XL019 | JAK2 Inhibitor | AmBeed-信号通路专用抑制剂

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XL019 {[allProObj[0].p_purity_real_show]}

货号：A403201

XL019 is a selective and potent JAK2 inhibitor with IC50 value of 2.2 nM, with less potency to JAK1, JAK3, FLT3 and PDGFRβ with IC50 values of 134.3 nM, 214.2 nM, 139.7 nM and 125.4 nM, respectively.

XL019 化学结构
CAS号：945755-56-6

XL019 3D分子结构
CAS号：945755-56-6

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XL019 纯度/质量文件产品仅供科研

货号：A403201 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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JAK 亚型比较

产品名称	JAK1 ↓ ↑	JAK2 ↓ ↑	JAK3 ↓ ↑	Tyk2 ↓ ↑	其他靶点	纯度
Decernotinib	+++ JAK1, Ki: 11 nM JAK1, IC50: 11 nM	+++ JAK2, Ki: 13 nM	++++ JAK3, Ki: 2.5 nM	+++ TYK2, Ki: 13 nM		99%+
ZM39923 HCl	+ JAK1, pIC50: 4.4		+ JAK3, pIC50: 7.1		EGFR	97%
Cerdulatinib	+++ JAK1, IC50: 12 nM	+++ JAK2, IC50: 6 nM	+++ JAK3, IC50: 8 nM	++++ TYK2, IC50: 0.5 nM		99%+
Momelotinib	+++ JAK1, IC50: 11 nM	++ JAK2, IC50: 18 nM	+ JAK3, IC50: 155 nM			99%+
XL019	+ JAK1, IC50: 134.3 nM	++++ JAK2, IC50: 2.2 nM	+ JAK3, IC50: 214.2 nM		FLT3	99%+
Ruxolitinib	+++ JAK1, IC50: 3.3 nM	++++ JAK2, IC50: 2.8 nM				98%
Tofacitinib	+ JAK1, IC50: 112 nM	++ JAK2, IC50: 20 nM	++++ JAK3, IC50: 1 nM			98%
Ruxolitinib (S enantiomer)	+++ JAK1, IC50: 3.3 nM	++++ JAK2, IC50: 2.8 nM		++ TYK2, IC50: 19 nM		98%
Filgotinib	+++ JAK1, IC50: 10 nM	++ JAK2, IC50: 28 nM	+ JAK3, IC50: 810 nM	+ TYK2, IC50: 116 nM		99%
Baricitinib	+++ JAK1, IC50: 5.9 nM	+++ JAK2, IC50: 5.7 nM		++ TYK2, IC50: 53 nM		99%
Gandotinib	++ JAK1, IC50: 19.8 nM	++++ JAK2, IC50: 0.288 nM JAK2 (V617F), Ki: 0.245 nM	++ JAK3, IC50: 48.0 nM	++ TYK2, IC50: 44 nM	FLT3	99%+
Oclacitinib maleate	+++ JAK1, IC50: 10nM	++ JAK2, IC50: 18nM	+ JAK3, IC50: 99nM	+ TYK2, IC50: 84nM		98+%
NVP-BSK805 2HCl	++ JAK1, IC50: 31.63 nM	++++ JAK2, IC50: ~0.5 nM	++ JAK3, IC50: 18.68 nM	+++ TYK2, IC50: 10.76 nM		99+%
Peficitinib		✔				98%
Go6976		✔			FLT3	99%+
AZD-1480		++++ JAK2, IC50: 0.26 nM				99%+
Fedratinib		+++ JAK2 (V617F), IC50: 3 nM JAK2, IC50: 3 nM			FLT3,RET	99%+
WP1066		+ JAK2, IC50: 2.3 μM				98%
Curcumol		✔				98%
AZ960		++++ JAK2, Ki: 0.45 nM JAK2, IC50: <3 nM				97%
GLPG0634 analog		✔				99%+
CEP-33779		++++ JAK2, IC50: 1.8 nM				99%+
FLLL32		+ JAK2, IC50: <5 μM				99%+
WHI-P154			+ JAK3, IC50: 1.8 μM		EGFR,Src,VEGFR	98%
BMS-911543		++++ JAK2, IC50: 1.1 nM	+ JAK3, IC50: 75 nM	++ TYK2, IC50: 66 nM		98%
TG101209		+++ JAK2, IC50: 6 nM	+ JAK3, IC50: 169 nM		FLT3,RET	99%+
AT9283		++++ JAK2, IC50: 1.2 nM	++++ JAK3, IC50: 1.1 nM			99%+
Pacritinib		++ JAK2 (V617F), IC50: 19 nM JAK2, IC50: 23 nM	+ JAK3, IC50: 520 nM	++ TYK2, IC50: 50 nM	FLT3	97%
Tofacitinib citrate		++ JAK2, IC50: 20 nM	++++ JAK3, IC50: 1 nM			99%
FM-381			++++ JAK3, IC50: 127 pM			98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

