MRX-2843 (UNC2371) | Mer inhibitor | Probechem Biochemicals

Chemical Structure : MRX-2843

CAS No.: 1429882-07-4

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MRX-2843 (UNC2371, MRX2843)

货号: 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.

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5 mg	￥1580	In stock
10 mg	￥2480	In stock
25 mg	￥4280	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	488.680
分子式	C29H40N6O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
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

参考文献

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.

MRX-2843 (UNC2371, MRX2843)

生物&药学活性

物理化学性质&存储条件

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MRX-2843 (UNC2371, MRX2843)

生物&药学活性

物理化学性质&存储条件

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