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| | (S)-7-(4-(1-(methylsulfonyl)piperidin-4-yl)phenyl)-N-(morpholin-2-ylmethyl)pyrido[3,4-b]pyrazin-5-amine Basic information |
| | (S)-7-(4-(1-(methylsulfonyl)piperidin-4-yl)phenyl)-N-(morpholin-2-ylmethyl)pyrido[3,4-b]pyrazin-5-amine Chemical Properties |
| Boiling point | 701.3±70.0 °C(Predicted) | | density | 1.37±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | pka | 8.54±0.40(Predicted) | | form | Solid | | color | Light green to green | | InChIKey | NJIAKNWTIVDSDA-FQEVSTJZSA-N | | SMILES | C12=C(NC[C@H]3OCCNC3)N=C(C3=CC=C(C4CCN(S(C)(=O)=O)CC4)C=C3)C=C1N=CC=N2 |
| | (S)-7-(4-(1-(methylsulfonyl)piperidin-4-yl)phenyl)-N-(morpholin-2-ylmethyl)pyrido[3,4-b]pyrazin-5-amine Usage And Synthesis |
| Uses | Sovleplenib (HMPL-523) is a highly potent, orally available and selective SYK inhibitor with an IC50 of 25 nM. Anti-tumor activity. Sovleplenib can be used for the research of immune thrombocytopenia (ITP)[1]. | | in vivo | Sovleplenib (HMPL-523) shows anti-tumor activity in vivo. Sovleplenib (100 mg/kg) inhibits tumor growth in REC-1 subcutaneous xenograft model[1].
Sovleplenib (HMPL-523; 100 mg/kg; daily oral administration) shows potent anti-tumor activity in B cell lymphoma REC-1 (TGI: 59%) in Syk dependent xenograft models [2]. | Animal Model: | Balb/c nude mice bearing subcutaneously implanted REC-1 cells or intravenously injected BA/F3 cells or BA/F3 TEL-SYK cells[1] | | Dosage: | 10 and 100 mg/kg | | Administration: | q.d.; for 8 days | | Result: | Inhibited tumor growth in REC-1 subcutaneous xenograft model at 100 mg/kg. |
| | References | [1] Su WG, et al. Preparation of pyridopyrazine derivatives for use as Syk inhibitors. WO2012167733 A1. [2] Na Yang, et al. HMPL-523, a Novel SYK Inhibitor Showed Anti-Tumor Activities In Vitro and In Vivo. Blood (2016) 128 (22): 3970. |
| | (S)-7-(4-(1-(methylsulfonyl)piperidin-4-yl)phenyl)-N-(morpholin-2-ylmethyl)pyrido[3,4-b]pyrazin-5-amine Preparation Products And Raw materials |
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