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ApexBio/MLN0905/10mM (in 1mL DMSO)/A8680

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¥23280.00
货号:A8680
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品牌:ApexBio
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Molarity CalculatorDilution Calculator
MLN0905Potent PLK1 inhibitor

Catalog No.A8680
SizePriceStockQty
10mM (in 1mL DMSO)
$257.00
In stock
5mg
$216.00
In stock
10mg
$366.00
In stock
50mg
$1,164.00
In stock

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Publications citing ApexBio Products

Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.
Nature.2018 Jun 13.
Nature.2018 Jun 27.
Nature.2018 Mar 29;555(7698):673-677.
Nature.2017 Sep 7;549(7670):96-100.
Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8
Nat Nanotechnol.2017 Dec;12(12):1190-1198.
Nature Biotechnology.2017 Jun;35(6):569-576
Nat Med.2018 Sep 17.
Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.
Cell.Available online 25 October 2018.
Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.
Cell.2018 Jun 28;174(1):172-186.e21.
Cell.2018 Feb 22;172(5):1007-1021.e17.
Cell.2017 Nov 30;171(6):1284-1300.e21.
Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.
Cell.2017 Jul 13;170(2):312-323
Nat Med.2018 Jan 29.
Nat Med.2017 Nov;23(11):1342-1351.
Cell.2017 Apr 6;169(2):286-300.
Cell.2015 Aug 27;162(5):987-1002.
Cell.2015 Feb 12;160(4):729-44.
Nature Medicine.2017 Apr;23(4):493-500.
Cancer Cell.2018 May 14;33(5):905-921.e5.
Cancer Cell.2018 Apr 9;33(4):752-769.e8.
Cancer Cell.2018 Mar 12;33(3):401-416.e8.
Cancer Cell.2017 Aug 14;32(2):253-267.e5.
Nat Methods.2018 Jul;15(7):523-526.
Cell Stem Cell.2018 May 3;22(5):769-778.e4.
Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.

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Quality Control

Quality Control & MSDS

View current batch:
    Purity = 98.00%
  • COA (Certificate Of Analysis)
  • MSDS (Material Safety Data Sheet)
  • Datasheet

Chemical structure

MLN0905

Biological Activity

DescriptionMLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM.
TargetsPLK1
IC502 nM

MLN0905 Dilution Calculator

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Chemical Properties

Cas No. 1228960-69-7SDF Download SDF
Chemical Name 2-[[5-[3-(dimethylamino)propyl]-2-methylpyridin-3-yl]amino]-9-(trifluoromethyl)-5,7-dihydropyrimido[5,4-d][1]benzazepine-6-thione
Canonical SMILES CC1=C(C=C(C=N1)CCCN(C)C)NC2=NC=C3CC(=S)NC4=C(C3=N2)C=CC(=C4)C(F)(F)F
Formula C24H25F3N6S M.Wt 486.56
Solubility ≥24.35mg/mL in DMSO Storage Store at -20°C
Physical AppearanceA solidShipping ConditionEvaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

MLN0905 is a potent inhibitor of PLK1 with IC50 value ranges from 3 to 24 nM [1].

Polo-like kinase 1 (PLK1) is a family of conserved serine/threonine kinases and plays an important role in regulating cell cycle. It has been revealed that PLK1 drives cell cycle progression by triggerting G2/M transition and is considered as a pro-oncogene which overexpressed in tumor cells [2].

MLN0905 is a selective PLK1 inhibitor and has similar effect as RNAi hnockdown. When tested with HT-29 cells, MLN0905 treatment significantly increased pHisH3 expression which indicated that cells were arrested in G2/M phase by inhibiting PLK1 expression [1].

In mouse model with human diffuse large B-cell lymphoma (DLBCL) cell line OCILY-19 subcutaneous xenograft, co-administration of MLN0905 and rituximab markedly reduced tumor volume and increased survival time through inhibiting PLK1 which resulted in mitotic arrest [1]. And the same result was achieved when using nude mice model with human colon tumor HT29 xenograft, MLN0905 treatment significantly inhibited tumor growth or progression [3].

References: [1].Shi, J.Q., et al., MLN0905, a small-molecule plk1 inhibitor, induces antitumor responses in human models of diffuse large B-cell lymphoma. Mol Cancer Ther, 2012. 11(9): p. 2045-53.[2].Espeut, J., et al., Natural Loss of Mps1 Kinase in Nematodes Uncovers a Role for Polo-like Kinase 1 in Spindle Checkpoint Initiation. Cell Rep, 2015. [3].Duffey, M.O., et al., Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905). J Med Chem, 2012. 55(1): p. 197-208.

ApexBio的3X FLAG Peptide FLAG标签系统利用与目标蛋白质1融合的短而亲水的8个氨基酸的肽段。FLAG肽与抗体M1结合。结合是钙依赖性方式2还是非依赖性3仍存在争议。该系统的缺点是单克隆抗体纯化基质不如其他基质稳定。通常,可以用特异性单克隆抗体检测小标签。为了改善对FLAG标签的检测,已经开发了3x FLAG系统。这种三级FLAG表位是亲水的,长22个氨基酸,可以检测到高达10 fmol的表达融合蛋白。激烈热球菌的带有FLAG标签的麦芽糖糊精结合蛋白已被结晶4,其晶体质量与未标记蛋白的晶体质量非常相似。 最后,可以通过用肠激酶处理去除FLAG标签,肠激酶对肽序列5的5个C末端氨基酸具有特异性。