C-11
目录号 : GC35574
C-11 是一种基于 tubulysin，用于抗体-药物偶联物 (ADCs) 的药物 -linker 连接物，对癌细胞具有细胞毒性。
Cas No.:2007965-97-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
C-11 is a tubulysin-based drug-linker conjugate for ADC, displays cytotoxicity for carcinoma cell lines[1].
C-11 exhibits cytotoxicity for N87 cells and MDA-MB-361-DYT2 cells with IC50s of 1.11 nM and 0.9 nM, respectively[1].
[1]. Leverett CA, et al. Design, Synthesis, and Cytotoxic Evaluation of Novel Tubulysin Analogues as ADC Payloads. ACS Med Chem Lett. 2016 Aug 26;7(11):999-1004.
| Cas No. | 2007965-97-9 | SDF | |
| Canonical SMILES | O=C(N(C)[C@@H](C(C)C)C[C@@H](OC(C)=O)C1=NC(C(N[C@@H](CC2=CC=C(N)C=C2)C[C@H](C)C(O)=O)=O)=CS1)[C@H]([C@@H](C)CC)NC([C@@]3(C)CCCN3C)=O | ||
| 分子式 | C38H58N6O7S | 分子量 | 742.97 |
| 溶解度 | Soluble in DMSO | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.3459 mL | 6.7297 mL | 13.4595 mL |
| 5 mM | 0.2692 mL | 1.3459 mL | 2.6919 mL |
| 10 mM | 0.1346 mL | 0.673 mL | 1.3459 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。
C-11 radiochemistry in cancer imaging applications
Curr Top Med Chem 2010;10(11):1060-95.PMID:20388115DOI:10.2174/156802610791384261.
Carbon-11 (C-11) radiotracers are widely used for the early diagnosis of cancer, monitoring therapeutic response to cancer treatment, and pharmacokinetic investigations of anticancer drugs. PET imaging permits non-invasive monitoring of metabolic processes and molecular targets, while carbon-11 radiotracers allow a "hot-for cold" substitution of biologically active molecules. Advances in organic synthetic chemistry and radiochemistry as well as improved automated techniques for radiosynthesis have encouraged investigators in developing carbon-11 tracers for use in oncology imaging studies. The short half-life of carbon-11 (20.38 minutes) creates special challenges for the synthesis of C-11 labeled tracers; these include the challenges of synthesizing C-11 target compounds with high radiochemical yield, high radiochemical purity and high specific activity in a short time and on a very small scale. The optimization of conditions for making a carbon-11 tracer include the late introduction of the C-11 isotope, the rapid formation and purification of the target compound, and the use of automated systems to afford a high yield of the target compound in a short time. In this review paper, we first briefly introduce some basic principles of PET imaging of cancer; we then discuss principles of carbon-11 radiochemistry, focus on specific advances in radiochemistry, and describe the synthesis of C-11 radiopharmaceuticals developed for cancer imaging. The carbon-11 radiochemistry approaches described include the N,O, and S-alkylations of [(11)C]methyl iodide/[(11)C]methyl triflate and analogues of [(11)C]methyl iodide and their applications for making carbon-11 tracers; we then address recent advances in exploring a transmetallic complex mediated [(11)C]carbonyl reaction for oncologic targets.
Diagnostic accuracy of C-11 choline and C-11 acetate for lymph node staging in patients with bladder cancer: a systematic review and meta-analysis
World J Urol 2018 Mar;36(3):331-340.PMID:29294164DOI:10.1007/s00345-017-2168-4.
Objective: We aimed to assess the diagnostic accuracy of C-11 choline and C-11 acetate positron emission tomography/computed tomography (PET/CT) for lymph node (LN) staging in bladder cancer (BC) patients through a systematic review and meta-analysis. Methods: The MEDLINE, EMBASE, and Cochrane Library database, from the earliest available date of indexing through June 30, 2017, were searched for studies evaluating the diagnostic performance of C-11 choline and C-11 acetate PET/CT for LN staging in BC. We determined the sensitivities and specificities across studies, calculated positive and negative likelihood ratios (LR+ and LR-), and constructed summary receiver operating characteristic curves. Results: Across 10 studies (282 patients), the pooled sensitivity was 0.66 (95% CI 0.54-0.75) without heterogeneity (χ2 = 12.4, p = 0.19) and a pooled specificity of 0.89 (95% CI 0.76-0.95) with heterogeneity (χ2 = 29.1, p = 0.00). Likelihood ratio (LR) syntheses gave an overall positive likelihood ratio (LR+) of 5.8 (95% CI 2.7-12.7) and negative likelihood ratio (LR-) of 0.39 (95% CI 0.28-0.53). The pooled diagnostic odds ratio (DOR) was 15 (95% CI 6-38). In meta-regression analysis, the study design (prospective vs retrospective) was the source of the study heterogeneity. Conclusion: C-11 choline and C-11 acetate PET/CT shows a low sensitivity and moderate specificity for the detection of metastatic LNs in patients with BC. Moreover, heterogeneity among the studies should be considered a limitation. Further large multicenter studies would be necessary to substantiate the diagnostic accuracy of C-11 choline and C-11 acetate PET/CT for this purpose.
