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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Syk-Sovleplenib
Sovleplenib

Chemical Structure : Sovleplenib

CAS No.: 1415792-84-5

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Sovleplenib (HMPL-523, HMPL523)

货号: 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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10 mg ￥2280 In stock
25 mg ￥3580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 482.603
分子式 C24H30N6O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
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

参考文献

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

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