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Submit ReviewPF 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.
Sold for research purposes under agreement from Pfizer Inc.
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。
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 49.05 | 100 |
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.
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 |
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
If you know of a relevant reference for PF 04449913 maleate, please let us know.
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