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Sovleplenib (Synonyms: HMPL-523)

Katalog-Nr.GC64279

Sovleplenib (HMPL-523) ist ein hochpotenter, oral verfÜgbarer und selektiver SYK-Inhibitor mit einem IC50 von 25 nM. Anti-Tumor-AktivitÄt. Sovleplenib kann zur Erforschung der Immunthrombozytopenie (ITP) verwendet werden.

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Sovleplenib Chemische Struktur

Cas No.: 1415792-84-5

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Sample solution is provided at 25 µL, 10mM.

Description of Sovleplenib

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.

Chemical Properties of Sovleplenib

Cas No. 1415792-84-5 SDF
Überlieferungen HMPL-523
Formula C24H30N6O3S M.Wt 482.6
Löslichkeit Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Sovleplenib

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1 mg 5 mg 10 mg
1 mM 2.0721 mL 10.3605 mL 20.7211 mL
5 mM 0.4144 mL 2.0721 mL 4.1442 mL
10 mM 0.2072 mL 1.0361 mL 2.0721 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 34 reference(s) in Google Scholar.)

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