606143-52-6
5-(4-Bromo-2-chlorophenylamino)-4-fluoro-1-methyl-1H-benzimidazole-6-carbohydroxamic acid 2-hydroxyethyl ester
CAS: 606143-52-6
Molecular Formula: C17H15BrClFN4O3
606143-52-6 - Names and Identifiers
606143-52-6 - Physico-chemical Properties
| Molecular Formula | C17H15BrClFN4O3 |
| Molar Mass | 457.68 |
| Density | 1.69 |
| Melting Point | >219°C (dec.) |
| Solubility | Soluble in DMSO (92 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (<1 mg/ |
| Appearance | Beige powder. |
| Color | White |
| pKa | 14.20±0.10(Predicted) |
| Storage Condition | -20° |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months. |
| Use | A MEK-1 non-ATP competitive inhibitor. |
| In vitro study | AZD6244 is a non-competitive inhibitor of ATP, inactivating ERK1/2 phosphorylation at IC50 concentrations less than 40 nM. AZD6244 also inhibits the growth of primary HCC cells by inhibiting the phosphorylation of ERK1/2 and p90RSK, accompanied by enhanced caspase-3 and caspase-7 division, and the increase of the broken Poly (ADP-ribose) polymerase. AZD6244 has little effect in P38,JNK,PI3K, and MEK5/ERK5 pathways. AZD6244 is sensitive to the detection of raf mutations in breast cancer cell lines and ras mutations in non-small cell lung cancer cell lines. |
| In vivo study | In vivo studies have shown that AZD6244 significantly inhibits ERK1/2 phosphorylation in 2-1318, 5-1318, and 26-1004 4-1318 grafts, and induces apoptosis by activating the caspase pathway in Primary 2-1318 cells. HT-29 the transplanted tumor is a rectal tumor model with B- raf mutation, AZD6244 can inhibit tumor growth in HT-29 transplanted tumor at a dose of 100 mg/kg, and the tumor index under the effect of AZD6244 is better than that under the effect of gemcitabine. In addition, AZD6244 can inhibit the growth of HCC xenografts, and the growth of HCC xenografts is related to the increase of cell apoptosis and the down regulation of cell cycle regulation. Includes: cyclin D1, cdc-2, CDK 2 ,CDK4, cyclin B1, and c-Myc. |
606143-52-6 - Risk and Safety
| HS Code | 29349990 |
606143-52-6 - Introduction
Selumetinib (AZD6244) is a potent and highly selective MEK1 inhibitor with IC50 of 14 nM, also inhibits ERK1/2 phosphorylation, IC50 of 10 nM, and has no inhibitory effect on p38α, MKK6, EGFR, ErbB2, ERK2, B- Raf, etc. Phase 3.
Last Update：2022-10-16 17:27:00
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CAS: 606143-52-6
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Product Name: Selumetinib Visit Supplier Webpage Request for quotationCAS: 606143-52-6
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: Selumetinib (AZD6244) Visit Supplier Webpage Request for quotationCAS: 606143-52-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Product Name: Selumetinib Request for quotation
CAS: 606143-52-6
Tel:
Email: chemedpharma@163.com
Mobile: 13256704711
CAS: 606143-52-6
Tel:
Email: chemedpharma@163.com
Mobile: 13256704711
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