1415792-84-5
1415792-84-5 structure
- Name: Sovleplenib
- Chemical Name: HMPL-523
- CAS Number: 1415792-84-5
- Molecular Formula: C24H30N6O3S
- Molecular Weight: 482.5984
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Syk
- Create Date: 2021-04-18 10:51:19
- Modify Date: 2024-01-04 10:35:12
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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].
| Name | HMPL-523 |
|---|---|
| Synonyms | (S)-7-(4-(1-(methylsulfonyl)piperidin-4-yl)phenyl)-N-(morpholin-2-ylmethyl)pyrido[3,4-b]pyrazin-5-amine |
| Description | 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]. |
|---|---|
| Related Catalog | |
| Target |
SYK[1] |
| In Vitro | Sovleplenib (HMPL-523) inhibits SYK, FLT3, KDR, LYN, FGFR2, and AUR A with IC50s of 0.025, 0.063, 0.390, 0.921, 3.214, 3.969 μM, respectively[1]. Sovleplenib (HMPL-523) blocks phosphorylation of BLNK, downstream protein of Syk, in human mantle cell line REC-1 and human plasma cell line ARH-7777 with IC50s of 0.105 µM and 0.173 μM, respectively[2]. Sovleplenib also inhibits cell viability of Ba/F3 Tel-Syk with the IC50 of 0.033 μM[2]. Sovleplenib also increases the apoptotic rate of REC-1 cells[2]. Sovleplenib shows the synergistic activities on killing human diffused large B cell lymphoma (DLBCL) in combination with other drugs such as BTK inhibitor, PI3Kδ inhibitors and Bcl2 family inhibitor[2]. |
| 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. |
| Density | 1.37±0.1 g/cm3 |
|---|---|
| Boiling Point | 701.3±70.0 °C |
| Molecular Formula | C24H30N6O3S |
| Molecular Weight | 482.5984 |