Plerixafor 8HCl (AMD3100 8HCl)

製品コードS3013 別名:JM 3100 8HCl

Plerixafor 8HCl (AMD3100 8HCl)化学構造

分子量(MW):794.47

Plerixafor 8HCl (AMD3100 8HCl) is the hydrochloride of Plerixafor, a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively.

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バルク問合せ

カスタマーフィードバック(4)

  • BLI of NSG mice engrafted with BV173, treated with no therapy (control), plerixafor: 1 mg/kg IP daily, ESKM 100 ug twice weekly, and a combination of ESKM and plerixafor. (A) Logarithmic plot of BLI of leukemia growth measured weekly. Error bars are 5-95% confidence intervals. There was a small but not significant difference between ESKM and combination treated group. (B) End of therapy (day 34) BLI.

    Blood 2014 123(21), 3296-304. Plerixafor 8HCl (AMD3100 8HCl) purchased from Selleck.

    Chemotaxis (Transwell invasion) assay showing the migration of BMSCs in response to CXCL12 (0–100 ng/ml) and the inhibitory effect of the CXCR4 antagonist AMD3100 (5 mg/ml, 30 min). *P < 0.05, compared with the control group (no treatment); #P < 0.05; n = 4 wells from separate cultures.

    J Clin Invest, 2015, 125(8): 3226-40. Plerixafor 8HCl (AMD3100 8HCl) purchased from Selleck.

  • Inhibition of SDF-1α signalling in subchondral bone attenuated cartilage degeneration (A) H&E staining of tibia subchondral bone and cartilage from sham, ACLT/PBS, and ACLT/AMD3100 groups. Calibration scale: bar = 100 μm; (B) Safranin O-Fast Green staining of articular cartilage in sagittal sections of tibia from mice treated with PBS or AMD3100 and sacrificed 30 days post ACLT or sham surgery. Calibration scale: bar = 100 μm; (C) MMP13 expression was detected by immunohistochemical staining of cartilage, and representative images are shown. A positive signal was indicated by the brown colour and marked by black arrows, meanwhile a negative control was present. Calibration scale: bar = 50 μm; (D) OARSI scores of sham or ACLT mice treated with PBS or AMD3100.Quantitative analysis of the percentage of MMP13+ chondrocytes in articular cartilage tissue sections in each group, reported as means ± SD. n = 10. * ACLT/PBS different from sham/PBS (p < 0.05), # ACLT/PBS different from ACLT/AMD3100 (p < 0.05).

    Int J Mol Sci, 2016, 17(6): 943.. Plerixafor 8HCl (AMD3100 8HCl) purchased from Selleck.

    CXCR4 is overexpressed in primary osteosarcoma cells and promotes invasion in U2OS cells. (A) We obtained primary cells derived from three patients suffering from osteosarcoma. The splitting of tumor tissues were performed by western blot analysis. The expression of CXCR4 in primary osteosarcoma cells were detected. OS1, OS2, OS3, three primary osteosarcoma cells. (B) Suppression of CXCR4 by plerixafor (CXCR4 inhibitor, 500 ng/ml, 48 h) downregulates the expression of MMP-2 and MMP-9. The downregulation can be reversed by SDF-1 (100 ng/ml, pre-incubate for 2 h). Sinomenine treatment had similar effect to plerixafor. The bands were quantitative analyzed by ImageJ software. *P<0.05, versus control. NS, no significance. #P<0.05 compare with plerixafor treatment. (C) Cells were treated with plerixafor and sinomenine, with or without SDF-1 simultaneously for 24 h. Then cells were harvested for Transwell assay. Representative images are presented. (x200 magnification).

    Int J Oncol, 2016, 48(5):2098-112.. Plerixafor 8HCl (AMD3100 8HCl) purchased from Selleck.

製品安全説明書

CXCR阻害剤の選択性比較

生物活性

製品説明 Plerixafor 8HCl (AMD3100 8HCl) is the hydrochloride of Plerixafor, a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively.
ターゲット
CXCL12 [1]
(Cell-free assay)
CXCR4 [1]
(Cell-free assay)
5.7 nM 44 nM
体外試験

