UNC2025
作者：齐岳
发布时间：2023-08-22
09:28:12
点击数：
产品名称：UNC2025
产品描述：
| 产品描述 | 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. |
| 靶点活性 | FLT3:0.8 nM, Mer:0.74 nM |
| 体外活性 | 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] |
| 体内活性 | 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] |
| 别名 | UNC 2025, mrx-6313, UNC-2025 |
| 分子量 | 476.669 |
| 分子式 | C28H40N6O |
| CAS No. | 1429881-91-3 |
存储
| 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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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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