产品
编 号：F160921
分子式：C29H40N6O
分子量：488.67
分子式：C29H40N6O
分子量：488.67
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规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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CAS No: 1429882-07-4
产品详情
生物活性：
MRX-2843 (UNC2371) is an orally active, ATP-competitive dual MERTK and FLT3 tyrosine kinases inhibitor (TKI) with enzymatic IC50s of 1.3 nM for MERTK and 0.64 nM for FLT3, respectively.
体内研究：
MRX-2843 is 78% orally bioavailable at a dose of 3 mg/kg with a Cmax of 1.3 μM and a t1/2 of 4.4 hours. In MOLM-14 parental xenografts, both quizartinib and MRX-2843 increase median survival compare with that of vehicle-treated mice (172.5 days versus 40 days and 121 days versus 36 days, respectively, P<0.001). In this model, quizartinib is more effective than MRX-2843 (P<0.005), although higher doses of MRX-2843 are not evaluated. In MOLM-14:D835Y xenografts, quizartinib prolongs survival compare with that of vehicle-treated mice, but the effect is minimal (median survival 45 days vs. 36 days, P<0.001). In MOLM-14:F691L xenografts, treatment with MRX-2843 prolongs survival by almost 2-fold in NSG and NSGS mice (median survival 87 vs. 44.5 days and 87 vs. 48 days, respectively, P<0.005). Increased survival is observed in response to treatment with MRX-2843 versus quizartinib, but the difference is only significant in NSG mice.
体外研究：
In the Kasumi-1 cell line, treatment with MRX-2843 results in dose-dependent inhibition of MERTK phosphorylation. Decreased phosphorylation is evident at concentrations as low as 10 nM, with near-complete abrogation of MERTK activation at 100 to 300 nM. Similarly, treatment of Kasumi-1 cells with MRX-2843 mediates inhibition of downstream signaling through pathways important for tumor cell survival and proliferation. MRX-2843 treatment results in a decrease in relative cell numbers, with an IC50 of 143.5±14.1 nM, indicating that MRX-2843 significantly inhibits tumor cell proliferation and/or survival. Similarly, there are 34.1%±5.6% and 67.1%±2.7% apoptotic and dead cells in NOMO-1 cultures treated with 150 nM or 300 nM MRX-2843, respectively, compare with 6.8%±0.7% in vehicle-treated cultures (PMRX-2843 相关抗体:
MRX-2843 (UNC2371) is an orally active, ATP-competitive dual MERTK and FLT3 tyrosine kinases inhibitor (TKI) with enzymatic IC50s of 1.3 nM for MERTK and 0.64 nM for FLT3, respectively.
体内研究：
MRX-2843 is 78% orally bioavailable at a dose of 3 mg/kg with a Cmax of 1.3 μM and a t1/2 of 4.4 hours. In MOLM-14 parental xenografts, both quizartinib and MRX-2843 increase median survival compare with that of vehicle-treated mice (172.5 days versus 40 days and 121 days versus 36 days, respectively, P<0.001). In this model, quizartinib is more effective than MRX-2843 (P<0.005), although higher doses of MRX-2843 are not evaluated. In MOLM-14:D835Y xenografts, quizartinib prolongs survival compare with that of vehicle-treated mice, but the effect is minimal (median survival 45 days vs. 36 days, P<0.001). In MOLM-14:F691L xenografts, treatment with MRX-2843 prolongs survival by almost 2-fold in NSG and NSGS mice (median survival 87 vs. 44.5 days and 87 vs. 48 days, respectively, P<0.005). Increased survival is observed in response to treatment with MRX-2843 versus quizartinib, but the difference is only significant in NSG mice.
体外研究：
In the Kasumi-1 cell line, treatment with MRX-2843 results in dose-dependent inhibition of MERTK phosphorylation. Decreased phosphorylation is evident at concentrations as low as 10 nM, with near-complete abrogation of MERTK activation at 100 to 300 nM. Similarly, treatment of Kasumi-1 cells with MRX-2843 mediates inhibition of downstream signaling through pathways important for tumor cell survival and proliferation. MRX-2843 treatment results in a decrease in relative cell numbers, with an IC50 of 143.5±14.1 nM, indicating that MRX-2843 significantly inhibits tumor cell proliferation and/or survival. Similarly, there are 34.1%±5.6% and 67.1%±2.7% apoptotic and dead cells in NOMO-1 cultures treated with 150 nM or 300 nM MRX-2843, respectively, compare with 6.8%±0.7% in vehicle-treated cultures (PMRX-2843 相关抗体:
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