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PF-07284892 (ARRY-558) is an orally active allosteric SHP2 inhibitor (IC50 = 21 nM) that reduces pERK expression and may be employed in solid tumour research.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $61 | - | In Stock | |
| 5 mg | $147 | - | In Stock | |
| 10 mg | $198 | - | In Stock | |
| 25 mg | $413 | - | In Stock | |
| 50 mg | $645 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $162 | - | In Stock |
| Description | PF-07284892 (ARRY-558) is an orally active allosteric SHP2 inhibitor (IC50 = 21 nM) that reduces pERK expression and may be employed in solid tumour research. |
| Targets&IC50 | SHP2:21 nM |
| In vitro | PF-07284892 (100 nM; 4, 18 h), in combination with lorlatinib (0-450 nM) or binimetinib (0-160 nM), reduces pERK expression in H3122 lorR-06 and VACO-432 cells.[2] |
| In vivo | After oral administration of 10 mg/kg PF-07284892, the compound exhibited oral bioavailability of 85%, 94%, 102%, and 64% in mice, rats, dogs, and monkeys respectively, demonstrating favorable oral absorption. [2] |
| Synonyms | PF07284892, ARRY-558, ARRY558 |
| Molecular Weight | 439.96 |
| Formula | C21H22ClN7S |
| Cas No. | 2498597-94-5 |
| Smiles | N[C@H]1C2(CC=3C1=CC=CC3)CCN(CC2)C=4N=CC(SC=5C(Cl)=C(N)N=CC5)=NN4 |
| Color | Yellow |
| Appearance | Solid |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (181.83 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (7.5 mM), Sonication is recommeded. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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