Lestaurtinib

Cat. No. 3395 7 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： JAK2, FLT3 and TrkA inhibitor; also inhibits AurA and AurB

别名： CEP-701

化学名： (9S,10S,12R)-2,3,9,10,11,12-Hexahydro-10-hydroxy-10-(hydroxymethyl)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one

纯度： ≥98% (HPLC)

引用文献 (7)

通路 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for Lestaurtinib

Lestaurtinib is a potent JAK2, FLT3 and TrkA inhibitor (IC₅₀ values are 0.9, 3 and < 25 nM, respectively). Also inhibits Aurora kinase A and B (IC₅₀ values are 8.1 and 2.3 nM, respectively) and prevents STAT5 phosphorylation (IC₅₀ = 20 - 30 nM). Exhibits antiproliferative activity in vitro (IC₅₀ = 30 - 100 nM in HEL92.1.7 cells) and is effective against myeloproliferative disorders in vivo.

技术数据 for Lestaurtinib

分子量	439.46
公式	C₂₆H₂₁N₃O₄
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	111358-88-4
PubChem ID	126565
InChI Key	UIARLYUEJFELEN-LROUJFHJSA-N
Smiles	O=C(NC3)C1=C3C(C4=CC=CC=C4N5[C@@]78C)=C5C2=C1C6=C(C=CC=C6)N2[C@](O7)(C[C@](CO)8O)[H]

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for Lestaurtinib

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	DMSO	20	46

制备储备液 for Lestaurtinib

以下数据基于产品分子量 439.46。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
0.46 mM	4.95 mL	24.73 mL	49.47 mL
2.3 mM	0.99 mL	4.95 mL	9.89 mL
4.6 mM	0.49 mL	2.47 mL	4.95 mL
23 mM	0.1 mL	0.49 mL	0.99 mL

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产品说明书 for Lestaurtinib

分析证书/产品说明书

化学品安全技术说明书

参考文献 for Lestaurtinib

参考文献是支持产品生物活性的出版物。

et al (1999) The novel Ann.N.Y.Acad.Sci. 252 et al (2007) Effect Ann.N.Y.Acad.Sci. 190 et al (2008) Lestaurinib Blood 5663

If class="highlight">Miknyoczki Trk receptor tyrosine kinase inhibitor CEP-701 (KT-5555) exhibits antitumor efficacy against human pancreatic carcinoma (Panc1) xenograft growth and in vivo invasiveness. 880 PMID: 10415871

class="highlight">Weisel of FLT3 inhibition on normal hematopoietic progenitor cells. 1106 PMID: 17442779

class="highlight">Hexner (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders. 111 PMID: 17984313

class="highlight">Gäbler effects of Janus and Aurora kinase inhibition by CEP701 in cells expressing Jak2V617F. 17 PMID: 23301855 you know of a relevant reference for Lestaurtinib, please let us know.

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关键词: Lestaurtinib, Lestaurtinib supplier, TrkA, JAK2, FLT3, inhibitors, inhibits, Neurotrophin, Receptors, Tyrosine, Kinases, RTKs, Janus-Activated, CEP701, aurora, kinases, AurA, AurB, CEP-701, JAK, Kinase, Trk, Aurora, 3395, Tocris Bioscience

7 篇 Lestaurtinib 的引用文献

引用文献是使用了 Tocris 产品的出版物。 Lestaurtinib 的部分引用包括：

Pinto et al (2018) Lestaurtinib is a potent inhibitor of anaplastic thyroid cancer cell line models. PLoS One 13 e0207152 PMID: 30419054

Rogers and Gahring (2015) Upregulation of Nicotinic Acetylcholine Receptor α4+β2 through a Ligand-Independent PI3Kβ Mechanism That Is Enhanced by TNFα and the Jak2/p38Mapk Pathways. Eur J Neurosci 10 e0143319 PMID: 26619345

Kharazi et al (2011) Impact of gene dosage, loss of wild-type allele, and FLT3 ligand on Flt3-ITD-induced myeloproliferation. Blood 118 3613 PMID: 21813452

Gäbler et al (2013) Cooperative effects of Janus and Aurora kinase inhibition by CEP701 in cells expressing Jak2V617F. J Cell Mol Med 17 265 PMID: 23301855

Deshpande et al (2012) Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms. Leukemia 26 708 PMID: 21926964

Beck et al (2016) Synthetic Lethal Screen Demonstrates That a JAK2 Inhibitor Suppresses a BCL6-dependent IL10RA/JAK2/STAT3 Pathway in High Grade B-cell Lymphoma. J Biol Chem 291 16686 PMID: 27268052

Gaji et al (2014) Expression of the essential Kinase PfCDPK1 from Plasmodium falciparum in Toxoplasma gondii facilitates the discovery of novel antimalarial drugs. Antimicrob Agents Chemother 58 2598 PMID: 24550330

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Pathways for Lestaurtinib

JAK-STAT Signaling Pathway

The JAK-STAT signaling pathway has several roles, including the control of cell proliferation and hematopoiesis. It is the main signal transduction cascade from cytokine receptors.