| Identification | Back Directory | [Name]
4-Piperidinamine, 1-[3-(2,3-dichlorophenyl)-1H-pyrazolo[3,4-b]pyrazin-6-yl]-4-methyl- | [CAS]
2160546-07-4 | [Synonyms]
IACS13909
LACS-13909
4-Piperidinamine, 1-[3-(2,3-dichlorophenyl)-1H-pyrazolo[3,4-b]pyrazin-6-yl]-4-methyl- | [Molecular Formula]
C17H18Cl2N6 | [MDL Number]
MFCD32899276 | [MOL File]
2160546-07-4.mol | [Molecular Weight]
377.27 |
| Chemical Properties | Back Directory | [Boiling point ]
577.3±50.0 °C(Predicted) | [density ]
1.402±0.06 g/cm3(Predicted) | [solubility ]
DMSO: Sparingly Soluble: 1-10 mg/ml
Ethanol: Sparingly Soluble: 1-10 mg/ml | [form ]
Solid | [pka]
8.00±0.50(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers[1]. | [in vivo]
IACS-13909 (70 mg/kg; oral administration; daily; for 21 days) treatment potently suppresses tumor growth in mice, with 100% tumor growth inhibition (TGI) observed following 21 days of dosing[1]. | Animal Model: | NSG mice (20-28 g) injected with KYSE-520 cells[1] | | Dosage: | 70 mg/kg | | Administration: | Oral administration; daily; for 21 days | | Result: | Potently suppressed tumor growth in mice. |
| [References]
[1] Yuting Sun, et al. Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR-Independent Resistance Mechanisms toward Osimertinib. Cancer Res. 2020 Nov 1;80(21):4840-4853. DOI:10.1158/0008-5472.CAN-20-1634 |
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