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Chemical Structure : MRX-2843
CAS No.: 1429882-07-4
Catalog No.: PC-49059Not For Human Use, Lab Use Only.
MRX-2843 (UNC2371) is a potent, selective, orally available ATP-competitive type 1 inhibitor of both Mer and Flt3 with IC50 of 1.3 and 1.0 nM, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $198 | In stock | |
| 25 mg | $328 | In stock | |
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| 200 mg | Get quote | ||
| 1 g | Get quote |
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MRX-2843 (UNC2371) is a potent, selective, orally available ATP-competitive type 1 inhibitor of both Mer and Flt3 with IC50 of 1.3 and 1.0 nM, respectively.
MRX-2843 shows 15-fold selectivity for these kinases over the other members of the TAM-family, AXL and TYRO-3 (IC50=15 and 17 nM), and other relevant tyrosine kinases.
MRX-2843 (10-100 nM) inhibits MERTK activation and mediates functional antileukemia effects in MERTK-dependent AML models, inhibits MERTK phosphorylation, MRX-2843 (25-300 nM) inhibits downstream signaling through pathways (phosphorylation of ERK1/2, AKT, and STAT6) in Kasumi-1 cells.
MRX-2843 inhibits FLT3 activation and mediates functional antileukemic effects in FLT3-ITD AML models, inhibitsphosphorylation of FLT3 and downstream signaling through STAT5, ERK1/2, and AKT, inhibits clonal expansion in MOLM-14 cultures (IC50=29.5 nM).
MRX-2843 selectively inhibits colony formation in primary AML patient samples and prolongs survival in patient-derived xenograft models of AML.
| M.Wt | 488.680 | |
| Formula | C29H40N6O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
trans-4-[2-[(2-Cyclopropylethyl)amino]-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]cyclohexanol |
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1. Minson KA, et al. JCI Insight. 2016 Mar;1(3):e85630.
2. Yan D, et al. Clin Cancer Res. 2018 Dec 15;24(24):6523-6535.
3. Yan D, et al. J Clin Invest. 2022 Jun 16:e150517.
4. Zhang W, et al. J Med Chem. 2014;57(16):7031–7041.
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