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网站主页 化工产品目录 生物化工 抑制剂 酪氨酸蛋白激酶/信号转导子和转录活化子抑制剂(JAK/STAT) JAK 抑制剂 帕克替尼 化合物 Pacritinib
  • 化合物 Pacritinib|T6020

化合物 Pacritinib|T6020

Pacritinib
937272-79-2
￥396 1mg 起订
￥588 2mg 起订
￥1120 5mg 起订
上海 更新日期：2024-09-14

TargetMol中国（陶术生物）

VIP12年
联系人：邵小姐
电话：021-021-33632979拨打
手机：15002134094 拨打
邮箱：marketing@targetmol.com

产品详情:

中文名称：
化合物 Pacritinib
英文名称：
Pacritinib
CAS号：
937272-79-2
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
≥95%
产品类别：
抑制剂
货号：
T6020

Product Introduction

Bioactivity

名称Pacritinib
描述Pacritinib (SB1518) (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23/22 nM, in cell-free assays).
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)
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.
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.
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 1 mg/ml, Sonication is recommended.
关键字Janus kinase | inhibit | SB 1518 | Fms like tyrosine kinase 3 | Cluster of differentiation antigen 135 | Inhibitor | FLT3 | SB-1518 | CD135 | Pacritinib | JAK
相关产品JAK-IN-10 | Tofacitinib Citrate | Gefitinib | Gilteritinib | Sorafenib tosylate | Nintedanib | Sorafenib | Pexidartinib | Fedratinib | Ruxolitinib phosphate | Ibrutinib | Delgocitinib
相关库抑制剂库 | 经典已知活性库 | 抗癌上市药物库 | 已知活性化合物库 | 激酶抑制剂库 | 抗衰老化合物库 | FDA 上市激酶抑制剂库 | 酪氨酸激酶分子库 | 药物功能重定位化合物库 | 抗癌临床化合物库
SB1518|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (12年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

化合物 Pacritinib相关厂家报价

  • 帕克替尼
  • 帕克替尼
  • 杭州柯莱生物医药科技有限公司
  • 2024-07-03
  • 询价
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