MRX-2843
作者：齐岳
发布时间：2023-08-22
09:28:22
点击数：
产品名称：MRX-2843
产品描述：
| 产品描述 | MRX-2843 is a potent and orally active inhibitor of MERTK and FLT3(IC50s of 1.3 nM and 0.64 nM, respectively). |
| 靶点活性 | FLT3:0.64 nM, MERTK:1.3 nM |
| 体外活性 | MRX-2843, a type 1 small-molecule tyrosine kinase inhibitor that abrogates activation of both MERTK and FLT3 and their downstream effectors.?MRX-2843 treatment induces apoptosis and inhibits colony formation in AML cell lines and primary patient samples expressing MERTK and/or FLT3-ITD, with a wide therapeutic window compared with that of normal human cord blood cells[1]. |
| 体内活性 | In murine orthotopic xenograft models, once-daily oral therapy prolonged survival 2- to 3-fold over that of vehicle-treated controls.?Additionally, MRX-2843 retained activity against quizartinib-resistant FLT3-ITD-mutant proteins with clinically relevant alterations at the D835 or F691 loci and prolonged survival in xenograft models of quizartinib-resistant AML.?Together, these observations validate MRX-2843 as a translational agent and support its clinical development for the treatment of AML[1]. |
| 别名 | UNC2371 |
| 分子量 | 488.67 |
| 分子式 | C29H40N6O |
| CAS No. | 1429882-07-4 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 26.25mg/ml (53.72 Mm),Need ultrasonic
( < 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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