| Bioactivity | 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[1][2]. |
| Target | IC50: 9 nM (Src), <3 nM (Lck), <3 nM (Lyn), 3 μM (Abl) |
| Invitro | A419259 是第二代吡咯并嘧啶，可阻断 CML 细胞系的增殖并诱导细胞凋亡。它 诱导 K-562 细胞凋亡，还抑制 Meg-01 增殖 (IC50=0.1 μM)[1]。在没有 IL-3 的情况下，A-419259 会强烈抑制 DAGM/Bcr-Abl 细胞增殖 (IC50=0.1-0.3 μM)[1]。A-419259 还抑制 CML 细胞系中的整体 SFK 活性，可阻断Src 激酶激活 (IC50=0.1-0.3 μM)[1]。A 419259 GMP (1 μM；16 h) 抑制内源 SFK (c-Src 和 Lck) 活性，从而抑制 Src 的驱动 mES 细胞向原始外胚层样细胞分化[2]。 A 419259 GMP (0.3, 1 μM；5 天) 对 mTeSR 培养基中生长的 hES 细胞的未分化集落形态没有影响[2]。 0 --> A 419259 相关抗体: |
| Name | A 419259 |
| CAS | 364042-47-7 |
| Formula | C29H34N6O |
| Molar Mass | 482.62 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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]. 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. |