A Mer and FLT3 inhibitor
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MRX-2843

Item No. 27923

Technical Information
Formal Name
trans-4-[2-[(2-cyclopropylethyl)amino]-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-cyclohexanol
CAS Number
1429882-07-4
Molecular Formula
C29H40N6O
Formula Weight
Purity
≥95%
A crystalline solid
Methanol: soluble
λmax
223, 255, 290 nm
SMILES
CN(CC1)CCN1CC(C=C2)=CC=C2C3=CN([C@@H]4CC[C@@H](O)CC4)C5=NC(NCCC6CC6)=NC=C53
InChi Code
InChI=1S/C29H40N6O/c1-33-14-16-34(17-15-33)19-22-4-6-23(7-5-22)27-20-35(24-8-10-25(36)11-9-24)28-26(27)18-31-29(32-28)30-13-12-21-2-3-21/h4-7,18,20-21,24-25,36H,2-3,8-17,19H2,1H3,(H,30,31,32)/t24-,25-
InChi Key
LBEJYFVJIPQSNX-SOAUALDESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    MRX-2843 is an inhibitor of Mer and FMS-like tyrosine kinase 3 (FLT3; IC50s = 1.3 and 1 nM, respectively).1 It also inhibits Axl and Tyro3 (IC50s = 15 and 17 nM, respectively). MRX-2843 (10-300 nM) inhibits Mer phosphorylation in MOLM-14 and MV4-11 acute myeloid leukemia (AML) cells and reduces clonal expansion of Kasumi-1 AML cells (IC50 = 143.5 nM).2 In vivo, MRX-2843 increases survival in NOMO-1 and MOLM-14 AML mouse xenograft models when administered at doses of 65 and 50 mg/kg, respectively.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhang, W., DeRychere, D., Hunter, D., et alUNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor. J. Med. Chem. 57(16), 7031-7041 (2014).

    2. Minson, K.A., Smith, C.C., DeRyckere, D., et alThe MERTK/FLT3 inhibitor MRX-2843 overcomes resistance-conferring FLT3 mutations in acute myeloid leukemia. JCI Insight 1(3), e85630 (2016).