[CAS NO. 1245792-67-9] BCI-215
PRODUCTS SPECIFICATIONS [1245792-67-9]
DESCRIPTION [1245792-67-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 396.32 |
| Molecular Formula | C22H22BrNO |
| SMILES | O=C1/C(C(NC2CCCCC2)C3=C1C=CC(Br)=C3)=C/C4=CC=CC=C4 |
1 Publications Citing Use of MCE
Summary
BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells [1] [2] .
IC50 & Target
DUSP-MKP [1]
In Vitro
BCI-215 concentration-dependently increases pERK levels in DUSP-overexpressing cells with IC
50
value in the micromolar range
[1]
.
BCI-215 (1-20 μM; 6 hours) retains fibroblast growth factor hyperactivating and cellular DUSP6/MKP-3 and DUSP1/MKP-1 inhibitory activity but is nontoxic to zebrafish embryos and an endothelial cell line
[1]
.
BCI-215 inhibits survival and motility of MDA-MB-231 human breast cancer cells but does not affect viability of cultured hepatocytes
[2]
.
BCI-215 is completely devoid of hepatocyte toxicity up to 100 µM
[2]
.
BCI-215 does not generate ROS in hepatocytes or in developing Zebrafish larvae.
BCI-215 (22 µM) has antimigratory and proapoptotic activities in breast cancer cells that correlate with induction of ERK phosphorylation
[2]
.
BCI-215 (20 µM; 1 hour) induces mitogenic and stress signaling in cancer cells without generating ROS
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Apoptosis Analysis [2]
| Cell Line: | MDA-MB-231 cells |
| Concentration: | 22 µM |
| Incubation Time: | |
| Result: | Caused apoptotic cell death at concentrations that induce ERK phosphorylation. |
Western Blot Analysis [2]
| Cell Line: | MDA-MB-231 cells |
| Concentration: | 20 µM |
| Incubation Time: | 1 hour |
| Result: | Induced a stress response that is not dependent on oxidation. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 33.33 mg/mL ( 84.10 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 0.83 mg/mL (2.09 mM); Clear solution
References
- [1] Korotchenko VN, et al. In vivo structure-activity relationship studies support allosteric targeting of a dual specificity phosphatase. Chembiochem. 2014 Jul 7;15(10):1436-45.
- [2] Kaltenmeier CT, et al. A Tumor Cell-Selective Inhibitor of Mitogen-Activated Protein Kinase Phosphatases Sensitizes Breast Cancer Cells to Lymphokine-Activated Killer Cell Activity. J Pharmacol Exp Ther. 2017 Apr;361(1):39-50.
Synonyms
