>>Signaling Pathways>> Tyrosine Kinase>> Spleen Tyrosine Kinase (Syk)>>Sovleplenib

Sovleplenib (Synonyms: HMPL-523)

Catalog No.GC64279

Sovleplenib(HMPL-523)는 IC50이 25nM인 매우 강력하고 경구로 이용 가능한 선택적 SYK 억제제입니다. 항종양 활성. Sovleplenib은 면역 혈소판 감소증(ITP) 연구에 사용할 수 있습니다.

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Sovleplenib Chemical Structure

Cas No.: 1415792-84-5

Size 가격 재고 수량
5 mg
US$612.00
재고 있음
10 mg
US$990.00
재고 있음

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents

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].

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].

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].

[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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Average Rating: 5 ★★★★★ (Based on Reviews and 34 reference(s) in Google Scholar.)

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