2024年9月1日 · MRX-2843 is a promising inhibitor of FLT3 and MERTK. We recently demonstrated that MRX-2843 is equally potent as gilteritinib in FLT3-ITD AML cell lines in vitro and primary patient samples ex vivo. In this study, we investigated the combination of VEN and MRX-2843 against FLT3-ITD AML cells.

2022年9月3日 · Both gilteritinib and MRX-2843 in combination with AZD5991 show synergistic antileukemic activity against AraC-resistant FLT3-mutated AML cells. Our findings provide support for the development of the Mcl-1 inhibitors in combination with FLT3 inhibitors for the treatment of AML, including those with acquired resistance to AraC.

AZD5991 enhances the antileukemic activity of the FLT3 inhibitors gilteritinib and MRX-2843 against FLT3-mutated AML in vitro, warranting further development. FMS-like tyrosine kinase 3 (FLT3)-internal tandem duplication (FLT3-ITD) mutations occur in about 25% of all acute myeloid leukemia (AML) patients and confer a poor prognosis.

MER tyrosine kinase (MERTK), a member of the TAM (TYRO3, AXL, MERTK) P1.12A.10 family of receptor tyrosine kinases mediates resistance to osimertinib. MRX-2843 is a novel small molecule MERTK TKI; we conducted a phase Ib study to evaluate the safety and efficacy of MRX-2843 in combination with osimertinib in participants (pts) with EGFRm NSCLC.

2022年9月3日 · FLT3 inhibitors have been developed to treat patients with FLT3-mutated AML and have shown promise, though the acquisition of resistance occurs, highlighting the need for combination therapies to prolong the response to FLT3 inhibitors. In this study, we investigated the selective Mcl-1 inhibitor AZD5991 in combination with the FLT3 inhibitors ...

2021年5月12日 · The BAT motif inhibits the ability of the Mre11-Rad50-Xrs2 complex (MRX) to capture DNA ends. It acts through a direct contact with Rad50 ATP-binding Head domains.

2016年3月18日 · A novel compound MRX-2843 more than doubled the median days of survival in laboratory models with a drug-resistant form of the acute myeloid leukemia, scientists report in a new article.

2022年8月1日 · The MERTK ligand GAS6 promoted downstream oncogenic signaling in EGFR-mutated (EGFRMT) NSCLC cells treated with OSI, suggesting a role for MERTK activation in OSI resistance. Indeed, treatment with MRX-2843, a first-in-class MERTK kinase inhibitor, resensitized GAS6-treated NSCLC cells to OSI.

2024年9月1日 · In this study, we investigated the combination of VEN and MRX-2843 against FLT3 -ITD AML cells. We found that VEN synergistically enhances cell death induced by MRX-2843 in FLT3 -mutated AML cell lines and primary patient samples.

2007年5月4日 · We linked a new MRX condition, MRX87, to Xp22-Xp21 interval. This is one of the three hot spot regions for X-linked mental retardation containing ARX, a gene prominently mutated in both syndromic and non syndromic cognitive impairments.