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Submit ReviewPF 06260933 dihydrochloride is a MAP4K4 (HGK) inhibitor (IC50 = 140 nM). Also inhibits MINK and TNIK (IC50 values are 8 and 13 nM, respectively). Improves fasting hyperglycemia in mice. Orally active.
Sold for research purposes under agreement from Pfizer Inc.
PF 06260933 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 369.68 |
公式 | C16H13ClN4.2HCl |
储存 | Desiccate at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 1883548-86-4 |
PubChem ID | 118701007 |
InChI Key | VRQXEOPUAQLBQI-UHFFFAOYSA-N |
Smiles | NC1=NC=C(C3=CN=C(N)C=C3)C=C1C2=CC=C(Cl)C=C2.Cl.Cl |
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 | |||
water | 36.97 | 100 | |
DMSO | 7.39 | 20 |
以下数据基于产品分子量 369.68。 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 | 2.71 mL | 13.53 mL | 27.05 mL |
5 mM | 0.54 mL | 2.71 mL | 5.41 mL |
10 mM | 0.27 mL | 1.35 mL | 2.71 mL |
50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
参考文献是支持产品生物活性的出版物。
Ammirati et al (2015) Discovery of an in vivo tool to establish proof-of-concept for MAP4K4-based antidiabetic treatment. ACS Med.Chem.Lett. 6 1128 PMID: 26617966
If you know of a relevant reference for PF 06260933 dihydrochloride, please let us know.
关键词: PF 06260933 dihydrochloride, PF 06260933 dihydrochloride supplier, PF06260933, dihydrochloride, MAP4K4, HGK, inhibitors, inhibits, antidiabetic, diabetes, MINK, TNIK, mitogen-activated, kinases, hepatocyte, germinal, pogenitor, kinase-like, center, kinase, Other, MAPK, Kinases, 5752, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PF 06260933 dihydrochloride 的部分引用包括:
Sebastian et al (2019) Development of MAP4 Kinase Inhibitors as Motor Neuron-Protecting Agents. Cell Chem Biol 26 1703-1715.e37 PMID: 31676236
Gao et al (2017) MAP4K4 is a novel MAPK/ERK pathway regulator required for lung adenocarcinoma maintenance. Mol Oncol 11 628 PMID: 28306189
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.