Selpercatinib

Pricing Availability   Qty
说明: Potent and selective RET inhibitor
化学名: 6-(2-Hydroxy-2-methylpropoxy)-4-[6-[6-[(6-methoxy-3-pyridinyl)methyl]-3,6-diazabicyclo[3.1.1]hept-3-yl]-3-pyridinyl]pyrazolo[1,5-a]pyridine-3-carbonitrile
纯度: ≥98% (HPLC)
说明书
引用文献
评论

生物活性 for Selpercatinib

Selpercatinib, is a potent and selective receptor tyrosine kinase RET inhibitor (EC50 = 4 nM). It shows > 100-fold selectivity for > 95% of 228 purified kinase domains in radiometric assays. In vitro, it inhibits proliferation of cancer cell lines containing RET mutations or gene fusions. In vivo, it inhibits tumor growth in diverse RET mouse models. Selpercatinib is orally bioavailable.

化合物库 for Selpercatinib

Selpercatinib is also offered as part of the Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。

技术数据 for Selpercatinib

分子量 525.6
公式 C29H31N7O3
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2152628-33-4
PubChem ID 134436906
InChI Key XIIOFHFUYBLOLW-UHFFFAOYSA-N
Smiles N#CC=1C=NN2C=C(OCC(O)(C)C)C=C(C=3C=NC(=CC3)N4CC5N(CC6=CN=C(OC)C=C6)C(C4)C5)C12

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 Selpercatinib

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 10.51 20

制备储备液 for Selpercatinib

以下数据基于产品分子量 525.6。 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
0.2 mM 9.51 mL 47.56 mL 95.13 mL
1 mM 1.9 mL 9.51 mL 19.03 mL
2 mM 0.95 mL 4.76 mL 9.51 mL
10 mM 0.19 mL 0.95 mL 1.9 mL

Molarity Calculator

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Reconstitution Calculator

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Dilution Calculator

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参考文献 for Selpercatinib

参考文献是支持产品生物活性的出版物。

Subbiah et al (2018) Selective RET kinase inhibition for patients with RET-altered cancers. Ann.Oncol. 29 1869 PMID: 29912274

Brandhuber et al (2016) The development of LOXO-292, a potent, KDR/VEGFR2-sparing RET kinase inhibitor for treating patients with RET-dependent cancers. International Conference on Molecular Targets and Cancer Therapeutics


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关键词: Selpercatinib, Selpercatinib supplier, RET, tyrosine, kinases, selective, potent, inhibitors, inhibits, orally, bioavailable, Other, RTKs, 7696, Tocris Bioscience

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