A 419259 trihydrochloride

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Cat.No. 3914 - A 419259 trihydrochloride | C29H34N6O.3HCl | CAS No. 1435934-25-0
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
Literature

Biological Activity

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.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 592.01. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Literature in this Area

Cancer

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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

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