Pacritinib | SB1518 | JAK2/FLT3 Inhibitor | AmBeed-信号通路专用抑制剂

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帕克替尼（SB1518） /Pacritinib {[allProObj[0].p_purity_real_show]}

货号：A134862 同义名： SB1518

Pacritinib (SB1518) 是一种强效抑制野生型 JAK2 (IC50 = 23 nM) 和 JAK2V617F 突变体 (IC50 = 19 nM) 的抑制剂，同时也抑制 FLT3 (IC50 = 22 nM) 及其突变体 FLT3D835Y (IC50 = 6 nM)。

Pacritinib 化学结构
CAS号：937272-79-2

Pacritinib 3D分子结构
CAS号：937272-79-2

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Pacritinib 纯度/质量文件产品仅供科研

货号：A134862 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

全球学术期刊中引用的产品: • Cell, 2024, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 更多 >

JAK 亚型比较
FLT3 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。

产品名称	FLT3 ↓ ↑	其他靶点	纯度
R406	✔	Syk	98%
Go6976	✔		99%+
Quizartinib	+++ FLT3 (ITD), IC50: 1.1 nM FLT3 (WT), IC50: 4.2 nM		98%
Gilteritinib	++++ FLT3, IC50: 0.29 nM		99%+
Amuvatinib	+ FLT3 (D835Y), IC50: 81 nM		99%+
Pacritinib	++ FLT3 (D835Y), IC50: 6 nM FLT3, IC50: 22 nM		97%
Dovitinib	++++ FLT3, IC50: 1 nM	c-Kit	99%+
Denfivontinib	++++ FLT3 (D835Y), IC50: 0.4 nM FLT3, IC50: 0.4 nM	RET	99%+
TAK-659 HCl	++ FLT3, IC50: 4.6 nM	Syk	99%+
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。

Pacritinib 生物活性

靶点	JAK3 JAK3, IC50:520 nM Tyk2 TYK2, IC50:50 nM JAK2 JAK2 (V617F), IC50:19 nM JAK2, IC50:23 nM FLT3 FLT3 (D835Y), IC50:6 nM FLT3, IC50:22 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. JAKs encompass a family of four (JAK1, JAK2, JAK3 and TYK2) intracellular, non-receptor tyrosine kinases, associated with cytokine receptors. Under normal conditions, activation of the receptor by cytokine binding leads to trans-phosphorylation of JAK and downstream phosphorylation of STAT proteins (pSTAT)^[3]. JAK2 phosphorylates cell surface receptors on tyrosine residues creating docking sites for STAT3 proteins. Once STAT3 is recruited to the receptor, it is phosphorylated by JAK2 allowing STAT3 to form a dimer and move into the nucleus where it can activate the transcription of target genes^[4]. Pacritinib is a JAK2 and fms-like tyrosine kinase-3 (FLT3) inhibitor with IC₅₀ 23 nM and 22 nM. It also suppresses the interleukin-1-directed inflammatory pathway via inhibition of interleukin 1 receptor-associated kinase 1 (IRAK1)^[5]. In a phase I study, thirteen AML (acute myeloid leukemia) patients were enrolled, treated with Pacritinib at a dose of 100 mg or 200 mg twice daily following a 3 + 3 dose-escalation in combination with cytarabine and daunorubicin or with decitabine induction. The result demonstrated that pacritinib was well tolerated and had preliminary anti-leukemic activity^[6]. In a vivo study, the Stelic animal model (STAM) mouse were given 200 mg/kg Pacritinib orally for twice a day for 10 days. Pacritinib-treated mice had significantly reduced fibrotic areas in liver compared to vehicle control and significantly lower levels of CK18 which demonstrated that pacritinib possess a good antifibrotic effect^[7]. Thirty-two mice were xenografted with BT147(brain tumor initiating cells) cells, and treated with pacritinib at a dose of 100 mg/kg. Pacritinib resulted in an increase median survival of 62.5 days which demonstrated pacritinib synergy with TMZ may be another considerable choice therapy for GBM(glioblastoma multiforme)^[4].
作用机制	Pacritinib can bind with the JAK2 enzyme binding pocket.