Plerixafor inhibits CXCL12-mediated chemotaxis with a potency lightly better than its affinity for CXCR4. [1] Plerixafor also antagonizes SDF-1/CXCL12 ligand binding with an IC50 of 651 nM. Plerixafor inhibits SDF-1 mediated GTP-binding, SDF-1 mediated calcium flux and SDF-1 stimulated chemotaxis with IC50 of 27 nM, 572 nM and 51 nM, respectively. Plerixafor does not inhibit calcium flux against cells expressing CXCR3, CCR1, CCR2b, CCR4, CCR5 or CCR7 when stimulated with their cognate ligands, nor does Plerixafor inhibit receptor binding of LTB4. Plerixafor does not, on its own, induce a calcium flux in the CCRF–CEM cells, which express multiple GPCRs including CXCR4, CCR4 and CCR7. [2]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHOK1 cells M4C4WmZ2dmO2aX;uJIF{e2G7 NWnKepZOTGm|cHzhZ4Vu\W62IH;mJHsyOjWLXWPESlFidHCqYTDmdo9uKEO[Q2K0JIV5eHKnc4Pl[EBqdiCFSF;LNUBk\WyuczygTWM2OD1yLkixJI5O NVX1UVZiOTd5MUWxNlg>
GHOST CXCR4 cell line MoDVSpVv[3Srb36gZZN{[Xl? MnTLTY5pcWKrdH;yfUBkd26lZX70doF1cW:wIH;mJINwdXCxdX7kJIFo[Wmwc4SgTGlXNTFiTFHJJJN1emGrbjDpckBIUE:VVDDDXGNTPCClZXzsJIxqdmVuIFnDOVA:OC57NTDuUS=> NVHGU5V{OTR4OUixPFk>
HEK293 cells Mnq5SpVv[3Srb36gZZN{[Xl? NHWyTnYzKGSjeYO= NFzvfVZCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBVOjBvcnXzbZN1[W62IFjJWlEhVkx2LUOgbY5n\WO2ZXSgbY4hUEWNMkmzJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZidnnyZYwhemWybHnjZZRqd25iYX\0[ZIhOiCmYYnzMEBKSzVyPUKuN{BvVQ>? NGm5Z2QyQTR3MUOwOS=>
PBMC cells NWX5NJpPTnWwY4Tpc44h[XO|YYm= NFHSbZdG\m[nY4TpeoUh[2:wY3XueJJifGmxbjDv[kBkd22yb4Xu[EBi\2GrboP0JGhKXi1zIEi5MlYhe3S{YXnuJIlvKFCETVOgZ4VtdHNuIFXDOVA:Oy56IH7N MUKxOFY6QDF6OR?=
human MT4 cells NHjv[5dHfW6ldHnvckBie3OjeR?= MW[0JIRigXN? Mmj1RY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOSB|QjDpcoZm[3SnZDDpckBpfW2jbjDNWFQh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjD2bZJ2eyC{ZYDsbYNifGmxbjDh[pRmeiB2IHThfZMh[nliTWTUJIF{e2G7LDDFR|UxRTRibl2= MUCyNFA1OzZ|OB?=
human Jurkat cells NFHzZXFHfW6ldHnvckBie3OjeR?= NFPpNIxCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IFPYR3I1KGmwIHj1cYFvKEq3cnvheEBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGPESlEucW6mdXPl[EBk\WyuIH3p[5JifGmxbjygTWM2OD1{Nz60JI5O M2DHRVE6OTh6MEex
MT-4 cells M{H6TGZ2dmO2aX;uJIF{e2G7 M13RZWVn\mWldHn2[UBkd26lZX70doF1cW:wIH;mJINwdXCxdX7kJIFo[Wmwc4SgTGlXNTFiSVnJRkB{fHKjaX6gbY4hVVRvNDDj[YxteyxiRVO1NF03PSCwTR?= MnvnNVQ3QThzOEm=
rat IR983F cells MkD0SpVv[3Srb36gZZN{[Xl? NF\MPY1FcXOybHHj[Y1mdnRib3[gX|EzPUmfQ2jDUFEzKG[{b32gR3hEWjRiaX6gdoF1KEmUOUizSkBk\WyuczygTWM2OD1zMEigcm0> NW\QToRrOTlyNUO3Olg>
CEM-SS cells M2noOmZ2dmO2aX;uJIF{e2G7 M3HUZWVn\mWldHn2[UBkd26lZX70doF1cW:wIH;mJINwdXCxdX7kJIFo[Wmwc4SgTGlXNTFiTFHJJJN1emGrbjDpckBETU1vU2OgZ4VtdHNuIFXDOVA:OTJ5IH7N MV[xOFY6QDF6OR?=
human HL60 cells MnPMSpVv[3Srb36gZZN{[Xl? NIDVZ4hFcXOybHHj[Y1mdnRib3[gX|EzPUmfU1TGNYFteGijIH\yc40hS1iFUkSgbY4hcHWvYX6gTGw3OCClZXzsd{whUUN3ME2xOU4zKM7:TR?= M1:4R|E6OTh6MEex
human MOLT4 cells MoTWSpVv[3Srb36gZZN{[Xl? M2HrfVExODBibl2= NGj6RZpKdmirYnn0bY9vKG:oIF3hZkAyOkd3IHLpcoRqdmdidH:gR3hEWjRiZYjwdoV{e2WmIHnuJIh2dWGwIF3PUHQ1KGOnbHzzJIF1KDFyMECgcm0h[nliRlHDV{BidmGueYPpdy=> NIPFO2EyQTR3MUOwOS=>
human MT2 cells NHTPVIhHfW6ldHnvckBie3OjeR?= MmXrNUB2\y:vTB?= NHSzSnA1KGSjeYO= NUHHPIQ4SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMTCzRkBqdm[nY4Tl[EBqdiCqdX3hckBOXDJiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB3cXKjbDDwNlQh[W62aXflckBxem:mdXP0bY9vKGG2IEGgeYcwdUxiYX\0[ZIhPCCmYYnzJIJ6KEWOSWPB NGTrVXkzOTF4OEOzOi=>
human U87 cells NFjkOFBHfW6ldHnvckBie3OjeR?= MWqxNFAxKG6P MkHURY51[WexbnnzeEBi[3Srdnn0fUBifCCFWFPSOEBqdiCqdX3hckBWQDdiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBUTEZzLXnu[JVk\WRibX;keYxifGmxbjDv[kBkSU2SIIDyc4R2[3Srb36gZZQhOTByMDDuUUBjgSCWUj3GVmVVKGG|c3H5 MnzjNVc6PTh|NES=

