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A 419259 (A-419259) trihydrochloride is a novel and potent Src family kinases inhibitor with IC50s of 9 nM, 3 nM and 3 nM for Src, Lck and Lyn, respectively.
| ln Vitro |
In contrast to other cytoplasmic tyrosine kinases, A 419259 TriHClide is a second-generation pyrrolopyrimidine that is intended to improve selectivity for the Src family. K-562 cells are inhibited by A-419259 with an IC50 of 0.1–0.3 μM, while Meg-01 proliferation is inhibited with an IC50 of about 0.1 μM. Moreover, A-419259 potently triggered apoptosis in K-562 cells, with dose-dependent increases beginning at 0.1 μM. In two Ph+ cell lines (K-562 and Meg-01), PP2 inhibits Src kinase autophosphorylation with an IC50 ranging from 3 to 10 μM, while A-419259 prevents kinase activation with an IC50 ranging from 0.1 to 0.3 μM. With an IC50 ranging from 0.1 to 0.3 μM, A-419259 significantly suppresses the proliferation of DAGM/Bcr-Abl cells in the absence of IL-3 [1]. A-419259 is a broad-spectrum pyrrolopyrimidine inhibitor that causes CML cell lines to undergo apoptosis and stops growth. In K562 and other CML cell lines, A-419259 suppresses total SFK activity with IC50 values ranging from 0.1 to 0.3 μM [2].
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| References |
[1]. Wilson MB, et al. Selective pyrrolo-pyrimidine inhibitors reveal a necessary role for Src family kinases in Bcr-Abl signal transduction and oncogenesis. Oncogene. 2002 Nov 21;21(53):8075-88.
[2]. Pene-Dumitrescu T, et al. 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 (2008) 27, 7055-7069 |
| Molecular Formula |
C₂₉H₃₇CL₃N₆O
|
|---|---|
| Molecular Weight |
592.00
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| Exact Mass |
590.209
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| CAS # |
1435934-25-0
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| Related CAS # |
A 419259;364042-47-7
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| PubChem CID |
76848881
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| Appearance |
White to yellow solid powder
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| LogP |
8.066
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
39
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| Complexity |
679
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ALRMEQIQFCUAMR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H34N6O.3ClH/c1-33-15-17-34(18-16-33)22-9-11-23(12-10-22)35-19-26(27-28(30)31-20-32-29(27)35)21-7-13-25(14-8-21)36-24-5-3-2-4-6-24;;;/h2-8,13-14,19-20,22-23H,9-12,15-18H2,1H3,(H2,30,31,32);3*1H
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| Chemical Name |
7-[4-(4-methylpiperazin-1-yl)cyclohexyl]-5-(4-phenoxyphenyl)pyrrolo[2,3-d]pyrimidin-4-amine;trihydrochloride
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| Synonyms |
RK 20449 trihydrochlorideA419259 RK-20449 A-419259
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O : ~50 mg/mL (~84.46 mM)
DMSO : ~1 mg/mL (~1.69 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (168.92 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6892 mL | 8.4459 mL | 16.8919 mL | |
| 5 mM | 0.3378 mL | 1.6892 mL | 3.3784 mL | |
| 10 mM | 0.1689 mL | 0.8446 mL | 1.6892 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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