A 419259 trihydrochloride NEW
| Price | $48 | $109 | $179 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-08 |
Product Details
| Product Name: A 419259 trihydrochloride | CAS No.: 1435934-25-0 |
| Purity: 99.47% | Supply Ability: 10g |
| Release date: 2024/11/08 |
Product Introduction
Bioactivity
| 名稱(chēng) | A 419259 trihydrochloride |
| 描述 | A 419259 trihydrochloride (RK 20449 trihydrochloride) is an Src family kinases inhibitor (IC50s: 9 nM, 3 nM and 3 nM for Src, Lck and Lyn). |
| 細(xì)胞實(shí)驗(yàn) | 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, 10^4 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 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 fluorescent plate reader and data are analyzed with SoftMax Pro software [1]. |
| 激酶實(shí)驗(yàn) | 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 [1]. |
| 體外活性 | A-419259 inhibits K-562 cells (IC50: 0.1~0.3 μM), and Meg-01 proliferation (IC50: ~0.1 μM). A-419259 also potently induces apoptosis in K-562 cells beginning at 0.1 μM and increasing in a dose-dependent manner. PP2 inhibits Src kinase autophosphorylation in both Ph+ cell lines (K-562 and Meg-01) with an IC50 between 3 and 10 μM, while A-419259 blocks kinase activation between 0.1 and 0.3 μM. A-419259 strongly inhibits DAGM/Bcr-Abl cell proliferation in the absence of IL-3 (IC50: 0.1~0.3 μM) [1]. A-419259 inhibits overall SFK activity in K562 and other CML cell lines with an IC50 value of 0.1-0.3 μM [2]. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : ≥53 mg/mL (89.53 mM) |
| 關(guān)鍵字 | RK20449 Trihydrochloride | A 419259 | A 419259 trihydrochloride | RK 20449 | Src | RK-20449 | A-419259 Trihydrochloride | RK20449 | A419259 | RK-20449 Trihydrochloride | Inhibitor | RK 20449 Trihydrochloride | inhibit | A-419259 | A 419259 Trihydrochloride | A419259 Trihydrochloride |
| 相關(guān)產(chǎn)品 | Nintedanib | Vemurafenib | Staurosporine | Tandutinib | Ibrutinib | Dasatinib | Ponatinib | Pelitinib | Tofacitinib | Masitinib |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 激酶抑制劑庫(kù) | 酪氨酸激酶分子庫(kù) | 抗癌細(xì)胞代謝庫(kù) | 血管生成庫(kù) | 抑制劑庫(kù) | 已知活性化合物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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