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RMC-4550

Catalog No. T16762 CAS 2172651-73-7

RMC-4550 is an effective and allosteric inhibitor of SHP2 (IC50: 0.583 nM).

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RMC-4550, CAS 2172651-73-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 56.00
5 mg	In stock	$ 122.00
10 mg	In stock	$ 198.00
25 mg	In stock	$ 455.00
50 mg	In stock	$ 672.00
100 mg	In stock	$ 956.00
1 mL * 10 mM (in DMSO)	In stock	$ 133.00

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Purity: 99.64%

Purity: 98.95%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	RMC-4550 is an effective and allosteric inhibitor of SHP2 (IC50: 0.583 nM).
Targets&IC50	SHP2:0.583 nM
In vitro	RMC-4550 stabilizes the auto-inhibited conformation of wild-type SHP2 enzyme, with a mode of inhibition similar to SHP099. RMC-4550 inhibits the activity of full-length wild-type SHP2 enzyme activated by a di-phosphotyrosine peptide but lacks activity against the free catalytic domain of SHP2 [1].
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[2].

Molecular Weight	437.36
Formula	C21H26Cl2N4O2
CAS No.	2172651-73-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 260 mg/mL (571.61 mM), Sonication is recommended.

References and Literature

1. Nichols RJ, et al. RAS nucleotide cycling underlies the SHP2 phosphatase dependence of mutant BRAF-, NF1- and RAS-driven cancers. Nat Cell Biol. 2018 Sep;20(9):1064-1073. 2. lena S. Koltun, Naing Aay et al. Abstract 4878: RMC-4550, an allosteric inhibitor of SHP2: Synthesis, structure, and anti-tumor activity. Experimental and Molecular Therapeutics AM2018-4878 Published July 2018

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Covalent Inhibitor Library Metabolism Compound Library Preclinical Compound Library Bioactive Compound Library Hematonosis Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max Phosphatase Inhibitor Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

RMC-4550 2172651-73-7 Metabolism Phosphatase Inhibitor inhibit RMC4550 RMC 4550 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.