UNC2025
作者：齊岳
發(fā)布時間：2023-08-22
09:28:12
點擊數(shù)：
產品名稱：UNC2025
產品描述：
| 產品描述 | UNC-2025（ IC50 of 0.74 nM and 0.8 nM） is a potent and orally bioavailable dual MER/FLT3 inhibitor. UNC-2025 is about 20-fold selectivity higher than Axl and Tyro3. |
| 靶點活性 | FLT3:0.8 nM, Mer:0.74 nM |
| 體外活性 | In 697 B-ALL cells, UNC-2025 potently inhibits Mer phosphorylation with IC50 of 2.7 nM. In A549 NSCLC and Molm-14 AML cell lines, UNC-2025 causes significant inhibition of colony formation dependent on Mer8 and Flt3. [1] In H2228 and H1299 cell lines, UNC-2025 inhibits MERTK oncogenic signaling downstream, such as basal and stimulated pAKT and pERK1/2. In four NSCLC cell lines, UNC-2025 also induces apoptotic cell death, and decreases colony formation. [2] |
| 體內活性 | In mice bearing 697 acute leukemia tumors, UNC-2025 (3 mg/kg, p.o.) shows good solubility and DMPK properties, and results in effective target inhibition. [1] In mice bearing H2228 or A549 tumors, UNC-2025 (50 mg/kg, p.o.) inhibits tumor growth. [2] |
| 別名 | UNC 2025, mrx-6313, UNC-2025 |
| 分子量 | 476.669 |
| 分子式 | C28H40N6O |
| CAS No. | 1429881-91-3 |
存儲
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: 100 mg/mL (194.88 mM)
Ethanol: 8 mg/mL(15.59 mM),warming
DMSO: 25 mg/mL(48.72 mM),warming
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業(yè)務范圍包括化學試劑和產品的研發(fā)、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學品、中間體和化工材料等領域。
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