LY2835219 (Synonyms: Abemaciclib; LY2835219 methanesulfonate) |
| Catalog No.GC16822 |
LY2835219는 CDK4와 CDK6의 강력하고 선택적인 억제제로 세포무한 실험에서 CDK4와 CDK6에 대한 IC50가 각각 2nM과 10nM이다.
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Cas No.: 1231930-82-7
Sample solution is provided at 25 µL, 10mM.
LY2835219는 CDK4와 CDK6의 강력하고 선택적인 억제제로 세포무한 실험에서 CDK4와 CDK6에 대한 IC50가 각각 2nM과 10nM이다.
LY2835219 (0.001-10μM; 24시간)는 농도 의존적으로 p-Rb를 억제하고 세포가 G1단계(2N DNA 함량)에서 중단되고 증식 억제로 인한 세포 수가 감소한다. LY2835219는 낮은 나노몰 강도로 CDK4와 CDK6을 억제하고 Rb인산화를 억제하여 G1 중단과 증식 억제를 유발하고 그 활동은 Rb 기능이 정상인 세포에 특이적이다[2]. LY2835219 (0.1, 0.2, 0.4μM; 24시간)는 ABCB1과 ABCG2 과표현 세포에서 전통 화학요법제의 세포 독성을 증강시킨다[3].
LY2835219 (50mg/kg; 구강 투여; 56일)은 Colo-205 이종 이식 종양을 가진 쥐에서 효과적이고 잘 견디어냈다. 최대 56일 동안 투여 후 쥐의 체중 감소가 없었고 종양 성장도 눈에 띄지 않았다[2]. LY2835219 (45mg/kg; 구강 투여; 14일)는 RAD001과 함께 HNSCC 이종 이식 종양에 대한 시너지적인 항종양 효과를 보였다[4].
References:
[1].Corona SP, Generali D. Abemaciclib: a CDK4/6 inhibitor for the treatment of HR+/HER2- advanced breast cancer. Drug Des Devel Ther. 2018 Feb 16;12:321-330.
[2]. Gelbert LM, Cai S, Lin X, Sanchez-Martinez C, Del Prado M, Lallena MJ, Torres R, Ajamie RT, Wishart GN, Flack RS, Neubauer BL, Young J, Chan EM, Iversen P, Cronier D, Kreklau E, de Dios A. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine. Invest New Drugs. 2014 Oct;32(5):825-37.
[3]Wu T, Chen Z, To KKW, Fang X, Wang F, Cheng B, Fu L. Effect of abemaciclib (LY2835219) on enhancement of chemotherapeutic agents in ABCB1 and ABCG2 overexpressing cells in vitro and in vivo. Biochem Pharmacol. 2017 Jan 15;124:29-42.
[4]. Ku BM, Yi SY, Koh J, Bae YH, Sun JM, Lee SH, Ahn JS, Park K, Ahn MJ. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma. Oncotarget. 2016 Mar 22;7(12):14803-13.
| 세포 실험 [1]: | |
세포 라인 | Colo-205 대장암 세포 |
제조 방법 | Colo-205 대장암 세포는 LY2835219 (0.001-10μM)으로 24시간 동안 처리합니다. |
반응 조건 | LY2835219: 0.001-10μM; 24시간 동안 |
응용 분야 | LY2835219로 처리된 Colo-205 대장암 세포에서 p-Rb에 대한 농도 의존성 억제가 관찰되었고 G1 단계(2N DNA 함량)에서의 세포 중단에 해당되고 증식 억제로 인해 세포 수가 감소했습니다. |
| 동물 실험 [2]: | |
동물 모형 | Colo-205 인간 이중 이식 중양 모델 |
제조 방법 | LY2835219는 1% hydroxyethyl cellulose + 0.1% 항포인 25mM PBS pH 2에 구성되어 구강 투여 방식(최종량 0.2 mL)으로 지정된 용량과 일정에 따라 투여되었습니다. |
제형 | LY2835219 (50mg/kg; po; 56일 동안) |
응용 분야 | Colo-205 인간 이종 이식 종양 쥐에서 최대 56일 동안 투여했을 때 LY2835219는 효과적이고 잘 견디어냈고 체중의 현저한 감소나 종양의 과도한 성장이 없었습니다. |
References: | |
| Cas No. | 1231930-82-7 | SDF | |
| Synonyms | Abemaciclib; LY2835219 methanesulfonate | ||
| Chemical Name | N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine;methanesulfonic acid | ||
| Canonical SMILES | CCN1CCN(CC1)CC2=CN=C(C=C2)NC3=NC=C(C(=N3)C4=CC5=C(C(=C4)F)N=C(N5C(C)C)C)F.CS(=O)(=O)O | ||
| Formula | C27H32F2N8.CH4O3S | M.Wt | 602.7 |
| Solubility | ≥ 30.15mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.6592 mL | 8.296 mL | 16.592 mL |
| 5 mM | 331.8 μL | 1.6592 mL | 3.3184 mL |
| 10 mM | 165.9 μL | 829.6 μL | 1.6592 mL |
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- Purity: >99.00%
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Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)
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