MRX-2843

SKU: orb1308007

Description

MRX-2843 (UNC2371) is a potent, orally bioavailable small molecule inhibitor targeting MERTK and FLT3 with IC50 values of 1.3 nM and 0.64 nM, respectively. It is a valuable research tool for studying oncology, particularly in acute myeloid leukemia (AML), and has demonstrated activity in both cellular assays and in vivo tumor models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1429882-07-4
• MW: 488.67
• Purity: 99.51% (May vary between batches)
• Formula: C₂₉H₄₀N₆O
• SMILES: CN1CCN(Cc2ccc(cc2)-c2cn([C@H]3CC[C@H](O)CC3)c3nc(NCCC4CC4)ncc23)CC1
• Target: FLT
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.09 mM);DMSO:26.25 mg/mL (53.72 mM)

Bioactivity

• Target IC50:
  FLT3:0.64 nM|MerTK:1.3 nM
• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MRX-2843, MRX 2843, MRX2843, inhibit, MERTK, Inhibitor, FLT3, Fms like tyrosine kinase 3, CD135, Cluster of differentiation antigen 135, UNC2371, UNC-2371, UNC 2371

Compound Identifiers

PubChem CID

89495685