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CAS No.: 1369761-01-2

Cerdulatinib HCl Catalog No. CSN19204

Synonyms: PRT062070 hydrochloride;PRT2070 hydrochloride;PRT062070 HCl

Cerdulatinib HCl is a dual JAK/SYK inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. It also inhibits other kinases with IC50 less than 200 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Tyk2

IC50:0.5nM JAK1

IC50:12nM Syk

IC50:32nM JAK2

IC50:6nM JAK3

IC50:8nM
描述The JAK/STAT pathway forms a critical node affecting multiple signaling pathways in both the innate and adaptive immune responses. JAK family members include Janus kinases 1, 2, and 3 (JAK1, JAK2, and JAK3, respectively) and tyrosine kinase 2 (TYK2). JAK1 and JAK2 and TYK2 are broadly activated by different cytokines across cell types, while JAK3 is limited to primarily hematopoietic cells. Cerdulatinib Hydrochloride is a hydrochloride form of Cerdulatinib. Cerdulatinib/PRT-062070 is an orally active nonspecific kinase inhibitor with an IC₅₀ of 0.5, 12, 6, or 8 nM for TYK2, JAK1, JAK2, or JAK3, respectively. At the cellular level, cerdulatinib demonstrates specificity towards JAK1/JAK3 and TYK2, but not JAK2-mediated responses and it is currently in phase 1/2A clinical trials for CLL (chronic lymphocytic leukemia) as well as other B-cell Non Hodgkin lymphomas, with first in man clinical trial data and therapeutic responses in patients resistant to ibrutinib already reported. The specificity of cerdulatinib was also demonstrated by its lack of inhibition of T cell receptor signaling or protein kinase C signaling in whole blood. On a tissue microarray of 62 primary DLBCL (large B-cell lymphoma) tumors with 58% expressed either phosphorylated SYK or STAT3 or both. Cerdulatinib induced DLBCL cells apoptosis which was associated with caspase-3 and PARP cleavage with IC₅₀ of 32 nM and 12 nM for SYK and JAK1. PBMCs from CLL patients were treated with cerdulatinib ranging from 0-1μM. Cerdulatinib induced apoptosis of CLL cells in a time- and concentration-dependent manner, and particularly in IGHV unmutated samples with greater BCR-signaling capacity and response to IL-4, which showed that Cerdulatinib is a promising therapeutic for the treatment of CLL either alone or in combination with venetoclax.
参考文献

[1] Guo A, Lu P, et al. Dual SYK/JAK inhibition overcomes ibrutinib resistance in chronic lymphocytic leukemia: Cerdulatinib, but not ibrutinib, induces apoptosis of tumor cells protected by the microenvironment. Oncotarget. 2017 Feb 21;8(8):12953-12967.
[2] Ma J, Xing W, et al. Cerdulatinib, a novel dual SYK/JAK kinase inhibitor, has broad anti-tumor activity in both ABC and GCB types of diffuse large B cell lymphoma. Oncotarget. 2015 Dec 22;6(41):43881-96.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0747 mL
- 10.3735 mL
- 20.7469 mL
- 5 mM
- 0.4149 mL
- 2.0747 mL
- 4.1494 mL
- 10 mM
- 0.2075 mL
- 1.0373 mL
- 2.0747 mL

技术信息

CAS号

1369761-01-2

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H28ClN7O3S

运输

蓝冰

分子量

482.00

别名

PRT062070 hydrochloride;PRT2070 hydrochloride;PRT062070 HCl;PRT-2070 HCl;PRT-2070;PRT-062070;Cerdulatinib

溶解度

DMSO	25.0 mg/mL (51.9 mM) warming
Water	insoluble

动物实验配方

IP	4% DMSO+water	1 mg/mL	clear
PO	0.5% CMC-Na	23 mg/mL	suspension

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靶点	Description	IC50
Tyk2		IC50:0.5nM
JAK1		IC50:12nM
Syk		IC50:32nM
JAK2		IC50:6nM
JAK3		IC50:8nM

Cerdulatinib HCl Catalog No. CSN19204

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