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ApexBio/Cevipabulin/10mM (in 1mL DMSO)/B5922

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¥29640.00
货号:B5922
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品牌:ApexBio
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CevipabulinAnti-microtubule agent

Catalog No.B5922
SizePriceStockQty
10mM (in 1mL DMSO)
$241.00
In stock
5mg
$218.00
In stock
10mg
$374.00
In stock
50mg
$1,154.00
In stock
100mg
$1,482.00
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.

Quality Control

Quality Control & MSDS

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

Chemical structure

Cevipabulin

Cevipabulin Dilution Calculator

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Cevipabulin Molarity Calculator

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Chemical Properties

Cas No. 849550-05-6SDF Download SDF
Chemical Name (S)-5-chloro-6-(2,6-difluoro-4-(3-(methylamino)propoxy)phenyl)-N-(1,1,1-trifluoropropan-2-yl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Canonical SMILES C[C@@](NC1=C(C(Cl)=NC2=NC=NN12)C3=C(F)C=C(OCCCNC)C=C3F)([H])C(F)(F)F
Formula C18H18ClF5N6O M.Wt 464.82
Solubility Soluble in DMSO Storage Store at -20°C
Shipping 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

Cevipabulin (TTI-237) is a new anti-microtubule agent [1][2][3][4].

Microtubules are a component of the cytoskeleton that participate in many crucial cellular functions, include maintaining the structure of the cell, forming the cytoskeleton and chromosome separation.

Cevipabulin (TTI-237) is a new anti-microtubule agent with antitumor activity. In COLO 205 cells, TTI-237 inhibited cell proliferation with IC50 value of 31 nM [1]. At low ratios of TTI-237: tubulin heterodimer (about 1:30), TTI-237 increased depolymerization kinetics in response to low temperature, but stabilized the aggregates at high ratios (about 1:4). TTI-237 inhibited the exchange of [3H]GTP at the exchangeable nucleotide site of the tubulin heterodimer [2]. Cevipabulin (TTI-237) increased tubulin polymerization. Cevipabulin was stable and water-soluble, and could be administered i.v. or p.o. in saline [3]. TTI-237 inhibited the binding of [3H]vinblastine to tubulin, but significantly increased turbidity development that more closely resembled the effect of docetaxel. In Hela cells, TTI-237 (34 nmol/L) induced multiple spindle poles and multi-nuclear cells. At 20-40 nmol/L, TTI-237 produced sub-G1 nuclei, while at > 50 nmol/L, TTI-237 induced G2-M block.

In athymic mice bearing LoVo human colon adenocarcinoma, TTI-237 exhibited good antitumor activity in a dose-dependent way. In mice bearing U87-MG human glioblastoma, TTI-237 (25 mg/kg) given both i.v. and p.o. were equally effective [4].

References:[1]. Zhang N, Ayral-Kaloustian S, Nguyen T, et al. 2-cyanoaminopyrimidines as a class of antitumor agents that promote tubulin polymerization. Bioorg Med Chem Lett, 2007, 17(11): 3003-3005.[2]. Beyer CF, Zhang N, Hernandez R, et al. The microtubule-active antitumor compound TTI-237 has both paclitaxel-like and vincristine-like properties. Cancer Chemother Pharmacol, 2009, 64(4): 681-689. [3]. Ayral-Kaloustian S, Zhang N, Beyer C. Cevipabulin (TTI-237): preclinical and clinical results for a novel antimicrotubule agent. Methods Find Exp Clin Pharmacol, 2009, 31(7): 443-447.[4]. Beyer CF, Zhang N, Hernandez R, et al. TTI-237: a novel microtubule-active compound with in vivo antitumor activity. Cancer Res, 2008, 68(7): 2292-2300.

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。