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MRX-2843 is a potent and orally active inhibitor of MERTK and FLT3 with IC50 values of 1.3 nM and 0.64 nM, respectively. MRX-2843 induces apoptosis and inhibits colony formation in AML cell lines. In MOLM-14 cells, treatment with MRX-2843 inhibits phosphorylation of FLT3 and downstream signaling through STAT5, ERK1/2 and AKT.
In vivo, 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).
| Molecular Weight | 488.67 |
| Formula | C29H40N6O |
| CAS Number | 1429882-07-4 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related FLT3 Products |
|---|
| Quizartinib (AC220)
Quizartinib (AC220) is a uniquely potent and selective FLT3 inhibitor. |
| KW-2449
KW-2449 is a novel multitargeted kinase inhibitor of FLT3, ABL and Aurora kinase with IC50 values of 6.6 nM, 14 nM and 48 nM. |
| Tandutinib
Tandutinib (MLN518, CT53518) is an orally active multitargeted tyrosine kinase inhibitor of FLT3 (IC50 = 0.22 μM), and it also inhibits c-Kit and PDGFR with IC50 values of 0.17 μM and 0.20 μM, respectively. Tandutinib has the ability to cross the blood-brain barrier. |
| FF-10101
FF-10101 is a novel irreversible FLT3 inhibitor. |
| TCS 359
TCS 359 is a potent FLT3 inhibitor with IC50 of 42 nM. |
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Products are for research use only. Not for human use. We do not sell to patients.
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