AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl(T315I). Phase 2.

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  • HEL cells were treated with 0.5, 1 or 5 uM of AT9283 or left untreated for 3 hrs. The expression and phosphorylation state of STAT5 (P-STAT5) and Jak2 (P-Jak2) was assessed by Western blot immunodetection.

    J Cell Mol Med 2013 17(2), 265-76. AT9283 purchased from Selleck.

    AM-005 inhibits the growth of HT29 cells in vivo. The tumor volume was measured after intragastric administration of AM-005 (15 mg/kg or 25 mg/kg). The 25 mg/kg AT9283 was used as a positive control. The results are the mean tumor volume盨D for groups of n = 8.

    Drug Development Reseach 2013 272-281. AT9283 purchased from Selleck.

  • HEL cells were treated for 3 hours with the indicated concerntrations of AT9283. AT9283 inhibitors Jak2-V617F mediated signal transduction at submicromolar concentrations in intact cells . At concentrations of 490 nm the Jak2-V617F inhibition is almost complete and has reached almost background levels (for background STAT5 phosphorylation see 4400nm)



    Dr. Claude Haan and Catherine Rolvering of Universite du Luxembourg. AT9283 purchased from Selleck.




製品説明 AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl(T315I). Phase 2.
JAK3 [1]
(Cell-free assay)
JAK2 [1]
(Cell-free assay)
Aurora A [1]
(Cell-free assay)
Aurora B [1]
(Cell-free assay)
Abl1 (T315I) [1]
(Cell-free assay)
1.1 nM 1.2 nM ~3.0 nM ~3.0 nM 4 nM

AT9283 leads to a clear polyploid phenotype by inhibiting the activity of Aurora B kinase in HCT116 cells with IC50 of 30 nM. Furthermore, AT9283 also produces the potent inhibition on HCT116 colony formation. [1]

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 cells NF7oRpFEgXSxdH;4bYPDqGG|c3H5 MYexNE0yPCCmYYnz NHnuc2NEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYYPz[ZN{\WRiYYOgcpVu[mW{IH;mJINwdG:waXXzJIFnfGW{IEGwJJRwKDF2IHThfZMh[nliY3;sc456KG[xcn3pcoch[XO|YYmsJGlEPTB;MD6wNVIh|ryP NUm5cJhtOTlzNEO1Olc>
HT-29 cells M37jeWZ2dmO2aX;uJIF{e2G7 NHy1fXc4OiCq MYXBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwM{izJO69VQ>? NG[zVpMzOzZ4NEC5PS=>
A549 cells NYnSTIFMTnWwY4Tpc44h[XO|YYm= M4XHS|czKGh? M37lVGFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkWxNkDPxE1? MkD1NlM3PjRyOUm=
LoVo cells MYHGeY5kfGmxbjDhd5NigQ>? Mlu2O|IhcA>? MUDBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCOb2\vJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC53NUOg{txO M2LvVVI{PjZ2MEm5
K562 cells NYTTc|JSTnWwY4Tpc44h[XO|YYm= NFn1SW04OiCq NGn5SIRCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MT62JO69VQ>? MVGyN|Y3PDB7OR?=
U937 cells M{PLNmZ2dmO2aX;uJIF{e2G7 MYW3NkBp NYHBZnp5SW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gWVk{PyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5 M3PURVI{PjZ2MEm5


体内試験 In HCT116 human colon carcinoma xenograft bearing mice, AT9283 treatment (15 mg/kg and 20 mg/kg) for 16 days results in a significant tumor growth inhibition of 67% and 76%, respectively. In addition, AT9283 also exhibits a significantly longer half-life in tumors(2.5 hours) compared with plasma (0.5 hour) and modest oral bioavailability in mice (Fp.o. = 24%). [1]




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Aurora A and Aurora B Kinase Assays:

