increase the intracellular accumulation of chemotherapeutic agents.
|
|---|---|
| ln Vitro |
In vitro, ML230 inhibits ABCG2 with an EC50 of 0.13 μM and shows 36-fold selectivity over ABCB1. It selectively inhibits JC-1 efflux in Ig-MXP3 cells overexpressing ABCG2. ML230 enhances inhibition of IGROV-1/T8 ovarian cancer cell colony formation induced by topotecan.
|
| ln Vivo |
In vivo, intratumoral injection of ML-230 (100 nM) and topotecan reduces tumor size in an IGROV-1/T8 mouse xenograft model.
|
| Enzyme Assay |
The in vitro transporter inhibition assay for ML230 involves measuring the efflux of a fluorescent substrate, such as JC-1, from cells overexpressing ABCG2. The EC50 is determined from dose-response curves.
|
| Cell Assay |
Cellular assays for ML230 involve treating drug-resistant cancer cells with the compound and measuring the accumulation of chemotherapeutic agents.
|
| Animal Protocol |
In vivo animal studies for ML230 have been conducted in an IGROV-1/T8 mouse xenograft model.
|
| ADME/Pharmacokinetics |
ML230 has a molecular weight of 439.475 g/mol and a molecular formula of C25H21N5O3. It is soluble in DMSO.
|
| Toxicity/Toxicokinetics |
The toxicity profile of ML230 is limited. As a research compound, comprehensive toxicological evaluations have not been published.
|
| References | |
| Additional Infomation |
3-Furanyl-[4-[5-(2-furanyl)-2-phenyl-7-pyrazolo[1,5-a]pyrimidinyl]-1-piperazinyl] methyl ketone is an N-arylpiperazine.
ML230 is a research compound for studying ABC transporters and multidrug resistance. It has not entered clinical trials. Its mechanism involves ABCG2 inhibition. |
| Molecular Formula |
C25H21N5O3
|
|---|---|
| Molecular Weight |
439.465945005417
|
| Exact Mass |
439.164
|
| CAS # |
1776055-05-0
|
| PubChem CID |
44640177
|
| Appearance |
Light yellow to yellow solid powder
|
| LogP |
3.2
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
33
|
| Complexity |
681
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C1=COC=C1)N1CCN(C2=CC(C3=CC=CO3)=NC3=CC(C4C=CC=CC=4)=NN23)CC1
|
| InChi Key |
LRPGMVPQQLBMNE-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C25H21N5O3/c31-25(19-8-14-32-17-19)29-11-9-28(10-12-29)24-16-21(22-7-4-13-33-22)26-23-15-20(27-30(23)24)18-5-2-1-3-6-18/h1-8,13-17H,9-12H2
|
| Chemical Name |
furan-3-yl-[4-[5-(furan-2-yl)-2-phenylpyrazolo[1,5-a]pyrimidin-7-yl]piperazin-1-yl]methanone
|
| 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 |
| 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 : ~33.33 mg/mL (~75.84 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.69 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2755 mL | 11.3773 mL | 22.7547 mL | |
| 5 mM | 0.4551 mL | 2.2755 mL | 4.5509 mL | |
| 10 mM | 0.2275 mL | 1.1377 mL | 2.2755 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
