(E/Z)-Zotiraciclib NEW
| Price | $38 | $54 | $89 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-18 |
Product Details
| Product Name: (E/Z)-Zotiraciclib | CAS No.: 937270-47-8 |
| Purity: 99.12% | Supply Ability: 10g |
| Release date: 2024/11/18 |
Product Introduction
Bioactivity
| 名稱 | (E/Z)-Zotiraciclib |
| 描述 | (E/Z)-Zotiraciclib ((E/Z)-TG02) effectively inhibits CDK2, JAK2, and FLT3 with IC50s of 13 nM, 73 nM, and 56 nM, respectively. |
| 體外活性 | (E/Z)-Zotiraciclib has a highly novel kinase inhibitory spectrum inhibiting 17 kinases from a panel of 63, 11 of which are CDK/JAK/FLT family members. Human CYP1A2, 3A4, 2C9, and 2C19 isoforms are not inhibited by (E/Z)-Zotiraciclib at the highest tested concentration of 25 μM, but (E/Z)-Zotiraciclib inhibits CYP2D6 with an IC50 of 0.95 μM, approximately at the plasma Cmax?observed at the maximum tolerated dose. (E/Z)-Zotiraciclib inhibits cell proliferation concentrations in HCT-116 with an IC50 of 0.079 μM and HL-60 with an IC50 of 0.059 μM[1]. (E/Z)-Zotiraciclib is a novel small molecule potent CDK/JAK2/FLT3 inhibitor and mainly metabolized by CYP3A4 and CY1A2 in vitro[2]. |
| 體內活性 | Treatment with (E/Z)-Zotiraciclib (75 mg/kg p.o. q.d. 3×/week) significantly inhibits the growth of tumors with a mean TGI of 82%, while the lower dose(50 mg/kg p.o. 3×/week) is marginally effective. Treatment with (E/Z)-Zotiraciclib using either regime significantly inhibits the growth of tumors with mean TGIs of 42% and 63% for the oral and ip delivery methods, respectively[1]. In pharmacokinetic studies, (E/Z)-Zotiraciclib shows moderate to high systemic clearance (relative to liver blood flow), high volume of distribution (>0.6 L/kg), the oral bioavailability of 24%, ~4 and 37% in mice, rats, and dogs, respectively; and extensive tissue distribution in mice[2]. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 11 mg/mL (29.53 mM), Sonication is recommended. |
| 關鍵字 | multiple myeloma | JAK2 | Fms like tyrosine kinase 3 | Cyclin dependent kinase | JAK | FLT3 | (E/Z)-SB 1317 | Janus kinase | (E/Z)-Zotiraciclib | CD135 | leukemias | Inhibitor | (E/Z)-SB-1317 | CDK | CDK2 | Cluster of differentiation antigen 135 | inhibit | cancer | (E/Z) Zotiraciclib | (E/Z)Zotiraciclib |
| 相關產品 | Ribociclib | Gilteritinib | Nintedanib | Ruxolitinib | Sorafenib | Tofacitinib Citrate | Pexidartinib | Sorafenib tosylate | Ruxolitinib phosphate | CASIN | Sodium Oxamate | Abemaciclib |
| 相關庫 | 經典已知活性庫 | 酪氨酸激酶分子庫 | 激酶抑制劑庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 抗癌活性化合物庫 | 抗癌藥物庫 |
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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