AP 24534

Cat. No. 4274 5 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： Potent multi-kinase and pan-Bcr-Abl inhibitor

别名： Ponatinib

化学名： 3-(2-Imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-benzamide

纯度： ≥98% (HPLC)

引用文献 (5)

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 AP 24534

AP 24534 is a potent multi-kinase and pan-Bcr-Abl inhibitor. Displays potent activity against cell lines expressing native Bcr-Abl or Bcr-Abl^T3151 (IC₅₀ values are 0.37 and 2.0 nM respectively); also inhibits other Abl kinase domain mutants at nanomolar potencies. Exhibits inhibitory activity against PDGFRα, c-Src and c-Kit (IC₅₀ values are 1.1, 5.4 and 12.5 nM respectively); potently inhibits FGFR and VEGFR family kinases. Orally active. Identified as targeting human host proteins that interact with SARS-CoV-2.

技术数据 for AP 24534

分子量	532.56
公式	C₂₉H₂₇F₃N₆O
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	943319-70-8
PubChem ID	24826799
InChI Key	PHXJVRSECIGDHY-UHFFFAOYSA-N
Smiles	CC1=CC=C(C(NC4=CC=C(CN5CCN(C)CC5)C(C(F)(F)F)=C4)=O)C=C1C#CC2=CN=C3N2N=CC=C3

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 AP 24534

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	DMSO	53.26	100
	ethanol	26.63	50

制备储备液 for AP 24534

以下数据基于产品分子量 532.56。 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
1 mM	1.88 mL	9.39 mL	18.78 mL
5 mM	0.38 mL	1.88 mL	3.76 mL
10 mM	0.19 mL	0.94 mL	1.88 mL
50 mM	0.04 mL	0.19 mL	0.38 mL

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产品说明书 for AP 24534

分析证书/产品说明书

化学品安全技术说明书

参考文献 for AP 24534

参考文献是支持产品生物活性的出版物。

O'Hare et al (2009) AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell 16 401 PMID: 19878872

Huang et al (2010) Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)-methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-Abelson (BCR-ABL) J.Med.Chem. 53 4701 PMID: 20513156

Gozgit et al (2011) Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies. Mol.Cancer Ther. 10 1028 PMID: 21482694

Gordon et al (2020) A SARS-CoV-2-human protein-protein interaction map reveals drug targets and potential drug-repurposing. Nature 583 PMID: 32353859

If you know of a relevant reference for AP 24534, please let us know.

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