MRX-2843
作者：齊岳
發(fā)布時間：2023-08-22
09:28:22
點擊數(shù)：
產(chǎn)品名稱：MRX-2843
產(chǎn)品描述：
| 產(chǎn)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). |
| 靶點活性 | FLT3:0.64 nM, MERTK:1.3 nM |
| 體外活性 | 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]. |
| 體內(nèi)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]. |
| 別名 | UNC2371 |
| 分子量 | 488.67 |
| 分子式 | C29H40N6O |
| CAS No. | 1429882-07-4 |
存儲
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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西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
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