Assays for Aurora A and B are performed in a DELFIA format. Aurora A enzyme is incubated with AT9283 and 3 μM cross-tide substrate (biotin-CGPKGPGRRGRRRTSSFAEG) in 10 mM MOPS, pH 7, 0.1 mg/mL BSA, 0.001% Brij-35, 0.5% glycerol, 0.2 mM EDTA, 10 mM MgCl2, 0.01% β-mercaptoethanol, 15 μM ATP, and 2.5% DMSO. Aurora B enzyme is incubated with AT9283, 3 μM of the above substrate in 25 mM Tris, pH 8.5, 5 mM MgCl2, 0.1 mg/mL BSA, 0.025% Tween-20, 1 mM DTT, 15 μM ATP, and 2.5% DMSO. Reactions are allowed to proceed for 60 minutes and 45-90 minutes for Aurora A and Aurora B, respectively, before quenching with EDTA. The reaction mixtures are then transferred to a neutravidin-coated plate, and phosphorylated peptide is quantified by means of a phospho-specific antibody and a europium labeled secondary antibody using time-resolved fluorescence (excitation, 337 nm; emission, 620 nm). IC50 values for the control compounds are 92 nM (Aurora A assay) and 17 nM (Aurora B).


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  • 細胞株: HCT 116 cells
  • 濃度: 1 nM - 10 μM
  • 反応時間: 72 hours
  • 実験の流れ:

    HCT 116 cells are cultured in DMEM + 10% FBS + GLUTAMAX I. Black 96-well flat-bottomed (clear) tissue culture treated plates are seeded in 200 μL of medium and incubated for approximately 16 hours at 37°C in a humidified atmosphere of 5% CO2 in air. Cells are treated with test compound at nine different concentrations (spanning 1 nM to 10 μM, plus DMSO vehicle control) and then incubated for 72 hours. Polyploidy morphological observations of the cells are then noted. The concentration of AT9283 required to produce a distinct polyploid phenotype is reported. Cells are seeded at a concentration of 75−100 cells/mL relevant culture media onto 6- or 24-well tissue culture plates and allowed to recover for 16 hours. Test compound (11 concentrations spanning 0.1 nM to 10 μM) or vehicle control (DMSO) is added to duplicate wells to give a final DMSO concentration of 0.1%. Following compound addition, colonies are allowed to grow between 10 and 14 days for optimum discrete colony counting. Colonies are fixed in 2 mL of Carnoys fixative (25% acetic acid, 75% MeOH) and stained in 2 mL of 0.4% w/v crystal violet. The numbers of colonies in each well is counted. IC50 values are calculated by sigmoidal dose-response (variable slope) IC50 curves using Prism Graphpad software.



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  • 動物モデル: HCT116 cells are injected s.c. Into the hind flank of male BALB/c mice.
  • 製剤: Belinostat is dissolved in 10% DMSO, 20% water, 70% hydroxypropyl- β-cyclodextrin (25% w/v aq).
  • 投薬量: 15 mg/kg and 20 mg/kg
  • 投与方法: Administered via i.p.

溶解度 (25°C)

体外 DMSO 76 mg/mL (199.25 mM)
Ethanol 38 mg/mL (99.62 mM)
Water 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):
2% DMSO+30% PEG 300+ddH2O

* 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。


分子量 381.43


CAS No. 896466-04-9
in solvent
別名 N/A





質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)


  • 質量





開始濃度 x 開始体積 = 最終濃度 x 最終体積


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

  • C1



  • 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):




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


質量 濃度 体積 分子量


NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01431664 Completed Leukemia Cancer Research UK September 2011 Phase 1
NCT01145989 Completed Multiple Myeloma NCIC Clinical Trials Group|Canadian Cancer Trials Group June 2010 Phase 2
NCT00985868 Active not recruiting Unspecified Childhood Solid Tumor Protocol Specific Cancer Research UK September 2009 Phase 1
NCT00443976 Completed Non-Hodgkins Lymphoma|Unspecified Adult Solid Tumor Protocol Specific NCIC Clinical Trials Group|Canadian Cancer Trials Group January 2007 Phase 1
NCT00522990 Terminated Acute Myeloid Leukemia|Acute Lymphoblastic Leukemia|Chronic Myeloid Leukemia|Myelodysplastic Syndromes|Myelofibrosis Astex Pharmaceuticals September 2006 Phase 1|Phase 2



Handling Instructions


  • * 必須


JAK Inhibitors with Unique Features


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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