PF 04449913 maleate

Pricing Availability   Qty
说明: Potent Smo antagonist
别名: glasdegib,PF-913
化学名: 1-((2R,4R)-2-(1H-Benzimidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate salt
纯度: ≥98% (HPLC)
说明书
引用文献
评论
文献 (1)

生物活性 for PF 04449913 maleate

PF 04449913 maleate is a potent Smo antagonist (IC50 = 5 nM). Attenuates the leukemia-initiation potential of AML cells in a serial transplantation mouse model. Also eliminates self-propagation capacity of AML cells.

许可信息

Sold for research purposes under agreement from Pfizer Inc.

化合物库 for PF 04449913 maleate

PF 04449913 maleate is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen FDA-Approved Drugs and Tocriscreen Stem Cell Library. 了解 Tocris 化合物库的更多信息。

技术数据 for PF 04449913 maleate

分子量 490.51
公式 C21H22N6O.C4H4O4
储存 Store at +4°C
纯度 ≥98% (HPLC)
CAS Number 2030410-25-2
PubChem ID 122640033
InChI Key VJCVKWFBWAVYOC-UIXXXISESA-N
Smiles OC(/C=C\C(O)=O)=O.CN1CC[C@@H](NC(NC2=CC=C(C#N)C=C2)=O)C[C@@H]1C3=NC4=CC=CC=C4N3

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for PF 04449913 maleate

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 49.05 100

制备储备液 for PF 04449913 maleate

以下数据基于产品分子量 490.51。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.04 mL 10.19 mL 20.39 mL
5 mM 0.41 mL 2.04 mL 4.08 mL
10 mM 0.2 mL 1.02 mL 2.04 mL
50 mM 0.04 mL 0.2 mL 0.41 mL

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产品说明书 for PF 04449913 maleate

参考文献 for PF 04449913 maleate

参考文献是支持产品生物活性的出版物。

Munchhof et al (2011) Discovery of PF-04449913, a potent and orally bioavailable inhibitor of smoothened. ACS Med.Chem.Lett. 3 106 PMID: 24900436

Fukushima et al (2016) Small-molecule Hedgehog inhibitor attenuates the leukemia-initiation potential of acute myeloid leukemia cells. Cancer Sci. 107 1422 PMID: 27461445

Giordani et al (2016) The human Smoothened inhibitor PF-04449913 induces exit from quiescence and loss of multipotent Drosophila hematopoietic progenitor cells. Oncotarget 7 55313 PMID: 27486815


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