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アッセイ
Methods Test Index PMID
Immunofluorescence
CXCR4; 

PubMed: 28521261     


Representative immunofluorescence images of competition-binding affinity assay of three selected compounds compared to AMD3100. CXCR4 receptors on the cell surface are shown in red fluorescent color in this binding affinity assay using biotinylated TN14003 that binds to CXCR4. When our test compounds are preincubated with the cells and block the binding of biotinylated TN14003, the red fluorescent color gets reduced. The effective concentration (EC) of AMD3100 was 1000 nM, while compounds Ie, IIj and Iq showed much better EC of only 1, 1 and 10 nM, respectively.

β-arrestin2; 

PubMed: 31186083     


Confocal microscopy analysis of CXCR4 and BA2 in Jurkat cells pretreated with vehicle, AMD3100, or X4-2-6 and stimulated with CXCL12, as indicated. Arrows indicate CXCR4 (red), BA2 (green), or colocalization (orange). Images are representative of three independent experiments. Scale bars, 10 μM. DAPI, 4′,6-diamidino-2-phenylindole, dihydrochloride.

28521261 31186083
体内試験 A single topical application of Plerixafor promotes wound healing in diabetic mice by increasing cytokine production, mobilizing bone marrow EPCs, and enhancing the activity of fibroblasts and monocytes/macrophages, thereby increasing both angiogenesis and vasculogenesis. [3] Cohorts of mice are administered with PBS, IGF1, PDGF, SCF, or VEGF for five consecutive days and Plerixafor on the 5th day. The number and size of the colonies are highest in IGF1 plus Plerixafor injected mice compared to PDGF, SCF and VEGF treated groups, in combination with Plerixafor. [4]

お薦めの試験操作(参考用のみ)

動物試験:[4]
- 合併
  • 動物モデル: Twelve-week-old C57BL/6 mice with segmental bone defect
  • 製剤: PBS
  • 投薬量: 5 mg/kg
  • 投与方法: Administered via i.p.
    (参考用のみ)

溶解度 (25°C)

体外 Water 100 mg/mL (125.87 mM)
DMSO Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
Saline
混合させたのち直ちに使用することを推奨します。
30 mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 794.47
化学式

C28H54N8.8HCl

CAS No. 155148-31-5
保管
in solvent
別名 JM 3100 8HCl

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03653247 Recruiting Biological: Plerixafor|Drug: Busulfan|Genetic: BIVV003 Sickle Cell Disease Bioverativ a Sanofi company|Bioverativ Therapeutics Inc. June 28 2019 Phase 1|Phase 2
NCT03547830 Recruiting Drug: Plerixafor|Drug: Gcsf Chronic Granulomatous Disease Federal Research Institute of Pediatric Hematology Oncology and Immunology April 13 2019 Phase 2
NCT03442673 Recruiting Drug: Vinorelbine|Drug: Gemcitabine|Drug: G-CSF Multiple Myeloma University Hospital Inselspital Berne September 17 2018 Phase 2
NCT03226691 Completed Drug: Plerixafor Sickle Cell Disease National Heart Lung and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) July 25 2017 Phase 1

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

CXCRシグナル伝達経路

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID