Tyrosine kinase inhibitor
目录号 : GC37849
本产品为酪氨酸激酶抑制剂。
Cas No.:1021950-26-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
A Tyrosine kinase inhibitor.
[1]. Inoue T, et al. Two cases of gastrointestinal perforation after radiotherapy in patients receiving tyrosine kinase inhibitor for advanced renal cell carcinoma. World J Surg Oncol. 2012 Aug 20;10(1):167. [2]. Bowen JM, et al. Development of a rat model of oral small molecule receptor tyrosine kinase inhibitor-induced diarrhea. Cancer Biol Ther. 2012 Nov 1;13(13). [3]. Sun FK, et al. Multi-targeted tyrosine kinase inhibitor sunitinib: a novel strategy for sporadic malignant pheochromocytoma. Chin Med J (Engl). 2012 Jun;125(12):2231-4. [4]. Thamm DH. Tyrosine kinase inhibitor special issue. Vet Comp Oncol. 2012 Sep;10(3):161-2. doi: 10.1111/j.1476-5829.2012.00339.x. [5]. Eriksson A, et al. The novel tyrosine kinase inhibitor AKN-028 has significant antileukemic activity in cell lines and primary cultures of acute myeloid leukemia. Blood Cancer J. 2012 Aug 3;2:e81. doi: 10.1038/bcj.2012.28.
| Cas No. | 1021950-26-4 | SDF | |
| Canonical SMILES | O=C(NC1=CC=C(C=C1)F)C2(CC2)C(NC3=CC=C(C=C3)OC4=C5C(NC(C(NCCN6CCOCC6)=O)=C5)=NC=C4)=O | ||
| 分子式 | C31H31FN6O5 | 分子量 | 586.61 |
| 溶解度 | DMSO: ≥ 46 mg/mL (78.42 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7047 mL | 8.5236 mL | 17.0471 mL |
| 5 mM | 0.3409 mL | 1.7047 mL | 3.4094 mL |
| 10 mM | 0.1705 mL | 0.8524 mL | 1.7047 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Anlotinib: a novel multi-targeting Tyrosine kinase inhibitor in clinical development
J Hematol Oncol 2018 Sep 19;11(1):120.PMID:30231931DOI:10.1186/s13045-018-0664-7.
Anlotinib is a new, orally administered Tyrosine kinase inhibitor that targets vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR), platelet-derived growth factor receptors (PDGFR), and c-kit. Compared to the effect of placebo, it improved both progression-free survival (PFS) and overall survival (OS) in a phase III trial in patients with advanced non-small-cell lung cancer (NSCLC), despite progression of the cancer after two lines of prior treatments. Recently, the China Food and Drug Administration (CFDA) approved single agent anlotinib as a third-line treatment for patients with advanced NSCLC. Moreover, a randomized phase IIB trial demonstrated that anlotinib significantly prolonged the median PFS in patients with advanced soft tissue sarcoma (STS). Anlotinib also showed promising efficacy in patients with advanced medullary thyroid carcinoma and metastatic renal cell carcinoma (mRCC). The tolerability profile of anlotinib is similar to that of other tyrosine kinase inhibitors that target VEGFR and other tyrosine kinase-mediated pathways; however, anlotinib has a significantly lower incidence of grade 3 or higher side effects compared to that of sunitinib. We review the rationale, clinical evidence, and future perspectives of anlotinib for the treatment of multiple cancers.
CD70 is a therapeutic target upregulated in EMT-associated EGFR Tyrosine kinase inhibitor resistance
Cancer Cell 2023 Feb 13;41(2):340-355.e6.PMID:36787696DOI:10.1016/j.ccell.2023.01.007.
Effective therapeutic strategies are needed for non-small cell lung cancer (NSCLC) patients with epidermal growth factor receptor (EGFR) mutations that acquire resistance to EGFR tyrosine kinase inhibitors (TKIs) mediated by epithelial-to-mesenchymal transition (EMT). We investigate cell surface proteins that could be targeted by antibody-based or adoptive cell therapy approaches and identify CD70 as being highly upregulated in EMT-associated resistance. Moreover, CD70 upregulation is an early event in the evolution of resistance and occurs in drug-tolerant persister cells (DTPCs). CD70 promotes cell survival and invasiveness, and stimulation of CD70 triggers signal transduction pathways known to be re-activated with acquired TKI resistance. Anti-CD70 antibody drug conjugates (ADCs) and CD70-targeting chimeric antigen receptor (CAR) T cell and CAR NK cells show potent activity against EGFR TKI-resistant cells and DTPCs. These results identify CD70 as a therapeutic target for EGFR mutant tumors with acquired EGFR TKI resistance that merits clinical investigation.
Tyrosine kinase inhibitor nilotinib induced palmoplantar erythrodysesthesia: A rare case
J Oncol Pharm Pract 2022 Apr;28(3):763-765.PMID:35465793DOI:10.1177/10781552211072465.
Introduction: Nilotinib is a second generation Tyrosine kinase inhibitor (TKI) used in the treatment of Chronic Myeloid Leukemia (CML). The development of tyrosine kinase inhibitors has transformed chronic phase chronic myeloid leukemia from a disease with a poor prognosis to a treatable chronic disease. Long-term treatment with tyrosine kinase inhibitors means that patients must be clinically managed and monitored for years. While under Nilotinib tretament, the development of palmoplantar erythrodyesthesia is a very rare condition compared to other oncological drugs. Case report: A 66-year-old male patient, who was diagnosed with chronic phase CML in 2019 had been placed under imatinib treatment . He had major molecular response loss in 2021, and was started on second generation TKI nilotinib 2 × 400mg/day, considering his comorbidities. We present a case of a 66-year-old patient with CML who developed palmoplantar erythrodysesthesia on the 21st day starting nilotinib treatment. Conclusion: It is important to manage the side effects that develop in long-term treatments. Adverse events can have a negative impact on patient compliance and quality of life and lead to poor clinical outcomes Our case is the first to develop PPE after beginning nilotinib use. We present this phenomenon to raise awareness and ignite a review of management strategies.In this case, we wanted to emphasize the importance of managing side effects.
Cardiovascular safety of the Tyrosine kinase inhibitor nintedanib
Br J Clin Pharmacol 2021 Oct;87(10):3690-3698.PMID:33620103DOI:10.1111/bcp.14793.
The intracellular Tyrosine kinase inhibitor nintedanib has shown great efficacy for the treatment of idiopathic pulmonary fibrosis (IPF) and other interstitial lung diseases. However, the incidence rate of myocardial infarction (MI) among participants in landmark IPF trials was remarkable, peaking at 3/100 patient-years. Although subjects with IPF often have a high cardiovascular (CV) risk profile, the occurrence of MI in nintedanib-treated patients may not be fully explained by clustering of CV risk factors. Nintedanib inhibits the vascular endothelial growth factor, platelet-derived growth factor and fibroblast growth factor pathways, which play important roles in the biology of the atherosclerotic plaque and in the response of the heart to ischaemia. Hence, unwanted CV effects may partly account for nintedanib-related MI. We review the evidence supporting this hypothesis and discuss possible actions for a safe implementation of nintedanib in clinical practice, building on the experience with tyrosine kinase inhibitors acquired in cardio-oncology.
Tyrosine kinase inhibitor therapy in chronic myeloid leukemia: update on key adverse events
Expert Rev Hematol 2015 Aug;8(4):457-79.PMID:25938861DOI:10.1586/17474086.2015.1041910.
Current treatment recommendations for chronic myeloid leukemia (CML) are guided by results from multiple clinical trials involving tyrosine kinase inhibitors that target BCR-ABL1. Consideration of the unique clinical benefits and potential risks associated with each Tyrosine kinase inhibitor approved for the treatment of CML is crucial for physicians when recommending the most appropriate therapy for each patient. Monitoring for and prompt management of adverse events may increase adherence to therapy and optimize patient outcomes. Here we provide an overview of the efficacy and safety of tyrosine kinase inhibitors approved for the treatment of CML, as well as recommendations for the management of key adverse events reported with these agents in clinical trials involving patients with CML.