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| ln Vitro |
In comparison to other cytoplasmic tyrosine kinases, 419259 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 blocks 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 proliferation. In K562 and other CML cell lines, A-419259 inhibits 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 [3]. Anthony Cheung, et al. Anti-Folate Receptor Alpha-Directed Antibody Therapies Restrict the Growth of Triple-negative Breast Cancer. Clin Cancer Res. 2018 Oct 15;24(20):5098-5111 |
| Molecular Formula |
C29H34N6O
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|---|---|
| Molecular Weight |
482.62
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| Exact Mass |
482.279
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| CAS # |
364042-47-7
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| Related CAS # |
A 419259 trihydrochloride;1435934-25-0
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| PubChem CID |
6539952
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
8.066
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
36
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| Complexity |
679
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FDVSOQRNTAPCHB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H34N6O/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)
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| Chemical Name |
7-[4-(4-methylpiperazin-1-yl)cyclohexyl]-5-(4-phenoxyphenyl)pyrrolo[2,3-d]pyrimidin-4-amine
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| Synonyms |
A419259 A 419259A-419259 trihydrochloride RK-20449 RK 20449RK20449
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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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~207.20 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.18 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0720 mL | 10.3601 mL | 20.7202 mL | |
| 5 mM | 0.4144 mL | 2.0720 mL | 4.1440 mL | |
| 10 mM | 0.2072 mL | 1.0360 mL | 2.0720 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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