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首页-小分子抑制剂&激动剂-Wnt/Notch/Hedgehog-Smoothened (Smo)-Glasdegib
Glasdegib

Chemical Structure : Glasdegib

CAS No.: 1095173-27-5

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Glasdegib (PF-04449913;PF04449913)

货号: PC-36044Not For Human Use, Lab Use Only.

Glasdegib (PF-04449913) is a potent, orally bioavailable smoothened (SMO) inhibitor with IC50 of 5 nM in the Gli-luciferase reporter assays, binds to human SMO (AA181-787) with IC50 of 4 nM.

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10 mg ￥1980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Glasdegib (PF-04449913) is a potent, orally bioavailable smoothened (SMO) inhibitor with IC50 of 5 nM in the Gli-luciferase reporter assays, binds to human SMO (AA181-787) with IC50 of 4 nM.
Glasdegib (PF-04449913) inhibits sonic hedgehog (Shh) stimulated luciferase expression in mouse embryonic fibroblasts with an IC50 of 6.8 nM, significantly reduces medulloblastoma growth in a Ptch1+/-p53+/- allograft model at doses that decreased murine Shh target gene expression.
Glasdegib (PF-04449913) reduced downstream GLI2 protein and cell cycle regulatory gene expression in humanized stromal co-cultures and LSC (leukemia stem cells) xenografts.

物理化学性质&存储条件

分子量 374.448
分子式 C21H22N6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea

参考文献

1. Munchhof MJ, et al. ACS Med Chem Lett. 2011 Dec 21;3(2):106-11.

2. Wagner AJ, et al. Clin Cancer Res. 2015 Mar 1;21(5):1044-51.

3. Sadarangani A, et al. J Transl Med. 2015 Mar 21;13:98.

4. Martinelli G, et al. Lancet Haematol. 2015 Aug;2(8):e339-46.

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