212631-79-3
212631-79-3 structure
- Name: PD184352 (CI-1040)
- Chemical Name: pd 184352
- CAS Number: 212631-79-3
- Molecular Formula: C17H14ClF2IN2O2
- Molecular Weight: 478.659
- Catalog: Biochemical Inhibitor Mitogen-activated protein kinase (MAPK) MEK inhibitor
- Create Date: 2018-06-11 18:52:00
- Modify Date: 2024-01-02 11:34:36
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CI-1040 (PD184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.
| Name | pd 184352 |
|---|---|
| Synonyms |
Benzamide, 2-[(2-chloro-4-iodophenyl)amino]-N-(cyclopropylmethoxy)-3,4-difluoro-
CI-1040 2-[(2-Chloro-4-iodophenyl)amino]-N-(cyclopropylmethoxy)-3,4-difluorobenzamide 2-(2-Chloro-4-iodophenylamino)-N-cyclopropylmethoxy-3,4-difluorobenzamide CI-1040 2-((2-Chloro-4-iodophenyl)amino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide 2-(2-chloro-4-iodophenylamino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide |
| Description | CI-1040 (PD184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1. |
|---|---|
| Related Catalog | |
| Target |
MEK1:17 nM (IC50) |
| In Vitro | CI-1040 directly inhibits MEK1 with an IC50 of 17 nM. It has also been shown to have little activity against a panel of related kinases with IC50 values more than 2.5 orders of magnitude higher. Treatment of whole cells with CI-1040 completely inhibits the mitogen-stimulated phosphorylation of ERK. CI-1040 at a concentration of 1 μM is found to inhibit phosphorylation of ERK1 and ERK2 by 99% and 92%, respectively in MDA-MB-231 breast cancer cells[1]. CI-1040 induces apoptosis and inhibits proliferation in U-937 cells in a dose and time-dependent manner. CI-1040 induces a significant increase in PUMA mRNA and protein levels[2]. |
| In Vivo | The systemic administration of the MEK inhibitor CI-1040 reduces adenoma formation to a third and significantly restores lung structure. The proliferation rate of lung cells of mice treated with CL-1040 is decreased without any obvious effects on differentiation of pneumocytes[3]. |
| Cell Assay | The MEK inhibitor CI-1040 is dissolved in DMSO as 10 mM stock solutions and used in cell culture at final concentration 50 mg/mL. U-937 cells are pretreated for 24 hrs with 5 and 20 uM CI- 1040, then transfected with wt-p53 siRNA or PUMA siRNA for 48 hrs. Then 20 mL of MTT solution are added to each well and incubated further for 2 hours. Upon termination, the supernatant is aspirated and the MTT formazan formed by metabolically viable cells is dissolved in 100 mL of isopropanol. The plates are mixed for 30 minutes on a gyratory shaker, and absorbance is measured at 595 nm using a plate reader[2]. |
| Animal Admin | Mice: The lung cancer mouse model is generated by targeting constitutively active C-Raf kinase to the lung. BAY 43-9006 or CI-1040 is daily intraperitoneal injected at a dose of 100 mg/kg from 4 months of age over a period of 21 days. Lungs were isolated and analyzed at the end of the treatment period[3]. |
| References |
| Density | 1.7±0.1 g/cm3 |
|---|---|
| Melting Point | 166-169ºC |
| Molecular Formula | C17H14ClF2IN2O2 |
| Molecular Weight | 478.659 |
| Exact Mass | 477.975647 |
| PSA | 50.36000 |
| LogP | 8.01 |
| Index of Refraction | 1.656 |
| Storage condition | -20°C Freezer |
| Water Solubility | DMSO: ≥30mg/mL |
| Symbol |
GHS09 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H400 |
| Precautionary Statements | P273 |
| Hazard Codes | N |
| Risk Phrases | 50/53 |
| Safety Phrases | 60-61 |
| RIDADR | UN 3077 9 / PGIII |
| HS Code | 2924299090 |
| HS Code | 2924299090 |
|---|---|
| Summary | 2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0% |