Pasireotide (aspartate)
目录号 : GC44571
A somatostatin receptor agonist
Cas No.:820232-50-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Pasireotide is a somatostatin receptor (SSTR) agonist that binds selectively to SST1, SST2, SST3, and SST5 over SST4 (IC50s = 9.3, 1, 1.5, 0.16, and >100 nM, respectively, for human recombinant receptors). It dose-dependently inhibits growth hormone release stimulated by growth hormone-releasing hormone (GHRH) in primary rat anterior pituitary cells and inhibits adrenocorticotropic hormone (ACTH) secretion by some primary human corticotrope adenomas at a concentration of 10 nM. Pasireotide (10 nM) also inhibits ACTH release from and proliferation of mouse AtT20 pituitary corticotrope cells in vitro and inhibits tumor growth of subcutaneously implanted AtT20 cells in vivo in nude mice when administered at a dose of 1.5 μg per day. Pasireotide (0.03 mg/kg) decreases plasma ACTH concentrations and tumor size in dogs with ACTH-dependent Cushing's disease. Formulations containing pasireotide have been used in the treatment of acromegaly and Cushing's disease.
| Cas No. | 820232-50-6 | SDF | |
| Canonical SMILES | O=C([C@H](CC1=CC=CC=C1)N2)N3[C@](C[C@@H](OC(NCCN)=O)C3)([H])C(N[C@H](C4=CC=CC=C4)C(N[C@H](CC5=CNC6=C5C=CC=C6)C(N[C@@H](CCCCN)C(N[C@@H](CC7=CC=C(OCC8=CC=CC=C8)C=C7)C2=O)=O)=O)=O)=O.OC(C[C@H](N)C(O)=O)=O.OC(C[C@H](N)C(O)=O)=O | ||
| 分子式 | C58H66N10O9•2C4H7NO4 | 分子量 | 1313.4 |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.7614 mL | 3.8069 mL | 7.6138 mL |
| 5 mM | 0.1523 mL | 0.7614 mL | 1.5228 mL |
| 10 mM | 0.0761 mL | 0.3807 mL | 0.7614 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。
Phase II trial of SOM230 (Pasireotide LAR) in patients with unresectable hepatocellular carcinoma
J Hepatocell Carcinoma 2018 Jan 12;5:9-15.PMID:29392123DOI:10.2147/JHC.S153672.
Background: A phase II trial of Pasireotide was performed to assess its efficacy and safety in advanced or metastatic hepatocellular carcinoma (HCC). Patients and methods: Patients with advanced HCC and Child-Pugh score ≤7 received Pasireotide LAR 60 mg intramuscularly every 28 days. Primary endpoint was disease control rate. Secondary endpoints were time to tumor progression, response rate, treatment-related adverse events, and overall survival. Serum insulin growth factor-1 was measured before and after Pasireotide. Results: Twenty patients were treated and evaluable. Eighteen patients (90%) had prior therapy; 16 patients (80%) had multiple therapies. Median age was 65, 75% had Barcelona Clinic Liver Cancer stage C, and 55% had metastatic disease. The main toxicity was hyperglycemia. Rare adverse effects included reversible grade 4 elevation in alanina transaminase/aspartate transaminase in one patient. The best response was stable disease in 9 patients (45%). Median time to tumor progression for the 20 patients was 3 months, and median survival was 9 months. Conclusion: Pasireotide had limited clinical benefit as second-line or third-line treatment in patients with advanced or metastatic HCC. Low baseline insulin growth factor-1 level may be indicative when SOM230 treatment may be ineffective, and decreasing levels after treatment may be indicative of disease control.
Effect of SOM230 (Pasireotide) on corticotropic cells: action in dogs with Cushing's disease
Neuroendocrinology 2011;94(2):124-36.PMID:21525729DOI:10.1159/000327429.
SOM230 (Pasireotide) is a multiligand somatostatin (SRIF) analog able to bind to somatostatin receptor (SSTR) subtypes 1, 2, 3 and 5, and trigger antisecretory and antiproliferative signaling cascades. Canines have become in vivo models to test the pharmacological treatment of corticotropinomas because they frequently develop Cushing's disease in a spontaneous manner, due to adrenocorticotropic hormone (ACTH)-producing pituitary adenomas. Different levels of expression of SSTR2 and SSTR5 have been shown in both mouse AtT20 cells and canine tumoral corticotropinoma cells. The objective of this study was to evaluate whether SOM230 controls both tumor cell growth and hormone synthesis, therefore controlling the disease. SOM230 was tested in dogs suffering from Cushing's disease (10 animals were treated continuously during 6 months, and another 10 were treated with 3 cycles consisting of 2 months of treatment followed by a 2-month rest period). A significant decrease in ACTH, urinary cortisol creatinine ratio, adenoma size (magnetic nuclear resonance) and improvement of clinical signs were obtained, without side effects. AtT20 cells treated with SOM230 suppressed pro-opiomelanocortin (POMC) promoter activity through SSTR2, via the G(i) α-subunit, and reduced Nur77/Nurr1 transcriptional activity. We conclude that SOM230, in addition to its well-described antisecretory effects, inhibits, as shown in AtT20 cells, ACTH synthesis at the POMC transcriptional level, an effect mediated mainly through SSTR2, and limits tumor growth. The controlled Cushing's disease in the dogs that received the treatment indicates that SOM230 has a potential therapeutic use in humans suffering from Cushing's disease.