Pacritinib 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
NCT02251821	Primary Myelofibrosis ... 展开 >> Secondary Myelofibrosis 收起 <<	Phase 2	Recruiting	-	United States, Washington ... 展开 >> Fred Hutch/University of Washington Cancer Consortium Recruiting Seattle, Washington, United States, 98109 Contact: Rachel B. Salit 206-667-1317 rsalit@fredhutch.org Principal Investigator: Rachel B. Salit 收起 <<
NCT02823171	Healthy	Phase 1	Completed	-	United States, Indiana ... 展开 >> Covance Clinical Research Unit Inc. Evansville, Indiana, United States, 47710 收起 <<
NCT02342353	Non-Small Cell Lung Cancer ... 展开 >> Nonsmall Cell Lung Cancer Carcinoma, Non-Small-Cell Lung 收起 <<	Phase 1	Terminated(Drug shortage)	-	United States, Missouri ... 展开 >> Washington University School of Medicine Saint Louis, Missouri, United States, 63110 收起 <<

Pacritinib 参考文献

[1]Beauverd Y, McLornan DP, Harrison CN. Pacritinib: a new agent for the management of myelofibrosis? Expert Opin Pharmacother. 2015;16(15):2381-90. doi: 10.1517/14656566.2015.1088831. PMID: 26389774.

[2]Jensen KV, Cseh O, Aman A, Weiss S, Luchman HA. The JAK2/STAT3 inhibitor pacritinib effectively inhibits patient-derived GBM brain tumor initiating cells in vitro and when used in combination with temozolomide increases survival in an orthotopic xenograft model. PLoS One. 2017 Dec 18;12(12):e0189670. doi: 10.1371/journal.pone.0189670. PMID: 29253028; PMCID: PMC5734728.

[3]Tremblay D, Mascarenhas J. Pacritinib to treat myelofibrosis patients with thrombocytopenia. Expert Rev Hematol. 2018 Sep;11(9):707-714. doi: 10.1080/17474086.2018.1500456. Epub 2018 Jul 19. PMID: 30001163.

[4]Jensen KV, Cseh O, Aman A, Weiss S, Luchman HA. The JAK2/STAT3 inhibitor pacritinib effectively inhibits patient-derived GBM brain tumor initiating cells in vitro and when used in combination with temozolomide increases survival in an orthotopic xenograft model. PLoS One. 2017 Dec 18;12(12):e0189670. doi: 10.1371/journal.pone.0189670. PMID: 29253028; PMCID: PMC5734728.

[5]Al-Fayoumi S, Hashiguchi T, Shirakata Y, Mascarenhas J, Singer JW. Pilot study of the antifibrotic effects of the multikinase inhibitor pacritinib in a mouse model of liver fibrosis. J Exp Pharmacol. 2018 May 9;10:9-17. doi: 10.2147/JEP.S150729. PMID: 29785143; PMCID: PMC5953271.

Pacritinib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.58mL

2.12mL

1.06mL

21.16mL

4.23mL

2.12mL

Pacritinib 技术信息

CAS号	937272-79-2
分子式	C₂₈H₃₂N₄O₃
分子量	472.579

别名	SB1518
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,2-8°C

溶解度

DMSO: 4 mg/mL(8.46 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

IP 5% DMSO+water 0.2 mg/mL clear

PO 0.5% CMC-Na 50 mg/mL suspension

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

NCT02251821	Primary Myelofibrosis ... 展开 >> Secondary Myelofibrosis 收起 <<	Phase 2	Recruiting	-	United States, Washington ... 展开 >> Fred Hutch/University of Washington Cancer Consortium Recruiting Seattle, Washington, United States, 98109 Contact: Rachel B. Salit 206-667-1317 rsalit@fredhutch.org Principal Investigator: Rachel B. Salit 收起 <<
NCT02823171	Healthy	Phase 1	Completed	-	United States, Indiana ... 展开 >> Covance Clinical Research Unit Inc. Evansville, Indiana, United States, 47710 收起 <<
NCT02342353	Non-Small Cell Lung Cancer ... 展开 >> Nonsmall Cell Lung Cancer Carcinoma, Non-Small-Cell Lung 收起 <<	Phase 1	Terminated(Drug shortage)	-	United States, Missouri ... 展开 >> Washington University School of Medicine Saint Louis, Missouri, United States, 63110 收起 <<
NCT02807207	Healthy Subjects	Phase 1	Completed	-	United States, Indiana ... 展开 >> Covance Clinical Research Unit Inc. Evansville, Indiana, United States, 47710 收起 <<
NCT02584777	Primary Myelofibrosis	Phase 2	Withdrawn	August 2020	-
NCT02808455	Healthy Subjects	Phase 1	Completed	-	United States, Florida ... 展开 >> Covance Clinical Research Unit Daytona Beach, Florida, United States, 32117 收起 <<
NCT02891603	Graft Vs Host Disease ... 展开 >> GVHD 收起 <<	Phase 1 Phase 2	Recruiting	June 2020	United States, Florida ... 展开 >> H. Lee Moffitt Cancer Center and Research Institute Recruiting Tampa, Florida, United States, 33612 Principal Investigator: Joseph Pidala, M.D. Sub-Investigator: Melissa Alsina, M.D. Sub-Investigator: Marco Davila, M.D., Ph.D. Sub-Investigator: Linda Kelley, Ph.D. Sub-Investigator: Farhad Khimani, M.D. Sub-Investigator: Frederick Locke, M.D. Sub-Investigator: Asmita Mishra, M.D. Sub-Investigator: Taiga Nishihori, M.D. Sub-Investigator: Jose Ochoa-Bayona, M.D. Sub-Investigator: Lia Perez, M.D. Sub-Investigator: Hugo Fernandez, M.D, 收起 <<
NCT02469415	Leukemia	Phase 2	Terminated(FDA Clinical Hold)	-	United States, Texas ... 展开 >> University of Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT02323607	Recurrent Adult Acute Myeloid ... 展开 >>Leukemia Secondary Acute Myeloid Leukemia Therapy-Related Acute Myeloid Leukemia Untreated Adult Acute Myeloid Leukemia 收起 <<	Phase 1	Suspended(internal data analys... 展开 >>is) 收起 <<	September 30, 2018	United States, Ohio ... 展开 >> Arthur G. James Cancer Hospital and Solove Research Institute at Ohio State University Medical Center Columbus, Ohio, United States, 43210 收起 <<
NCT02469415	-		Terminated(FDA Clinical Hold)	-	-
NCT02410551	-		Terminated	-	-
NCT02410551	Myeloproliferative Diseases	Phase 2	Terminated	-	United States, Texas ... 展开 >> University of Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT02807077	Myelofibrosis	Phase 1	Completed	-	Germany ... 展开 >> APEX GmbH Munich, Germany, D-81241 Moldova, Republic of Republican Clinical Hospital Chisinau, Moldova, Republic of, MD-2025 Romania Carol Davila Nephrology Hospital Bucharest Bucharest, Romania 收起 <<
NCT02277093	-		Terminated(FDA issued a clinic... 展开 >>al hold as pacritinib had increased side effects) 收起 <<	-	-
NCT02564536	Chronic Myelomonocytic Leukemi... 展开 >>a Juvenile Myelomonocytic Leukemia Atypical Chronic Myeloid Leukemia Myeloproliferative Neoplasm Myelodysplastic Syndromes Myelofibrosis 收起 <<	Phase 1	Withdrawn(Lack of funding foll... 展开 >>owing full FDA clinical hold) 收起 <<	June 30, 2020	-
NCT03165734	Primary Myelofibrosis ... 展开 >> Post-polycythemia Vera Myelofibrosis Post-essential Thrombocythemia Myelofibrosis 收起 <<	Phase 2	Recruiting	March 1, 2019	-
NCT03601819	Lymphoma, T-Cell, Cutaneous ... 展开 >> Lymphoma, T-Cell, Peripheral Chronic Lymphocytic Leukemia Lymphoproliferative Disorders Waldenstrom Macroglobulinemia Lymphoplasmacytic Lymphoma Mantle Cell Lymphoma 收起 <<	Phase 1	Not yet recruiting	September 2021	United States, Michigan ... 展开 >> University of Michigan Rogel Cancer Center Ann Arbor, Michigan, United States, 48109 收起 <<
NCT01773187	Primary Myelofibrosis ... 展开 >> Post-polycythemia Vera Myelofibrosis Post-essential Thrombocythemia Myelofibrosis 收起 <<	Phase 3	Terminated	-	-
NCT02807051	Drug Interaction Study	Phase 1	Completed	-	United States, Florida ... 展开 >> Covance Clinical Research Unit Daytona Beach, Florida, United States, 32117 收起 <<
NCT02055781	Primary Myelofibrosis ... 展开 >> Post-polycythemia Vera Myelofibrosis Post-essential Thrombocythemia Myelofibrosis 收起 <<	Phase 3	Terminated	-	-
NCT02277093	Colorectal Cancer	Phase 2	Terminated(FDA issued a clinic... 展开 >>al hold as pacritinib had increased side effects) 收起 <<	-	United States, Missouri ... 展开 >> Washington University School of Medicine Saint Louis, Missouri, United States, 63110 收起 <<
NCT02807116	Healthy Subjects	Phase 1	Completed	-	United States, Florida ... 展开 >> Covance Clinical Research Unit Daytona Beach, Florida, United States, 32117 收起 <<
NCT02677948	Chronic Lymphocytic Leukemia ... 展开 >> Lymphoma, Small Lymphocytic 收起 <<	Phase 1 Phase 2	Withdrawn(FDA has placed all t... 展开 >>rials involving Pacritinib on Full Clinical Hold) 收起 <<	October 2018	United States, Michigan ... 展开 >> University of Michigan Comprehensive Cancer Center Ann Arbor, Michigan, United States, 48109 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 收起 <<
NCT02532010	Acute Myeloid Leukemia (AML)	Phase 2	Terminated(The study was put o... 展开 >>n clinical hold by the sponsor since Feb 9th 2016, and was later decided not to re-open due to financial constraints.) 收起 <<	-	United States, New York ... 展开 >> Weill Cornell Medical College New York, New York, United States, 10021 收起 <<
NCT03645824	Myelofibrosis	Phase 2	Recruiting	March 2023	Belgium ... 展开 >> ZNA Recruiting Antwerpen, Belgium Contact: Breems UZ Gent Recruiting Gent, Belgium Contact: Mazure UZ Leuven Recruiting Leuven, Belgium Contact: DeVos AZ Delta Recruiting Roeselare, Belgium Contact: DeLeu Netherlands AMC Not yet recruiting Amsterdam, Noord-Holland, Netherlands Contact: Zeerleder Erasmus Medical Center Recruiting Rotterdam, Zuid-Holland, Netherlands, 3000 CA Contact: Peter AW te Boekhorst, MD Principal Investigator: Peter AW te Boekhorst, MD VUMC Recruiting Amsterdam, Netherlands Contact: Meijer MUMC Recruiting Maastricht, Netherlands Contact: Schouten UMC Radboud Recruiting Nijmegen, Netherlands Contact: Schaap 收起 <<
NCT02765724	Myelofibrosis	Phase 1	Completed	-	Germany ... 展开 >> APEX GmbH Munich, Germany, D-81241 Moldova, Republic of Republican Clinical Hospital Chisinau, Moldova, Republic of, MD-2025 收起 <<
NCT02532010	-		Terminated(The study was put o... 展开 >>n clinical hold by the sponsor since Feb 9th 2016, and was later decided not to re-open due to financial constraints.) 收起 <<	-	-
NCT02803762	Healthy	Phase 1	Completed	-	Netherlands ... 展开 >> QPS Netherlands B.V. Groningen, Netherlands, 9713 GZ 收起 <<

帕克替尼（SB1518） /Pacritinib {[allProObj[0].p_purity_real_show]}

Pacritinib 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Pacritinib 质控信息

Pacritinib 生物活性

Pacritinib 临床研究

Pacritinib 参考文献

Pacritinib 实验方案

Pacritinib 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

热门区域

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JAK3	JAK3, IC50:520 nM
Tyk2	TYK2, IC50:50 nM
JAK2	JAK2 (V617F), IC50:19 nM JAK2, IC50:23 nM
FLT3	FLT3 (D835Y), IC50:6 nM FLT3, IC50:22 nM

帕克替尼（SB1518） /Pacritinib {[allProObj[0].p_purity_real_show]}

Pacritinib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Pacritinib 质控信息

Pacritinib 生物活性

Pacritinib 临床研究

Pacritinib 参考文献

Pacritinib 实验方案

Pacritinib 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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热门区域

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Pacritinib 纯度/质量文件产品仅供科研