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ApexBio/ASP3026/10mM (in 1mL DMSO)/A3193

价格
¥14000.00
货号:A3193
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品牌:ApexBio
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商品描述
Related Products
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Molarity CalculatorDilution Calculator
ASP3026ALK inhibitor,potent and selective

Catalog No.A3193
SizePriceStockQty
10mM (in 1mL DMSO)
$90.00
In stock
5mg
$70.00
In stock
10mg
$100.00
In stock
50mg
$300.00
In stock
200mg
$700.00
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 = 98.02%
  • COA (Certificate Of Analysis)
  • HPLC
  • NMR (Nuclear Magnetic Resonance)
  • MSDS (Material Safety Data Sheet)
  • Datasheet

Chemical structure

ASP3026

Biological Activity

DescriptionASP3026 is a selective inhibitor of ALK with IC50 value of 3.5 nM.
TargetsALK
IC503.5 nM

ASP3026 Dilution Calculator

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Chemical Properties

Cas No. 1097917-15-1SDF Download SDF
Synonyms ASP 3026;ASP-3026
Chemical Name 2-N-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)-1,3,5-triazine-2,4-diamine
Canonical SMILES CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC=NC(=N2)NC3=C(C=C(C=C3)N4CCC(CC4)N5CCN(CC5)C)OC
Formula C29H40N8O3S M.Wt 580.74
Solubility ≥14.5 mg/mL in DMSO, ≥4.9 mg/mL in EtOH with ultrasonic and warming, <2.51 mg/ml="" in="" h2o=""> 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

ASP3026 is a selective inhibitor of ALK with IC50 value of 3.5 nM [1].

ASP3026 is a potent ALK inhibitor and has a different selectivity with the reported ALK inhibitor crizotinib. When tested with a panel of 86 tyrosine kinases, ASP3026 showed the highest selectivity for ALK, ROS and ACK kinases. In NCI-H2228 NSCLC cells expressing EML4-ALK, five-day treatment of ASP3026 resulted in a cell growth inhibition with IC50 value of 64.8 nM. ASP3026 also inhibited the viability of NPM-ALK+ ALCL cells with IC50 values of 0.4, 0.75, 1 and 2.5 µM in SU-DHL-1, SUP-M2, SR-786 and Karpas 299 cells, respectively [2, 3].

In mouse model with NCI-H2228 subcutaneous xenograft, oral administration of ASP3026 caused significant reduction of phosphorylated ALK and tumor growth. 30 mg/kg/d ASP3026 for 2 weeks induced tumor regression by 78%. In mice injected with Karpas 299 cells, ASP3026 treatment caused remarkable lymphoma regression [2, 3].

References:[1] Kuromitsu S, Mori M, Shimada I, et al. Anti-tumor activity of ASP3026, a novel and selective ALK inhibitor of anaplastic lymphoma kinase (ALK).Annual Meeting of the American Association for Cancer Research (AACR), Orlando, FL. 2011.[2] Mori M, Ueno Y, Konagai S, et al. The Selective Anaplastic Lymphoma Receptor Tyrosine Kinase Inhibitor ASP3026 Induces Tumor Regression and Prolongs Survival in Non–Small Cell Lung Cancer Model Mice. Molecular cancer therapeutics, 2014, 13(2): 329-340.[3] George S K, Vishwamitra D, Manshouri R, et al. The ALK inhibitor ASP3026 eradicates NPM-ALK+ T-cell anaplastic large-cell lymphoma in vitro and in a systemic xenograft lymphoma model. Oncotarget, 2014, 5(14): 5750-5763.

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。