CAS NO: | 1095173-27-5 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Glasdegib (PF-04449913) is a potent and orally bioavailablesmoothenedinhibitor. Glasdegib (PF-04449913) binds to humanSMO(amino acids 181-787) with anIC50of 4 nM[1]. | ||||||||||||||||
IC50& Target | IC50: 4 nM (Smo)[1] | ||||||||||||||||
体外研究 (In Vitro) | Glasdegib (PF-04449913) inhibits sonic hedgehog (Shh) stimulated luciferase expression in mouse embryonic fibroblasts with an IC50of 6.8 nM; and significantly reduces medulloblastoma growth in a Ptch1+/-p53+/-allograft model at doses that decreased murine Shh target gene expression. In stromal co-culture experiments, FACS analysis demonstrates a significant reduction in BC LSC by Glasdegib (PF-04449913) when compared with normal progenitors. Importantly, human BC LSC engrafted RAG2-/-γC-/-mice treated daily with Glasdegib (PF-04449913) compared with vehicle treated controls have a significant spleen weight reduction (p=0.006). This reduction in leukemic burden corresponded with decreased GLI2 protein expression, as determined by both nanoproteomic analysis of FACS purified human progenitors and GLI2 confocal fluorescence microscopic analysis of splenic sections[1]. | ||||||||||||||||
体内研究 (In Vivo) | Human BC LSC engrafted RAG2-/-γC-/-mice treated daily with Glasdegib (PF-04449913) compared with vehicle treated controls had a significant spleen weight reduction (p=0.006). When CD34+cord blood engrafted NSG mice are treated with Glasdegib (PF-04449913), the frequency of human CD45+cells, progenitors and both myeloid and lymphoid cell fate commitment remained comparable to vehicle treated controls indicating that unlike LSC, normal human HSC cell fate decisions are Hh pathway independent. These results highlight the important niche dependent effects of selective SMO inhibition that induce GLI2 downregulation in a cell type and context specific manner[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 374.44 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C21H22N6O | ||||||||||||||||
CAS 号 | 1095173-27-5 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : ≥ 83.33 mg/mL(222.55 mM) *"≥" means soluble, but saturation unknown. 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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