A 419259 GMP is the GMP grade A 419259 (HY-15764), inducing cell apoptosis. GMP-grade small molecules can be used as auxiliary reagents in cell therapy. A 419259 (RK-20449) is a broad-spectrum pyrrole-pyrimidine inhibitor targeting Src, Lck, and Lyn with IC50s of 9 nM, <3 nM, and <3 nM, respectively.
For research use only. We do not sell to patients.
- CAS No.: 364042-47-7
- Formula: C29H34N6O
- Molecular Weight:482.63
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 9 nM (Src), <3 nM (Lck), <3 nM (Lyn), 3 μM (Abl)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MV4-11 | GI50 |
40 nM
Compound: RK-20449
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Growth inhibition of human MV4-11 cells after 3 days by Alamar blue assay
Growth inhibition of human MV4-11 cells after 3 days by Alamar blue assay
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[PMID: 29037944] |
A419259 is a second-generation pyrrolopyrimidine that blocks proliferation and induces apoptosis in CML cell lines. It induces apoptosis in K-562 cells and also inhibits Meg-01 proliferation (IC50=0.1 μM)[1].
In the absence of IL-3, A-419259 strongly inhibits DAGM/Bcr-Abl cell proliferation (IC50=0.1-0.3 μM)[1].
A-419259 also inhibits overall SFK activity in CML cell lines and blocks Src kinase activation (IC50=0.1-0.3 μM)[1].
A 419259 GMP (1 μM; 16 h) inhibits endogenous SFK (c-Src and Lck) activity, thereby inhibiting Src-driven differentiation of mES cells toward primitive ectoderm-like cells[2].
A 419259 GMP (0.3, 1 μM; 5 days) has no effect on undifferentiated colony morphology of hES cells grown in mTeSR medium[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 364042-47-7
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Appearance Solid
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Molecular Weight 482.63
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Formula C29H34N6O
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Color White to light yellow
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SMILES
NC1=C2C(N([C@H]3CC[C@H](N4CCN(C)CC4)CC3)C=C2C5=CC=C(OC6=CC=CC=C6)C=C5)=NC=N1
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Synonyms
RK-20449 (GMP)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
DMSO : 100 mg/mL (207.20 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[2]. Zhang X, et al. Src-family tyrosine kinase activities are essential for differentiation of human embryonic stem cells. Stem Cell Res. 2014 Nov;13(3 Pt A):379-89. [Content Brief]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0720 mL | 10.3599 mL | 20.7198 mL | 51.7995 mL |
| 5 mM | 0.4144 mL | 2.0720 mL | 4.1440 mL | 10.3599 mL | |
| 10 mM | 0.2072 mL | 1.0360 mL | 2.0720 mL | 5.1800 mL | |
| 15 mM | 0.1381 mL | 0.6907 mL | 1.3813 mL | 3.4533 mL | |
| 20 mM | 0.1036 mL | 0.5180 mL | 1.0360 mL | 2.5900 mL | |
| 25 mM | 0.0829 mL | 0.4144 mL | 0.8288 mL | 2.0720 mL | |
| 30 mM | 0.0691 mL | 0.3453 mL | 0.6907 mL | 1.7267 mL | |
| 40 mM | 0.0518 mL | 0.2590 mL | 0.5180 mL | 1.2950 mL | |
| 50 mM | 0.0414 mL | 0.2072 mL | 0.4144 mL | 1.0360 mL | |
| 60 mM | 0.0345 mL | 0.1727 mL | 0.3453 mL | 0.8633 mL | |
| 80 mM | 0.0259 mL | 0.1295 mL | 0.2590 mL | 0.6475 mL | |
| 100 mM | 0.0207 mL | 0.1036 mL | 0.2072 mL | 0.5180 mL |
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