XL019 生物活性

靶点	JAK1 JAK1, IC50:134.3 nM JAK3 JAK3, IC50:214.2 nM JAK2 JAK2, IC50:2.2 nM
描述	The JAK/STAT3 pathway is activated by various cancer types, including glioma, and blockade of the pathway induces cell death in cancer cells. JAK2 is a member of the Janus family of cytoplasmic tyrosine kinases, with other members being JAK1, JAK3, and TYK. The normal function of JAK2 is to transmit signals following ligand binding of type I cytokine receptors, most notably the erythropoietin (EPO) and thrombopoietin receptors (MPL), the JAK2 _V617F mutation results in loss of inhibition of its tyrosine kinase activity, and therefore its continuous activity leads to increased signaling through the JAK-signal transducer and activator of transcription (STAT) pathway^[3]. XL019 is a potent and selective JAK2 inhibitor with IC₅₀ of 2.2 nM, exhibiting >50-fold selectivity over JAK1, JAK3 and TYK2. It has been studied in a phase 1 clinical trial but was forced to terminate due to CNS side effects. KBV20C cancer cells were stimulated for 72 h with 5 nM vincristine, 5 μM XL019, 5 nM vincristine with 5 μM XL019. XL019 reduced cellular viability and increased apoptosis in vincristine-treated KBV20C cells. The result demonstrated that XL019 can sensitize drug-resistant KBV20C cancer cells to vincristine treatment by reducing the proliferation of vincristine-treated KBV20C cells. XL019 also induced early apoptosis of KBV20C cells in response to vincristine treatment via increasing G2 phase arrest. Moreover, G2 phase arrest and apoptosis of cells co-treated with vincristine and XL019 resulted from the up-regulation of phosphorylated retinoblastoma protein (pRb), p21, and the DNA-damage protein, phosphorylated H2A histone family, member X (pH2AX)^[4].
作用机制	The aniline substituted biarylpyrimidine core of XL019 can bind to the JAK2 binding site.

XL019 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00522574	Myeloproliferative Disorders ... 展开 >> Myelofibrosis Polycythemia Vera Thrombocythemia, Essential 收起 <<	Phase 1	Terminated(Due to emerging saf... 展开 >>ety data) 收起 <<	-	United States, California ... 展开 >> UCSF - Division of Hematology/Oncology San Francisco, California, United States, 94143 United States, Florida H. Lee Moffitt Cancer Center & Research Institute Tampa, Florida, United States, 33612 United States, Massachusetts Dana Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, New York Mt. Sinai School of Medicine New York, New York, United States, 10029 United States, Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT00595829	Polycythemia Vera	Phase 1	Terminated	-	United States, California ... 展开 >> UCLA School of Medicine, Center for Health Sciences Los Angeles, California, United States, 90095 UCSF - Division of Hematology/Oncology San Francisco, California, United States, 94143 United States, Florida H. Lee Moffitt Cancer Center & Research Institute Tampa, Florida, United States, 33612 United States, Michigan University of Michigan Health System Ann Arbor, Michigan, United States, 48109 United States, New York Weill Cornell Medical College New York, New York, United States, 10065 收起 <<

XL019 参考文献

[1]Forsyth T, Kearney PC, et al. SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7653-8.

[2]Verstovsek S. Therapeutic potential of JAK2 inhibitors. Hematology Am Soc Hematol Educ Program. 2009:636-42. doi: 10.1182/asheducation-2009.1.636.

[3]Tam CS, Verstovsek S. Investigational Janus kinase inhibitors. Expert Opin Investig Drugs. 2013 Jun;22(6):687-99. doi: 10.1517/13543784.2013.774373. Epub 2013 Feb 23. PMID: 23432430.

[4]Cheon JH, Kim JY, Lee BM, Kim HS, Yoon S. P-gp Inhibition by XL019, a JAK2 Inhibitor, Increases Apoptosis of Vincristine-treated Resistant KBV20C Cells with Increased p21 and pH2AX Expression. Anticancer Res. 2017 Dec;37(12):6761-6769. doi: 10.21873/anticanres.12136. PMID: 29187454.

XL019 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.25mL

0.45mL

0.22mL

11.25mL

2.25mL

1.12mL

22.50mL

4.50mL

2.25mL

XL019 技术信息

CAS号	945755-56-6
分子式	C₂₅H₂₈N₆O₂
分子量	444.529

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

溶解度

DMSO: 25 mg/mL(56.24 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

XL019 {[allProObj[0].p_purity_real_show]}

XL019 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

XL019 质控信息

XL019 生物活性

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XL019 实验方案

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JAK1	JAK1, IC50:134.3 nM
JAK3	JAK3, IC50:214.2 nM
JAK2	JAK2, IC50:2.2 nM

XL019 {[allProObj[0].p_purity_real_show]}

XL019 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

XL019 质控信息

XL019 生物活性

XL019 临床研究

XL019 参考文献

XL019 实验方案

XL019 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

细胞研究

临床研究

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XL019 纯度/质量文件产品仅供科研