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Plerixafor/普乐沙福 {[allProObj[0].p_purity_real_show]}

货号:A195007 同义名: AMD 3100; JM3100

Plerixafor是一种 CXCR4 受体拮抗剂,能够抑制 CXCL12 介导的趋化作用,IC50 分别为 44 nM 和 5.7 nM。

Plerixafor/普乐沙福 化学结构 CAS号:110078-46-1
Plerixafor/普乐沙福 化学结构
CAS号:110078-46-1
Plerixafor/普乐沙福 3D分子结构
CAS号:110078-46-1
Plerixafor/普乐沙福 化学结构 CAS号:110078-46-1
Plerixafor/普乐沙福 3D分子结构 CAS号:110078-46-1
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Plerixafor/普乐沙福 纯度/质量文件 产品仅供科研

货号:A195007 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 CXCR1 CXCR2 CXCR4 其他靶点 纯度
Reparixin 99%+
SB225002 +++

CXCR2, IC50: 22 nM

99%+
Plerixafor ++

CXCR4, IC50: 44 nM

99%
AMD 3465 6HBr 98%
WZ811 ++++

CXCR4, EC50: 0.3 nM

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。

Plerixafor/普乐沙福 生物活性

靶点
  • CXCR4

    CXCR4, IC50:44 nM

描述 Through binding with CC- and CXC-chemokines, CCR and CXCR, the subsets of the chemokine receptor family can trigger an intracellular signal transduction cascade, thus mediating the recruitment of immune cells to the in£ammation or infection sites and implicated in several immuno-related disease states, organogenesis, angiogenesis and tumor growth and metastasis. AMD3100 is a selective antagonist of CXCR4 with IC50 values ranging in 0.01-0.13μg/ml for antagonizing SDF-1, but not itself, activated calcium flux in different cells tested, including CXCR4-transfected U87 and CD4 cells, freshly isolated PBMCs, SupT1, THP-1, HSB-2, Molt-4 and L1210 cells. The inhibitory effect of AMD3100 against the induced endocytosis of CXCR4 is selectively SDF-1-dependent but not phorbol ester. Pre-incubated with AMD3100 at concentration of 0.04, 0.2, 1, 5 and 25μg/ml could dose-dependently inhibit the SDF-1-induced (200 ng/ml) chemotaxis of human PBMCs[1]. In vivo study showed that intraperitoneal injection with 5mg/kg AMD3100 can alter the potential of mesenchymal stem cells mobilization induced by different growth factors, including IGF-1, SCF, PDGF and VEGF, in mice, which may be mediated through Akt/PI3K, MEK1/2-Erk1/2 and smad2/3 as key signaling pathways[2].
作用机制 Not found

Plerixafor/普乐沙福 细胞实验

Cell Line
Concentration Treated Time Description References
KU812F cells 50 μM 3 h Reduced adhesion of CML cells to BM microenvironment components Leukemia. 2012 May;26(5):985-90.
KU812F cells 50 μM 3 h Reduced drug resistance of CML cells to nilotinib Leukemia. 2012 May;26(5):985-90.
EJ cells 50 μM 24 h Inhibited the proliferation and migration capacity of EJ cells by blocking CXCR4 downstream signaling Sci Adv. 2023 Mar;9(9):eabq8225.
MDA-MB-231 cells 10 μg/mL 1 h To study the uptake of Plerixafor-modified nanocarriers in CXCR4-expressing MDA-MB-231 cells, results showed that Plerixafor-modified nanocarriers had a higher uptake rate in CXCR4-expressing cells compared to unmodified carriers. Biomacromolecules. 2015 Aug 10;16(8):2412-7.

Plerixafor/普乐沙福 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Radiation-induced wound healing deficit model Subcutaneous injection 5 mg/kg Single injection Plerixafor combined with G-CSF enhanced the efficacy of MSC-FMB in correcting radiation-induced wound healing deficits J Invest Dermatol. 2013 Feb;133(2):553-61
Mice Spinal cord injury model Subcutaneous injection 5 mg/kg Once daily for 3 days Plerixafor treatment increased the number of HSPCs released into the blood by more than 6-fold, with a corresponding increase in the number of HSPCs found in the spleen, and reversed the post-SCI leukopenia. Nat Commun. 2020 Jul 24;11(1):3702
Mice BCR-ABL-positive leukemia mouse model Subcutaneous injection 5 mg/kg Once daily for 10 days Reduced leukemia burden and prolonged survival Leukemia. 2012 May;26(5):985-90.
Nude mice EJ xenograft model Intravenous injection 100 μM, 100 μl Once every 2 days for a total of five times Plerixafor significantly inhibited tumor growth, with a mean tumor volume of 647±147 mm3, compared to 1086±257 mm3 in the saline group Sci Adv. 2023 Mar;9(9):eabq8225.
Rhesus macaque Rhesus gene therapy model Intravenous injection 1 mg/kg Single dose, after 5 days of G-CSF administration Mobilization of CD34+ cells for gene therapy model Nat Commun. 2023 Oct 12;14(1):6291

Plerixafor/普乐沙福 动物研究

Dose Mice[3]: 0.625 mg/kg - 10 mg/kg (s.c.) Rat[3]: 25 mg/kg (s.c.), 2 mg/kg (i.v.)
Administration s.c., i.v.
Pharmacokinetics
Animal Rats[3]
Dose 1 mg/kg
Administration s.c.
T1/2 0.1 h (absorption)
Tmax 0.5 h
AUC0-7 5410 pmol·h/ml
Cmax 3082 pmol/ml
t1/2λ1 0.9 h
AUC 5444 pmol·h/ml

Plerixafor/普乐沙福 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
NCT01164475 - Completed - -
NCT01711073 End Stage Liver DIsease Phase 1 Unknown September 2013 United States, New Jersey ... 展开 >> University of Medicine and Dentistry of New Jersey Recruiting Newark, New Jersey, United States, 07101 Contact: Baburao Koneru, MD       koneruba@umdnj.edu 收起 <<
NCT01123499 - Recruiting - United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Recruiting Bethesda, Maryland, United States, 20892 Contact: Sandra Maxwell, B.S.N.    301-402-1773    maxwells@niaid.nih.gov 收起 <<

Plerixafor/普乐沙福 参考文献

[1]Plerixafor

Plerixafor/普乐沙福 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.99mL

0.40mL

0.20mL

9.94mL

1.99mL

0.99mL

19.89mL

3.98mL

1.99mL

Plerixafor/普乐沙福 技术信息

CAS号110078-46-1
分子式C28H54N8
分子量 502.78
SMILES Code N1(CC2=CC=C(CN3CCNCCCNCCNCCC3)C=C2)CCNCCCNCCNCCC1
MDL No. MFCD05662218
别名 AMD 3100; JM3100; JKL 169; Mozobil; SDZ SID 791; SID791
运输蓝冰
InChI Key YIQPUIGJQJDJOS-UHFFFAOYSA-N
Pubchem ID 65015
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

DMSO: 1.5 mg/mL(2.98 mM),配合低频超声,水浴加热至45℃,并调节pH至5,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

无水乙醇: 45 mg/mL(89.5 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
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