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RMC-4550 is an effective and allosteric inhibitor of SHP2 (IC50: 0.583 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $56 | In Stock | |
5 mg | $122 | In Stock | |
10 mg | $198 | In Stock | |
25 mg | $455 | In Stock | |
50 mg | $672 | In Stock | |
100 mg | $956 | In Stock | |
1 mL x 10 mM (in DMSO) | $133 | In Stock |
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 |
Smiles | C[C@@H]1OCC2(CCN(CC2)c2nc(C)c(nc2CO)-c2cccc(Cl)c2Cl)[C@@H]1N |
Relative Density. | 1.39 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 260 mg/mL (571.61 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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