Ribociclib (LEE011)
製品コードS7440
分子量(MW)：434.54
Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor. Phase 3.
カスタマーフィードバック(4)
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IB analysis of whole cell lysates derived from mouse CT26 or 4T1 tumor cell lines treated with or without the CDK4/6 inhibitor, ribociclib.
Nature, 2017, 553(7686):91-95. Ribociclib (LEE011) purchased from Selleck.
The effects of the CDK inhibitor abemaciclib, palbociclib, and ribociclib on Trop2 ICD cleavage. CDK inhibitors decreased Trop2 ICD abundance after the second day of CDK inhibitor treatment.
Cancer Res, 2016, 76(22):6723-6734. Ribociclib (LEE011) purchased from Selleck.
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(B) The effects of AZD2014, BEZ235, lapatinib, LEE011, pazopanib on PI3K/AKT signaling in sarcoma PDC line were determined by immunoblotting analysis. Cells were treated with 1 μM of the indicated drugs for 72 h.
Transl Oncol, 2016, 9(3):197-202.. Ribociclib (LEE011) purchased from Selleck.
Analysis of apoptosis in leukemia cells induced by LEE011. Annexin V staining of cells following 48-h treatment with LEE011 at 2 or 5 µM compared with DMSO controls. Following 5-µM LEE011 treatment, the K562 apoptotic cell percentage was 5.9 ± 0.75 vs. 1.2 ± 0.66% for the DMSO group, P = 0.001; in MV4-11 cells, the apoptotic cell percentage was 24.2 ± 3.06 vs. 0.53 ± 0.40% for the DMSO group, P = 0.005; in U937 cells, the apoptotic cell percentage was 9.9 ± 2.81 vs. 0.57 ± 0.42% for the DMSO group, P = 0.027; in HL-60 cells, the apoptotic cell percentage was 28.23 ± 6.01 vs. 0.9 ± 0.8% for the DMSO group, P = 0.015; in THP-1 cells, the apoptotic cell percentage was 1.76 ± 0.4 vs. 1.56 ± 0.45% for the DMSO group, P = 0.59; in CCRF cells, the apoptotic cell percentage was 13.77 ± 3.16 vs. 1.2 ± 0.36% for the DMSO group, P = 0.019; in NB4 cells, the apoptotic cell percentage was 12.1 ± 1.35 vs. 0.86 ± 0.25% for the DMSO group, P = 0.004; and in SHI-1 cells the apoptotic cell percentage was 12.6 ± 2.81 vs. 1.87 ± 0.75% for the DMSO group, P = 0.017. These analyses were repeated three times. *P < 0.05; **P < 0.01
Cancer Cell Int, 2017, 17:35. Ribociclib (LEE011) purchased from Selleck.
製品安全説明書
CDK阻害剤の選択性比較
生物活性
| 製品説明 | Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor. Phase 3. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 特性 | Orally bioavailable CDK4/6-selective inhibitor that has been tested in Phase III clinical trials for treatment of advanced breast cancer. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| ターゲット |
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| 体外試験 |
LEE011, as dual CDK4/CDK6 inhibitor, significantly inhibits the growth of 12 of 17 neuroblastoma cell lines with mean IC50 of 307 nM. The growth inhibition of neuroblastoma cell lines is primarily cytostatic and is mediated by a G1 cell-cycle arrest and cellular senescence. [1] |
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| 細胞データ |
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| 体内試験 | LEE011 (200 mg/kg daily, p.o.) significantly causes tumor growth delay in mice harboring the BE2C or 1643 xenografts with no weight loss or other signs of toxicity. [1] |
お薦めの試験操作（参考用のみ）
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| 動物試験： |
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溶解度 (25°C)
| 体外 | DMSO | 7 mg/mL (16.1 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble |
* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。
