EOC317
作者：齐岳
发布时间：2023-08-25
09:06:58
点击数：
产品名称：EOC317
产品描述：
| 产品描述 | ACTB-1003 is an oral kinase inhibitor (IC50: 6/2/4 nM, for FGFR1/VEGFR2/Tie-2). |
| 靶点活性 | FGFR1:6 nM, Tie-2:4 nM, VEGFR2:2 nM |
| 体外活性 | ACTB-1003 targets cancer mutations via FGFR inhibition FGFR1 (IC50: 6 nM), angiogenesis through inhibition of VEGFR2 (2 nM) and Tie-2 (4 nM), and induces apoptosis likely by targeting RSK (5 nM) and p70S6K (32 nM). In cell lines with FGFR genetic alterations - OPM2 human multiple myeloma and the murine leukemia Ba/F3-TEL-FGFR1, ACTB-1003 can markedly and dose-dependently inhibit tumor growth. OPM2 cells harbor the FGFR3 t (4:14) translocation, FGFR3 K650E mutation and PTEN deletion while the Ba/F3-TEL-FGFR1 cells are driven by FGFR1 over-expression. |
| 体内活性 | ACTB-1003 inhibit tumor angiogenesis evident by the inhibition of CD31 staining in tumor sections. The combination ACTB-1003 with 5-FU or paclitaxel not diminish the activity or increasing the toxicity of these chemotherapy agents in the HCT-116 colon tumor xenograft model. |
| 别名 | ACTB1003, ACTB 1003, ACTB-1003 |
| 分子量 | 591.543 |
| 分子式 | C27H26F5N7O3 |
| CAS No. | 939805-30-8 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 35 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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