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Sovleplenib

Chemical Structure : Sovleplenib

CAS No.: 1415792-84-5

Sovleplenib (HMPL-523)

Catalog No.: PC-73445Not For Human Use, Lab Use Only.

Sovleplenib (HMPL-523) is a highly potent, selective, orally available SYK inhibitor with IC50 of 25 nM, demonstrates anti-tumor activity in B cell lymphomas.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Sovleplenib (HMPL-523) is a highly potent, selective, orally available SYK inhibitor with IC50 of 25 nM, demonstrates anti-tumor activity in B cell lymphomas.
HMPL-523 blocked phosphorylation of BLNK, downstream protein of Syk, in human mantle cell line REC-1 and human plasma cell line ARH-7777 with IC50 of 0.105 µM and 0.173 μM, respectively.
HMPL-523 also inhibited cell viability of Ba/F3 Tel-Syk with IC50 of 0.033 μM.
HMPL-523 potently inhibited cell viability in a panel of B -cell lymphoma cell lines with SYK/BCR deregulation with IC50 of 0.4 to 2 μM.
HMPL-523 increased the apoptotic rate of REC-1 cells, showed the synergistic activities on killing human DLBCL in combination with BTK inhibitor, PI3Kδ inhibitors and Bcl2 family inhibitor.
HMPL-523 (100 mg/kg, p.o.) showed potent anti-tumor activity in B cell lymphoma REC-1, demonstrated anti-tumor activity in Syk dependent xenograft models.

Physicochemical Properties

M.Wt 482.603
Formula C24H30N6O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-7-(4-(1-(Methylsulfonyl)piperidin-4-yl)phenyl)-N-(morpholin-2-ylmethyl)pyrido[3,4-b]pyrazin-5-amine

References

1. Na Yang, et al. Blood (2016) 128 (22): 3970.

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