AZD7507
产品名称:AZD7507
产品描述:
产品描述 | AZD7507 is a CSF-1R inhibitor with an IC50 of 32 nM. AZD7507 has antitumor activity. |
靶点活性 | CSF-1R:32 nM, hERG:>30 μM, NaV1.5:26 μM |
体外活性 | AZD7507 inhibits the proliferation of 3T3 cells engineered to express CSF-1R and stimulated with CSF-1. It shows inhibitory activity against hERG and NaV1.5, with IC50s of >30 and 26 μM[1]. |
体内活性 | Xenografted mice were given liposomal clodronate (Lipclod) to selectively deplete phagocytic macrophages; AZD7507 to inhibit the activation of CSF receptor 1 (CSFR1), thereby preventing monocyte differentiation into macrophages; or appropriate vehicle alone[2]. In Lipclod-, GW2580-, and AZD7507-treated mice, we observed a significant decrease the number of CD68+ macrophages in the xenografted. Mice with CC-LP-1 and SNU-1079, but not WITT-1, xenografts demonstrated both reduced tumor volume and mass after treatment with Lipclod, GW2580, and AZD7507. Furthermore, of the 8 SNU-1079 xenografts that were palpable at 3 weeks, only 4 from the GW2580 group and 6 from the AZD7507 group were large enough to recover at week 6, as they were no longer palpable and too small to detect. In the CC-LP-1 group, only 3 of the 8 tumors were detectable at 6 weeks. (In the WITT-1 line, 7 xenografts were recovered from the GW2580 and 8 from the AZD7507 group.) Depletion of macrophages using Lipclod, GW2580, or AZD7507 in all 3 xenografted lines resulted in a reduction in murine Wnt7b expression at the mRNA level[2]. |
分子量 | 454.5 |
分子式 | C23H27FN6O3 |
CAS No. | 1041852-85-0 |
存储
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 100 mg/mL (220.02 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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