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MRX-2843 (UNC2371) is a potent and orally active inhibitor of MERTK and FLT3(IC50s of 1.3 nM and 0.64 nM, respectively).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $59 | In Stock | |
5 mg | $147 | In Stock | |
10 mg | $239 | In Stock | |
25 mg | $478 | In Stock | |
50 mg | $689 | In Stock | |
100 mg | $982 | In Stock | |
1 mL x 10 mM (in DMSO) | $159 | In Stock |
Description | MRX-2843 (UNC2371) is a potent and orally active inhibitor of MERTK and FLT3(IC50s of 1.3 nM and 0.64 nM, respectively). |
Targets&IC50 | FLT3:0.64 nM, MerTK:1.3 nM |
In vitro | 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]. |
In vivo | 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]. |
Alias | UNC2371 |
Molecular Weight | 488.67 |
Formula | C29H40N6O |
Cas No. | 1429882-07-4 |
Smiles | CN1CCN(Cc2ccc(cc2)-c2cn([C@H]3CC[C@H](O)CC3)c3nc(NCCC4CC4)ncc23)CC1 |
Relative Density. | 1.31 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 26.25 mg/mL (53.72 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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