C-11 methionine positron emission tomography scans improve the preoperative localization of pathologic parathyroid glands in primary hyperparathyroidism
Scand J Surg 2022 Jan-Mar;111(1):14574969211036837.PMID:34399632DOI:10.1177/14574969211036837.
Background and objective: Preoperative localization of pathologic parathyroid glands is essential in the preparation of a parathyroidectomy. We evaluated the use of a C-11 methionine positron emission tomography/computed tomography scan in a 7-year period in selected patients with primary hyperparathyroidism. The indications to perform a C-11 methionine positron emission tomography/computed tomography were either persistent primary hyperparathyroidism after parathyroidectomy or inconclusive preoperative localization on ultrasound and sestaMIBI. Methods: A group of 36 patients was referred for a C-11 methionine positron emission tomography/computed tomography. Biochemical data, pathology, and results of sestaMIBI were collected retrospectively. The primary hyperparathyroidism patients were divided into two groups. In group 1 (N = 17), the C-11 methionine positron emission tomography/computed tomography was performed before parathyroidectomy. In group 2 (N = 19), the C-11 methionine positron emission tomography/computed tomography was performed after unsuccessful parathyroidectomy and before a reoperation. Results: Overall, in 30 of the 36 patients (83%), C-11 methionine positron emission tomography/computed tomography identified a true-positive pathologic parathyroid gland confirmed by an experienced pathologist, consistent with a positive predictive value of 91%. In group 1, 94% of the patients (N = 16) had pathologic parathyroid tissue identified by C-11 methionine positron emission tomography/computed tomography. This resulted in a clinical benefit in 13 patients (76%). In group 2, the benefit was slightly lower, as 74% of the patients (N = 14) had a true-positive C-11 methionine positron emission tomography/computed tomography scan resulting in a clinical benefit in nine patients (47%). Conclusions: In two selected groups of patients planned for an initial operation or reoperation of primary hyperparathyroidism and inconclusive conventional imaging, we found C-11 methionine positron emission tomography/computed tomography to give parathyroid surgeons a clinical benefit in the majority of cases, electing the patients for unilateral surgery.
Radiosynthesis of 6-[C-11]-D-glucose
Appl Radiat Isot 1993 Dec;44(12):1449-58.PMID:8257963DOI:10.1016/0969-8043(93)90098-u.
Availability of 6-[C-11]-D-glucose will permit positron emission tomography (PET) investigations of glucose utilization derived from the pentose shunt which supports biosynthesis in tissues. The first radiosynthesis of 6-[C-11]-D-glucose is described. As much as 1 mCi of 6-[C-11]-D-glucose, sufficient for animal studies, is obtained from [C-11]CO2 after 100 min with a 16% radiochemical yield (EOB). The radiosynthesis has many attractive features. The method uses [C-11]CH3I and combines a Wittig reaction and a stereoselective OsO4 catalyzed alkene hydroxylation. The OsO4 hydroxylation of the [C-11]-labeled alkene (9) is accomplished in less than 10 min with high stereoselectivity (94:6) in favor of the 6-[C-11]-D-gluco-isomer. HPLC purification (C-18) of the protected labeled sugar removes the undesired 6-[C-11]-L-ido-sugar at an early stage and avoids the use of an expensive low-capacity ion-exchange HPLC column. OsO4, a highly toxic reagent, is removed in the process by adsorption and inactivation on polymer-bound triphenylphosphine.
C-11, a New Antiepileptic Drug Candidate: Evaluation of the Physicochemical Properties and Impact on the Protective Action of Selected Antiepileptic Drugs in the Mouse Maximal Electroshock-Induced Seizure Model
Molecules 2021 May 24;26(11):3144.PMID:34074008DOI:10.3390/molecules26113144.
C-11 is a hybrid compound derived from 2-(2,5-dioxopyrrolidin-1-yl) propanamide, with a wide spectrum of anticonvulsant activity and low neurotoxicity. The aim of this study was to determine the effects of C-11 on the protective action of various antiepileptic drugs (i.e., carbamazepine CBZ, lacosamide LCM, lamotrigine LTG, and valproate VPA) against maximal electroshock-induced seizures (MES) in mice, as well as its neuroprotective and physicochemical/pharmacokinetic properties. Results indicate that C-11 (30 mg/kg, i.p.) significantly enhanced the anticonvulsant action of LCM (p < 0.001) and VPA (p < 0.05) but not that of CBZ and LTG in the MES test. Neither C-11 (30 mg/kg) alone nor its combination with other anticonvulsant drugs (at their ED50 values from the MES test) affected motor coordination; skeletal muscular strength and long-term memory, as determined in the chimney; grip strength and passive avoidance tests, respectively. Pharmacokinetic characterization revealed that C-11 had no impact on total brain concentrations of LCM or VPA in mice. Qualitative analysis of neuroprotective properties of C-11, after a single administration of pilocarpine, revealed no protective effect of this substance in the tested animals. Determination of physicochemical descriptors showed that C-11 meets the drug-likeness requirements resulting from Lipinski and Veber's rules and prediction of gastrointestinal absorption and brain penetration, which is extremely important for the CNS-active compounds.