化学情報
| 分子量 | 434.54 |
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| 化学式 | C23H30N8O |
| CAS No. | 1211441-98-3 |
| 保管 | 粉 |
| in solvent | |
| 別名 | N/A |
便利ツール
モル濃度計算器
求めたい質量、体積または濃度を計算してください。
質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)
モル濃度計算器方程式
*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA（製品ページで利用可能な）。
希釈計算器
貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます：
開始濃度 x 開始体積 = 最終濃度 x 最終体積
希釈の計算式
この方程式は、一般に略語を使われます：C1V1 = C2V2 ( 入力 出力 )
常に貯蔵液を準備するとき、小びんラベルとMSDS/COA（オンラインで利用できる）で見つかる製品のバッチに特有の分子量を使ってください。
分子量计算器
そのモル質量と元素組成を計算するために、合成物の化学式を入力してください：
チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2
モル濃度計算器
臨床試験
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02657343 | Recruiting | Breast Cancer | Dana-Farber Cancer Institute|Novartis | March 9 2016 | Phase 1|Phase 2 |
| NCT02422615 | Active not recruiting | Breast Neoplasms|Breast Diseases|Neoplasms|Neoplasms by Site|Fulvestrant|Antineoplastic Agents|Antineoplastic Agents Hormonal|Estrogen Receptor Antagonists|Hormone Antagonists|Hormones Hormone Substitutes and Hormone Antagonists|Molecular Mechanisms of Pharmacological Action|Pharmacologic Actions|Therapeutic Use | Novartis Pharmaceuticals|Novartis | June 9 2015 | Phase 3 |
| NCT03114527 | Recruiting | Soft Tissue Sarcoma | Fox Chase Cancer Center | August 8 2017 | Phase 2 |
| NCT02657928 | Active not recruiting | Estrogen Receptor Positive|Postmenopausal|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Recurrent Uterine Corpus Carcinoma | Mayo Clinic|National Cancer Institute (NCI) | July 8 2016 | Phase 2 |
| NCT01857193 | Active not recruiting | Breast Cancer | Novartis Pharmaceuticals|Novartis | September 6 2013 | Phase 1 |
| NCT03434262 | Recruiting | Anaplastic Astrocytoma|Anaplastic Ependymoma|Anaplastic Ganglioglioma|Anaplastic Meningioma|Anaplastic Oligodendroglioma|Pleomorphic Xanthoastrocytoma Anaplastic|Atypical Teratoid/Rhabdoid Tumor|Brain Cancer|Brain Tumor|Central Nervous System Neoplasms|Choroid Plexus Carcinoma|CNS Embryonal Tumor With Rhabdoid Features|Ganglioneuroblastoma of Central Nervous System|CNS Tumor|Embryonal Tumor of CNS|Ependymoma|Glioblastoma|Glioma|Glioma Malignant|Medulloblastoma|Medulloblastoma; Unspecified Site|Medulloepithelioma|Neuroepithelial Tumor|Neoplasms|Neoplasms Neuroepithelial|Papillary Tumor of the Pineal Region (High-grade Only)|Pediatric Brain Tumor|Pineal Parenchymal Tumor of Intermediate Differentiation (High-grade Only)|Pineoblastoma|Primitive Neuroectodermal Tumor|Recurrent Medulloblastoma|Refractory Brain Tumor|Neuroblastoma. CNS|Glioblastoma IDH-mutant|Glioblastoma IDH-wildtype|Medulloblastoma Group 3|Medulloblastoma Group 4|Glioma High Grade|Neuroepithelial Tumor High Grade|Medulloblastoma SHH-activated and TP53 Mutant|Medulloblastoma SHH-activated and TP53 Wildtype|Medulloblastoma Chromosome 9q Loss|Medulloblastoma Non-WNT Non-SHH NOS|Medulloblastoma Non-WNT/Non-SHH|Medulloblastoma PTCH1 Mutation|Medulloblastoma WNT-activated|Ependymoma Recurrent|Glioma Recurrent High Grade|Glioma Recurrent Malignant|Embryonal Tumor NOS|Glioma Diffuse Midline H3K27M-mutant|Embryonal Tumor With Multilayered Rosettes (ETMR)|Ependymoma NOS WHO Grade III|Ependymoma NOS WHO Grade II|Medulloblastoma G3/G4|Ependymoma RELA Fusion Positive | St. Jude Children''s Research Hospital|Novartis Pharmaceuticals | March 5 2018 | Phase 1 |
技術サポート
ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。
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