RMC-4550

Catalog No.S8718

RMC-4550 Chemical Structure

Molecular Weight(MW): 437.36

RMC-4550 is a potent SHP-2inhibitor with an IC50 of 1.55 nM and it has no significant activity vs. 468 kinases, the catalytic domain of 15 phosphatases and other cellular targets including GPCRs, transporters and ion channels.

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Choose Selective phosphatase Inhibitors

Biological Activity

Description RMC-4550 is a potent SHP-2inhibitor with an IC50 of 1.55 nM and it has no significant activity vs. 468 kinases, the catalytic domain of 15 phosphatases and other cellular targets including GPCRs, transporters and ion channels.
In vitro

RMC-4550 inhibits purified, activated full length human SHP2 with an IC50 of 1.55 nM, and has cellular IC50 of 39 nM in PC9 cells with a pERK readout. RMC-4550 has no detectable inhibitory activity up to 10 µM against the catalytic domain of SHP2, a panel of 14 additional protein phosphatases, and a panel of 468 protein kinases. RMC-4550 exhibits low to moderate cross species in vitro intrinsic clearance (3.6-24 µL/min/million cells) in hepatocytes, a high passive permeability (458 nm/s) and efflux ratio of 1[1].

Assay
Methods Test Index PMID
Growth inhibition assay
Cell proliferation ; 

PubMed: 30104724     


Effect of RMC-4550 on proliferation of NF1(LOF) cells in 3D culture. One day after seeding cells were treated with RMC-4550 and cell viability measured on Day 7 using CTG. Figure shows mean +/− S.D.; n = 3 independent experiments performed in technical duplicate. 

30104724
In vivo

RMC-4550 has moderate to high bioavailability and has a half-life amenable for once daily oral administration. In the EGFR-driven KYSE-520 human esophageal cancer xenograft model, RMC-4550 has a dose dependent efficacy consistent with target modulation, assessed by phospho-ERK inhibition in tumors. RMC-4550 is well tolerated at doses that achieved maximal and sustained efficacy in this model[1].

Protocol

Cell Research:

[2]

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  • Cell lines: HEK-293 cells
  • Concentrations: --
  • Incubation Time: 1 h
  • Method:

    30,000 HEK-293 cells per well are plated in 96-well plates in Biotin-free RPMI supplemented with 0.1% fetal bovine serum, 0.02% bovine serum albumin and 1% penicillin/streptomycin. Expression of SOS1 constructs is induced by the addition 0.1 μg/mL doxycycline for 24 hours. Cells are treated with serial 3-fold dilutions of RMC-4550 diluted in biotin-free media supplemented with 0.02% bovine serum albumin and 1% penicillin/streptomycin (final DMSO concentration equivalent to 0.1%) for one hour. For the final 5 minutes of drug treatment, cells are stimulated with 50 ng/mL EGF, lysed and subjected to ERK1/2 phosphorylation analysis.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: Female (6-8 week old) athymic nude mice implanted with NCI-H358 (Balb/c strain background) or MIA PaCa-2 (NCR nude strain background) tumor cells subcutaneously in the flank
  • Formulation: Captisol/ 50 mM acetate buffer pH4.6 (10%/90%, w/v)
  • Dosages: 3-60 mg/kg
  • Administration: PO
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (228.64 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 437.36
Formula

C21H26Cl2N4O2

CAS No. 2172651-73-7
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID