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Pacritinib

产品编号 T6020 CAS 937272-79-2

别名: SB1518

Pacritinib (SB1518) 是一种野生型 JAK2和 JAK2V617F 突变型抑制剂，IC50分别为 23 和 19 nM。它也抑制 FLT3及其突变型 FLT3D835Y，IC50分别为 22 和 6 nM。

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Pacritinib, CAS 937272-79-2

规格	价格/CNY	货期
1 mg	￥ 396	现货
2 mg	￥ 588	现货
5 mg	￥ 1,120	现货
10 mg	￥ 1,970	现货
25 mg	￥ 3,760	现货
50 mg	￥ 5,390	现货
100 mg	￥ 7,580	现货
500 mg	￥ 15,200	现货
1 mL * 10 mM (in DMSO)	￥ 1,160	现货

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其他形式的 Pacritinib:

Pacritinib hydrochloride
询价

选择批次

纯度: 99.52%

纯度: 99.27%

纯度: 98%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Pacritinib (SB1518) (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23/22 nM, in cell-free assays).
靶点活性	JAK3:520 nM
体外活性	Pacritinib is an effective inhibitor of both wild-type JAK2 and JAK2V617F mutant (IC50: 19 nM). The IC50s of Pacritinib are 50 nM for TYK2, 520 nM for JAK3 and 1280 nM for JAK1. Pacritinib effectively permeates cells to modulate signaling pathways downstream of JAK2, whether agonist activated or mutationally activated. Pacritinib induces apoptosis, cell cycle arrest and antiproliferative effects in JAK2WT- and JAK2V617F-dependent cells. Pacritinib inhibits cell proliferation of Karpas 1106P (IC50: 348 nM ) and Ba/F3-JAK2V617F (IC50: 160 nM ), respectively. Pacritinib inhibits endogenous colony growth derived from erythroid (IC50: 63 nM) and myeloid progenitors(IC50: 53 nM), respectively.[1] SB1518 also inhibits FLT3 and its mutant FLT3-D835Y (IC50: 6 nM ). Pacritinib inhibits FLT3 phosphorylation and downstream STAT, MAPK and PI3K signaling in FLT3-internal-tandem duplication (ITD), FLT3-wt cells and primary AML blast cells. Pacritinib treatment leads to a dose-dependent decrease of pFLT3, pSTAT5, pERK1/2 and pAkt in FLT3-ITD harboring MV4-11 cells with IC50 of 80, 40, 33 and 29 nM , respectively. Treatment of the primary AML blast cells with Pacritinib for 3 h leads to a dose-dependent decrease of pFLT3, pSTAT3 and pSTAT5 with an IC50 below 0.5 μM. Pacritinib induces apoptosis, cell cycle arrest and anti-proliferative effects in FLT3-mutant and FLT3-wt cells. Pacritinib inhibits cell proliferation of FLT3-ITD-harboring cells MV4-11 (IC50: 47 nM ) and primary AML blast (IC50: 0.19-1.3 nM ) cells.
体内活性	In JAK2V617F-dependent xenograft model, Pacritinib (150 mg/kg, p.o., q.d.) markedly ameliorates splenomegaly and hepatomegaly symptoms, with 60% normalization of spleen weight and 92% normalization of liver weight and is well tolerated without significant weight loss or any hematological toxicities, including thrombocytopenia and anemia. In JAK2V617F-dependent SET-2 xenograft model, Pacritinib dose-dependent inhibits tumor growth (40% for 75 mg/kg and 61% for 150 mg/kg).[1] Pacritinib treated once daily for 21 consecutive days, induces dose-dependent inhibition of tumor growth (38% for 25 mg/kg, 92% for 50 mg/kg and 121% for 100 mg/kg). Complete regression is observed in 3/10 and 8/8 mice for the 50 and 100 mg/kg/day groups, respectively.
激酶实验	kinase activity assays: All assays are carried out in 384-well white microtiter plates. Compounds are 4-fold serially diluted in 8 steps, starting from 10 μM. The reaction mixture consisted of 25 μL assay buffer (50 mM HEPES pH 7.5, 10 mM MgCl2, 5 mM MnCl2, 1 mM DTT, 0.1 mM Na3VO4, 5 mM β-glycerol phosphate). For FLT3 assays, the reaction contains 2.0 μg/mL FLT3 enzyme, 5 μM of poly(Glu,Tyr) substrate and 4 μM of ATP. For JAK1 assays, the reaction contains 2.5 μg/mL of JAK1 enzyme, 10 μM of poly(Glu,Ala,Tyr) substrate and 1.0 μM of ATP. For JAK2 assays, the reaction contained 0.35 μg/mL of JAK2 enzyme, 10 μM of poly (Glu,Ala,Tyr) substrate and 0.15 μM of ATP. For JAK3 assays, the reaction contained 3.5 μg/mL of JAK3 enzyme, 10 μM of poly (Glu,Ala,Tyr) substrate and 6.0 μM of ATP. For TYK2 assays, the reaction contained 2.5 μg/mL of TYK2 enzyme, 10 μM of poly (Glu,Ala,Tyr) substrate and 0.15 μM of ATP. The reaction is incubated at room temperature for 2 h prior to addition of 13 μL PKLight? detection reagent. After 10 min incubation luminescent signals are read on a multi-label plate reader.
细胞实验	Cells are seeded at 30-50% confluency in 96-well plates and are treated with different concentrations of compounds (in triplicate) for 48 h. Cell viability is monitored using the CellTiter-Glo assay.(Only for Reference)

别名	SB1518
分子量	472.58
分子式	C28H32N4O3
CAS No.	937272-79-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 11 mg/mL (23.27 mM), Heating is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.116 mL	10.5802 mL	21.1604 mL	52.9011 mL
	5 mM	0.4232 mL	2.116 mL	4.2321 mL	10.5802 mL
	10 mM	0.2116 mL	1.058 mL	2.116 mL	5.2901 mL
	20 mM	0.1058 mL	0.529 mL	1.058 mL	2.6451 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Hart S, et al. Leukemia, 2011, 25(11), 1751-1759. 2. Hart S, et al. Blood Cancer J, 2011, 1(11), e44.

文献引用

1. Chen K Y, Krischuns T, Varga L O, et al. A highly sensitive cell-based luciferase assay for high-throughput automated screening of SARS-CoV-2 nsp5/3CLpro inhibitors. Antiviral Research. 2021

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Pacritinib 937272-79-2 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors Tyrosine Kinases FLT JAK Janus kinase inhibit SB 1518 Fms like tyrosine kinase 3 SB1518 Cluster of differentiation antigen 135 Inhibitor FLT3 SB-1518 CD135 inhibitor

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Pacritinib

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords