A 419259 trihydrochloride

Name: A 419259 trihydrochloride
Brand: Tocris Bioscience
SKU: 3914
Rating: 5 (1 reviews)

Cat. No. 3914 6 Citations 1 Review Submit a Review Datasheet / COA / SDS

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Description: Inhibitor of Src family kinases

Chemical Name: 7-[trans-4-(4-Methyl-1-piperazinyl)cyclohexyl]-5-(4-phenoxyphenyl)-7H-Pyrrolo[2,3-d]pyrimidin-4-amine trihydrochloride

Purity: ≥98% (HPLC)

Datasheet

Citations (6)

Reviews (1)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for A 419259 trihydrochloride

A 419259 trihydrochloride is a potent Hck inhibitor (IC₅₀ = 0.43 nM). Also inhibits other Src family kinases (SFKs). Suppresses proliferation and induces apoptosis in CML cell lines including CD34⁺. Also inhibits acute myeloid leukemia (AML) stem cell proliferation in vitro and in vivo.

Compound Libraries for A 419259 trihydrochloride

A 419259 trihydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for A 419259 trihydrochloride

M. Wt	592.01
Formula	C₂₉H₃₄N₆O.3HCl
Storage	Desiccate at RT
Purity	≥98% (HPLC)
CAS Number	1435934-25-0
PubChem ID	76848881
InChI Key	ALRMEQIQFCUAMR-UHFFFAOYSA-N
Smiles	NC1=C2C(N([C@H]5CC[C@H](N6CCN(C)CC6)CC5)C=C2C3=CC=C(OC4=CC=CC=C4)C=C3)=NC=N1.Cl.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

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

Solubility Data for A 419259 trihydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	59.2	100
	DMSO	11.84	20

Preparing Stock Solutions for A 419259 trihydrochloride

The following data is based on the product molecular weight 592.01. 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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.69 mL	8.45 mL	16.89 mL
5 mM	0.34 mL	1.69 mL	3.38 mL
10 mM	0.17 mL	0.84 mL	1.69 mL
50 mM	0.03 mL	0.17 mL	0.34 mL

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Product Datasheets for A 419259 trihydrochloride

Certificate of Analysis / Product Datasheet

Safety Datasheet

References for A 419259 trihydrochloride

References are publications that support the biological activity of the product.

Wilson et al (2002) Selective pyrrolo-pyrimidine inhibitors reveal a necessary role for Src family kinases in Bcr-Abl signal transduction and oncogenesis. Oncogene 21 8075 PMID: 12444544

Pene-Dumitrescu et al (2008) An inhibitor-resistant mutant of Hck protects CML cells against the antiproliferative and apoptotic effects of the broad spectrum Src family kinase inhibitor A-419259. Oncogene 27 7055 PMID: 18794796

Saito et al (2013) A pyrrolo-pyrimidine derivative targets human primary AML stem cells in vivo. Sci.Transl.Med. 5 PMID: 23596204

If you know of a relevant reference for A 419259 trihydrochloride, please let us know.

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