LY2835219 free base |
| Catalog No.GC11823 |
LY2835219 free base is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2nM and 10nM in cell-free assays, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1231929-97-7
Sample solution is provided at 25 µL, 10mM.
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LY2835219 free base is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2nM and 10nM in cell-free assays, respectively[1].
LY2835219 free base (0.001-10μM; 24h) inhibited p-Rb in a concentration-dependent manner, resulting in cell arrest in the G1 phase (2 N DNA content) and a decrease in cell number due to inhibition of proliferation. LY2835219 free base inhibits CDK4 and CDK6 with low nanomolar potency, inhibits Rb phosphorylation resulting in a G1 arrest and inhibition of proliferation, and its activity is specific for Rb-proficient cells[2]. LY2835219 free base (0.1, 0.2 and 0.4μM; 24h) potentiated the cytotoxicity of conventional chemotherapeutic agents in ABCB1 and ABCG2-overexpressing cells[3].
LY2835219 free base (50mg/kg; po; 56d) was effective and well tolerated in mice bearing Colo-205 xenograft tumors. After administration for up to 56days, there was no significant weight loss in mice and no significant tumor growth[2]. LY2835219 free base (45mg/kg; po; 14d) combined with RAD001 had a synergistic anti-tumor effect on HNSCC xenograft tumors[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.
| Cell experiment [1]: | |
Cell lines | Colo-205 colorectal cells |
Preparation Method | Colo-205 colorectal cells treated with LY2835219 free base (0.001-10μM) for 24h. |
Reaction Conditions | LY2835219 free base: 0.001-10μM; 24h |
Applications | LY2835219 free base treated with Colo-205 colorectal cells showed a concentration-dependent inhibition of p-Rb and a corresponding arrest of cells in G1 (2 N DNA content), resulting in a decreased number of cells due to inhibition of proliferation. |
| Animal experiment [2]: | |
Animal models | Colo-205 human xenograft tumor model |
Preparation Method | LY2835219 free base was formulated in 1 % hydroxyethyl cellulose + 0.1 % antifoam in 25mM PBS pH 2 and administered orally by gavage (final volume 0.2 mL) at the indicated dose and schedule. |
Dosage form | LY2835219 free base (50mg/kg; po; 56d) |
Applications | LY2835219 free base is effective and well tolerated when administered up to 56 days in Colo-205 human xenograft tumor mice without significant loss of body weight or tumor outgrowth. |
References: | |
| Cas No. | 1231929-97-7 | SDF | |
| Chemical Name | N-(5-((4-ethylpiperazin-1-yl)methyl)pyridin-2-yl)-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazol-6-yl)pyrimidin-2-amine | ||
| Canonical SMILES | CCN1CCN(CC2=CN=C(NC3=NC=C(F)C(C4=CC5=C(N=C(C)N5C(C)C)C(F)=C4)=N3)C=C2)CC1 | ||
| Formula | C27H32F2N8 | M.Wt | 506.59 |
| Solubility | ≥ 4.83 mg/mL in DMSO with ultrasonic and warming, ≥ 6.34 mg/mL in EtOH with gentle warming | Storage | 4°C, protect from light |
| 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 | 1.974 mL | 9.8699 mL | 19.7398 mL |
| 5 mM | 0.3948 mL | 1.974 mL | 3.948 mL |
| 10 mM | 0.1974 mL | 0.987 mL | 1.974 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >97.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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