受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C26H24ClN3O3.HCl |
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分子量 | 498.40 | CAS No. | 1353859-00-3 | |
Solubility (25°C)* | 体外 | DMSO | 50 mg/mL warmed with 50ºC water bath (100.32 mM) | |
Water | 5 mg/mL warmed with 50ºC water bath (10.03 mM) | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | CX-6258 HCl is a potent, orally efficacious pan-Pim kinase inhibitor with IC50 of 5 nM, 25 nM and 16 nM for Pim1, Pim2, and Pim3, respectively. |
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in vitro | CX-6258 shows antiproliferative activity against a panel of human cancer cell lines with IC50 of 0.02-3.7 μM, mostly sensitive to acute leukemia cell lines. Combinations of CX-6258 with doxorubicin (10:1 molar ratio) and CX-6258 with paclitaxel (100:1 molar ratio) produces synergistic cell killing with combination index (CI50) values equal to 0.4 and 0.56, respectively. CX-6258 causes dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively. [1] |
in vivo | CX-6258 exhibits dose dependent efficacy in suppressing tumor growth in mice carrying MV-4-11 xenografts, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI [1] |
キナーゼアッセイ | Pim activity assay | |
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Pim-1 and Pim-2 inhibitions are measured in radiometric assays using human recombinant Pim-1 at [ATP] = 30 μM (substrate RSRHSSYPAGT) and human recombinant Pim-2 at [ATP] = 5 μM (substrate RSRHSSYPAGT). The radiometric assay for Pim-3 uses RSRHSSYPAGT as a substrate in the presence of [ATP] = 155 μM. | ||
細胞アッセイ | 細胞株 | ALL, AML, CML, PML and MM cell lines |
濃度 | ~10 μM | |
反応時間 | 96 hours | |
実験の流れ | ||
動物実験 | 動物モデル | Acute myeloid leukemia xenografts MV-4-11 |
投薬量 | 100 mg/kg | |
投与方法 | Orally daily |
Oncogenic PKA signaling increases c-MYC protein expression through multiple targetable mechanisms [ Elife, 2023, 12e69521] | PubMed: 36692000 |
A Single-Cell Landscape of High-Grade Serous Ovarian Cancer [ Nat Med, 2020, 10.1038/s41591-020-0926-0] | PubMed: 32572264 |
Targeting codon 158 p53-mutant cancers via the induction of p53 acetylation. [ Nat Commun, 2020, 29;11(1):2086] | PubMed: 32350249 |
Anti-platelet Properties of Pim Kinase Inhibition Is Mediated Through Disruption of Thromboxane A2 Receptor Signalling [ Haematologica, 2020, 28;haematol.2019.223529] | PubMed: 32467143 |
Thioguanine Induces Apoptosis in Triple-Negative Breast Cancer by Regulating PI3K-AKT Pathway [ Front Oncol, 2020, 10:524922] | PubMed: 33194583 |
PIM1 inhibitor synergizes the anti-tumor effect of osimertinib via STAT3 dephosphorylation in EGFR-mutant non-small cell lung cancer. [ Ann Transl Med, 2020, 8(6):366] | PubMed: 32355810 |
Pan-PIM kinase inhibitors enhance Lenalidomide's anti-myeloma activity via cereblon-IKZF1/3 cascade [ Cancer Lett, 2019, 440-441:1-10] | PubMed: 30312729 |
Global survey of cell death mechanisms reveals metabolic regulation of ferroptosis [ Nat Chem Biol, 2016, 12(7):497-503] | PubMed: 27159577 |
Pim1 kinase regulates c-Kit gene translation. [An N, et al. Exp Hematol Oncol, 2016, 10.1186/s40164-016-0060-3] | PubMed: 28042518 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。