A 419259
Based on 11 publication(s) in Google Scholar
A 419259 is a broad-spectrum pyrrolo-pyrimidine inhibitor, has high selectivity towards the Src family. A 419259 shows inhibitory effect for Src, Lck and Lyn with IC50 of 9 nM, <3 nM and <3 nM, respectively.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.88%
- CAS 番号: 364042-47-7
- 分子式: C29H34N6O
- 分子量:482.63
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 A 419259
More- Blood. 2016 Jun 23;127(25):3237-52. [Abstract]
- Adv Sci (Weinh). 2025 Jun 30:e17764. [Abstract]
- Aging Cell. 2026 Jan 20;25(2):e70352.
- J Med Chem. 2024 Nov 28;67(22):20571-20579. [Abstract]
- Commun Biol. 2026 Apr 9;9(1):780. [Abstract]
- Microb Pathog. 2024 Dec 25:199:107252. [Abstract]
- Biochem Biophys Res Commun. 2026 Aug 27:828:154112. [Abstract]
- Res Sq. 2026 May 8:rs.3.rs-9500406. [Abstract]
- Free University of Berlin. 2025 Aug 4.
- Patent. US20250228856A1.
- Patent. US20170333436A1.
生物活性
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 (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 (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.
化学情報
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CAS 番号 364042-47-7
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性状 Solid
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分子量 482.63
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分子式 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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別名
RK-20449
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (11)
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Journal Impact Factor
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Most Recent
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Blood
HCK is a survival determinant transactivated by mutated MYD88, and a direct target of ibrutinib. [Abstract]2016 Jun 23;127(25):3237-52. PMID: 27143257 -
Adv Sci (Weinh)
2025 Jun 30:e17764. PMID: 40586282 -
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J Med Chem
2024 Nov 28;67(22):20571-20579. PMID: 39513680 -
Commun Biol
Enhancing reprogramming towards induced human expanded pluripotency through substitution of SOX2 with engineered SOX17 transcription factors. [Abstract]2026 Apr 9;9(1):780. PMID: 41957290 -
Microb Pathog
Upregulation of haematopoetic cell kinase (Hck) activity by a secreted parasite effector protein (Ta9) drives proliferation of Theileria annulata-transformed leukocytes. [Abstract]2024 Dec 25:199:107252. PMID: 39730099 -
Biochem Biophys Res Commun
Hematopoietic cell kinase activation in skeletal myocytes contributes to local inflammation and pain sensitization in myofascial trigger points. [Abstract]2026 Aug 27:828:154112. PMID: 42269276 -
Res Sq
Cyclin-Dependent Kinase 5 Contributes to Bruton's Tyrosine Kinase Inhibitor Resistance via the IRE1α/XBP1 Axis in Mantle Cell Lymphoma. [Abstract]2026 May 8:rs.3.rs-9500406. PMID: 42147166 -
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溶剤 & 溶解度
DMSO : 12.5 mg/mL (25.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (2.59 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (2.59 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
In vitro kinase assays are performed on His(6)-tagged Lck (residues 62-509) and full-length c-Abl purified from Sf-9 cells, and commercial sources of Lyn, Src and PKC. Lck, Lyn, Src and Abl activities are measured with an ELISA-based assay. Flat bottom 96-well ELISA plates are incubated with a 200 μg/mL solution of Poly(Glu,Tyr) 4 : 1 substrate in phosphate buffered saline (PBS) for 1 h at 37°C and then washed with PBS containing 0.1% Tween-20 (PBS-T). Inhibitor dilutions are added to the washed plates already containing the appropriate enzyme in kinase assay buffer (250 mM Mopso, pH 6.75, 10 mM MgCl2, 2 mM MnCl2, 2.5 mM DTT, 0.02% BSA, 2 mM Na3VO4, 5% DMSO, 5 μM ATP). After incubation at room temperature for 20 min, plates are washed three times with PBS-T and plate-bound phosphotyrosine is detected with an anti-phosphotyrosine-HRP antibody conjugate and subsequent color development with K-Blue reagents. All assays are optimized to use the least amount of enzyme necessary for a reproducible signal-to-noise ratio[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
K-562 cells are grown in RPMI 1640 supplemented with 10% fetal calf serum (FCS), and 50 g/mL Gentamycin. Meg-01 cells are cultured in Vitacell modified RPMI 1640 (ATCC), supplemented with 10% FCS and 50 μg/mL Gentamycin. The human GM-CSF-dependent myeloid leukemia cell line TF-1 is grown in RPMI 1640 supplemented with 10% FCS, 50 μg/mL Gentamycin, and 1 ng/mL of recombinant human GM-CSF. DAGM murine myeloid leukemia cells are cultured in RPMI 1640 supplemented with 10% FCS, 50 μg/mL Gentamycin, and 0.5 ng/mL recombinant IL-3. Concentrated stock solutions of PP2 (5 mM) and A-419259 (2 mM) are prepared in DMSO and stored at -20°C. Cellular proliferation is measured using the Live/Dead growth assay. This assay employs calcein-AM, a fluorogenic esterase substrate that is taken up by viable cells and hydrolyzed intracellularly, releasing a green fluorescent product. Briefly, 104 cells are plated per well in 96-well plates for each day of a 4-day time course. Various concentrations of PP2, A-419259 or vehicle control are added to the wells (five wells per concentration per day) and the plates are incubated at 37°C. At each time point, one plate is centrifuged at 1500 g for 10 min to pellet the cells. Cells are washed with phosphate buffered saline (PBS), and calcein-AM is added to each well to a final concentration of 1 μM. Plates are incubated in the dark at room temperature for 1 h. The plates are then read at 485/530 nm (excitation/emission) using a SpectraMax Gemini XS fluorescent plate reader and data are analysed with SoftMax Pro software[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
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取扱説明書 (2659 KB)
参考文献
[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
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| 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 |
A 419259 関連分類
HY-15764 関連分類
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