Sovleplenib(HMPL-523) is a potent and selective SYK inhibitor with an IC50 of 0.025 μM and exhibits anti-tumor activity both in vitro and in vivo. Sovleplenib, in combination with BTK, PI3Kδ, and Bcl2 family inhibitors, results in synergistic killing of human diffuse large B-cell lymphoma (DLBCL).

 

Brand: BCM

 

Target: Syk

 

Signaling Pathways: Angiogenesis; Tyrosine Kinase/Adaptors

 

In Vitro: Sovleplenib (HMPL-523) exhibits inhibitory activity with IC50 values of 0.025 μM, 0.063 μM, 0.390 μM, 0.921 μM, 3.214 μM, and 3.969 μM against SYK, FLT3, KDR, LYN, FGFR2, and AUR A, respectively. Sovleplenib effectively blocks the phosphorylation of BLNK, a downstream protein of Syk, in human mantle cell line REC-1 and human plasma cell line ARH-7777, with IC50 values of 0.105 μM and 0.173 μM, respectively. Sovleplenib also significantly reduces cell viability in Ba/F3 Tel-Syk cells with an IC50 of 0.033 μM and increases the rate of apoptosis in REC-1 cells. Sovleplenib demonstrates synergistic effects in combination with other drugs, including BTK inhibitors, PI3Kδ inhibitors, and Bcl2 family inhibitors, in killing human-diffuse large B cell lymphoma (DLBCL).

 

Boiling Point: 701.3±70.0 °C(Predicted)

 

pKa: 8.54±0.40(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; Insoluble in Ethanol.

 

Isomeric SMILES: CS(=O)(=O)N1CCC(CC1)C2=CC=C(C=C2)C3=CC4=NC=CN=C4C(=N3)NC[C@@H]5CNCCO5  

 

InChIKey: NJIAKNWTIVDSDA-FQEVSTJZSA-N  

 

InChI: InChI=1S/C24H30N6O3S/c1-34(31,32)30-11-6-18(7-12-30)17-2-4-19(5-3-17)21-14-22-23(27-9-8-26-22)24(29-21)28-16-20-15-25-10-13-33-20/h2-5,8-9,14,18,20,25H,6-7,10-13,15-16H2,1H3,(H,28,29)/t20-/m0/s1

 

Attribute
[Chem Name]	7-[4-(1-methylsulfonylpiperidin-4-yl)phenyl]-N-[[(2S)-morpholin-2-yl]methyl]pyrido[3,4-b]pyrazin-5-amine
[Synonym]	Sovleplenib; HMPL-523
[CAS No.]	1415792-84-5
[MDL No.]	MFCD34549487
[Formula]	C24H30N6O3S
[Molecular]	482.6
[Form]	Solid Powder
[Storage]	Keep in dark place. Inert atmosphere. Store in freezer, under -20°C

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