| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
|
Purity: ≥98%
BCI-215 is a novel, potent and selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor which has cytotoxicity for tumor cells but not normal cells.
| ln Vitro |
In DUSP-overexpressing cells, BCI-215 concentration-dependently raises pERK levels with IC50 values in the micromolar range [1]. BCI-215 (1–20 μM; 6 hours) is harmless to zebrafish embryos and endothelial cell lines, but it maintains fibroblast growth factor hyperactivation and cellular DUSP6/MKP-3 and DUSP1/MKP-1 inhibitory action [1]. BCI-215 does not impact the viability of cultured hepatocytes, however it does impair the survival and motility of MDA-MB-231 human breast cancer cells [2]. When used at concentrations up to 100 µM, BCI-215 is totally non-hepatotoxic [2]. Neither growing zebrafish larvae nor hepatocytes produced ROS in response to BCI-215. In breast cancer cells, BCI-215 (22 µM) exhibits pro-apoptotic and anti-migratory properties that are linked to the activation of ERK phosphorylation [2]. BCI-215 (20 µM; 1 h) stimulates stress signaling and mitosis in cancer cells without producing reactive oxygen species (ROS) [2].
|
|---|---|
| Cell Assay |
Apoptosis analysis[2]
Cell Types: MDA-MB-231 Cell Tested Concentrations: 22 µM Incubation Duration: Experimental Results: Caused apoptosis at concentrations that induce ERK phosphorylation. Western Blot Analysis[2] Cell Types: MDA-MB-231 Cell Tested Concentrations: 20 µM Incubation Duration: 1 hour Experimental Results: Induction of oxidative-independent stress response. |
| References |
|
| Additional Infomation |
BCI-215 is an aromatic ketone that is 2,3-dihydro-1H-inden-1-one which is substituted at positions 2, 3, and 5 by (E)-benzylidene, cyclohexylamino, and bromine, respectively. A hyperactivator of fibroblast growth factor signaling in transgenic zebrafish that is devoid of developmental toxicity and restores defective MAPK activity caused by overexpression of DUSP1 and DUSP6 in mammalian cells. It has a role as an antineoplastic agent and an apoptosis inducer. It is a secondary amino compound, an aromatic ketone, an organobromine compound, an enone and a member of indanones.
|
| Molecular Formula |
C22H22BRNO
|
|---|---|
| Molecular Weight |
396.320185184479
|
| Exact Mass |
395.088
|
| CAS # |
1245792-67-9
|
| PubChem CID |
46912328
|
| Appearance |
White to light yellow solid powder
|
| LogP |
5.4
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
25
|
| Complexity |
504
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
BrC1C=CC2C(/C(=C/C3C=CC=CC=3)/C(C=2C=1)NC1CCCCC1)=O
|
| InChi Key |
JGWQWVVSCQBAFC-DEDYPNTBSA-N
|
| InChi Code |
InChI=1S/C22H22BrNO/c23-16-11-12-18-19(14-16)21(24-17-9-5-2-6-10-17)20(22(18)25)13-15-7-3-1-4-8-15/h1,3-4,7-8,11-14,17,21,24H,2,5-6,9-10H2/b20-13+
|
| Chemical Name |
(E)-2-Benzylidene-5-bromo-3-cyclohexylamino-indan-1-one
|
| Synonyms |
BCI-215 BCI 215 BCI215
|
| 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 (~84.10 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (2.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.83 mg/mL (2.09 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 8.3 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 | 2.5232 mL | 12.6161 mL | 25.2321 mL | |
| 5 mM | 0.5046 mL | 2.5232 mL | 5.0464 mL | |
| 10 mM | 0.2523 mL | 1.2616 mL | 2.5232 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
COA
