| Identification | Back Directory | [Name]
(S)-7-(4-(1-(methylsulfonyl)piperidin-4-yl)phenyl)-N-(morpholin-2-ylmethyl)pyrido[3,4-b]pyrazin-5-amine | [CAS]
1415792-84-5 | [Synonyms]
HMPL-523
EOS-61289
(S)-7-(4-(1-(methylsulfonyl)piperidin-4-yl)phenyl)-N-(morpholin-2-ylmethyl)pyrido[3,4-b]pyrazin-5-amine
Pyrido[3,4-b]pyrazin-5-amine, 7-[4-[1-(methylsulfonyl)-4-piperidinyl]phenyl]-N-[(2S)-2-morpholinylmethyl]- | [Molecular Formula]
C24H30N6O3S | [MDL Number]
MFCD34549487 | [MOL File]
1415792-84-5.mol | [Molecular Weight]
482.6 |
| Chemical Properties | Back Directory | [Boiling point ]
701.3±70.0 °C(Predicted) | [density ]
1.37±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
8.54±0.40(Predicted) | [color ]
Light green to green |
| Hazard Information | Back Directory | [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. |
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