Lerociclib dihydrochloride NEW
| Price | $31 | $44 | $72 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-18 |
Product Details
| Product Name: Lerociclib dihydrochloride | CAS No.: 2097938-59-3 |
| Purity: 97.40% | Supply Ability: 10g |
| Release date: 2024/11/18 |
Product Introduction
Bioactivity
| 名稱 | Lerociclib dihydrochloride |
| 描述 | Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective CDK4/CDK6 inhibitor, with IC50 values of 2 nM for CDK6/CyclinD3 and 1 nM for CDK4/CyclinD1. |
| 體外活性 | Lerociclib robustly induces sustained G1 arrest in CDK4/6 dependent cells with an EC50 of ~20 nM. A dose-dependent increase in G1 phase is observed when CDK4/6 dependent WM2664 cells are treated with G1T38 for 24 hours, maintaining this arrest up to 300 nM. WM2664 cells exhibit complete inhibition of RB phosphorylation at 30-1000 nM of Lerociclib for 24 hours compared to vehicle controls. G1T38 reduces RB phosphorylation within 1 hour post-treatment, reaching near-complete inhibition by 16 hours. G1T38 robustly inhibits proliferation in various tumor cell lines, including breast, melanoma, leukemia, and lymphoma, with EC50s as low as 23 nM. Within the CDK family, Lerociclib is least selective against CDK9/cyclin T, showing ~30-fold selectivity between CDK4/cyclin D1 and CDK9/cyclin T at the biochemical IC50. |
| 體內(nèi)活性 | In this HER2+ breast cancer model, Mice treated with Lerociclib elicits 8% tumor regression after 21 days of treatment while control animals have a 577% increase in tumor burden over the same treatment period.Compared to the vehicle-treated mice, daily treatment with 100 mg/kg of Lerociclib or palbociclib shows tumor regression within 10 days in the MCF7 xenograft model.After 27 days of treatment, tumor growth inhibition is observed in the 10, 50, and 100 mg/kg Lerociclib cohorts (approximately 12%, 74%, and 90% inhibition, respectively).Daily oral palbociclib treatment causes an 18%, 66%, and 87% tumor growth inhibition in the 10, 50, and 100 mg/kg dosage cohorts, respectively. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 1 mg/mL, Sonication is recommended. H2O : 4 mg/mL (7.31 mM), Sonication is recommended. |
| 關(guān)鍵字 | Inhibitor | G1T38 Dihydrochloride | Lerociclib Dihydrochloride | Lerociclib dihydrochloride | inhibit | G1T38 | CDK | Lerociclib | Cyclin dependent kinase |
| 相關(guān)產(chǎn)品 | Ribociclib | Ro-3306 | GSK 3 Inhibitor IX | Rafoxanide | Palbociclib monohydrochloride | CASIN | Palbociclib | GW 441756 | Sodium Oxamate | Abemaciclib | Dinaciclib | Abemaciclib methanesulfonate |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 激酶抑制劑庫(kù) | 抗癌臨床化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抑制劑庫(kù) | NO PAINS 化合物庫(kù) | 抗衰老化合物庫(kù) | 已知活性化合物庫(kù) | 抗癌藥物庫(kù) | 抗癌活性化合物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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