BT-13
目录号 : GC34509
BT-13是有效的、胶质细胞源性神经营养因子(GDNF)受体RET的选择性激动剂(独立于GDNF配体发挥作用)，促进体外感觉神经元神经突生长，减轻大鼠神经病变的发生。
Cas No.:924537-98-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
BT-13 is a potent and selective glial cell line-derived neurotrophic factor (GDNF) receptor RET agonist independently of GFLs, promoting neurite growth from sensory neurons in vitro and attenuates experimental neuropathy in the Rat[1]. GDNF receptor RET[1].
BT-13 stimulates phosphorylation of RET, as well as RET-dependent intracellular signaling, but activated neither NGF receptor TrkA nor BDNF receptor TrkB nor intracellular signaling in the absence of RET[1].
BT-13 (20 and 25mg/kg in rats induced by ligation of left L5 and L6 spinal nerves) has a slight antinociceptive/antihyperalgesic effect and protected DRG neurons in rats with surgery-induced neuropathy[1]. Animal Model: Rats induced by ligation of left L5 and L6 spinal nerves[1].
[1]. Sidorova YA, et al. A Novel Small Molecule GDNF Receptor RET Agonist, BT13, Promotes Neurite Growth from Sensory Neurons in Vitro and Attenuates Experimental Neuropathy in the Rat. Front Pharmacol. 2017 Jun 21;8:365.
| Cas No. | 924537-98-4 | SDF | |
| Canonical SMILES | O=S(C1=CC=C(OC)C(N2CCN(C(C3=CC=C(F)C=C3C(F)(F)F)=O)CC2)=C1)(N(CC)CC)=O | ||
| 分子式 | C23H27F4N3O4S | 分子量 | 517.54 |
| 溶解度 | DMSO: 25 mg/mL (48.31 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 | 1.9322 mL | 9.6611 mL | 19.3222 mL |
| 5 mM | 0.3864 mL | 1.9322 mL | 3.8644 mL |
| 10 mM | 0.1932 mL | 0.9661 mL | 1.9322 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。
High dose rate brachytherapy for prostate cancer: A prospective toxicity evaluation of a one day schedule including two 13.5 Gy fractions
Background and purpose: High dose-rate (HDR) brachytherapy (BT) provides a highly conformal method of dose delivery to the prostate. The purpose of this study is to prospectively determine the toxicity of the treatment protocol of 13.5 Gy × 2 fractions. Materials and methods: From 2010 through 2017, 119 patients with low (71%) or intermediate-risk prostate cancer were prospectively treated in a single institute with HDR-BT at 13.5 Gy × 2 fractions within one day. Median follow-up time was 4.4 years. Results: Actuarial rates of no biochemical evidence of disease, overall survival and metastasis-free survival for all patients were 96%,98% and 98%, respectively. The cumulative incidence of acute grade 2 and 3 genitourinary (GU) toxicity was 9% and 2%, respectively. The corresponding incidences of late GU toxicity were 18% and 1%. No grade ≥4 of either type of toxicity was detected. Multivariate analysis showed that having higher international prostate symptom score (IPSS; P = 0.041) or higher V200 (P = 0.013) was associated with a higher risk of experiencing any grade of acute GU toxicity. In addition, patients having a higher IPSS (P = 0.019) or a higher V150 (P = 0.033) were associated with a higher grade >1 acute GU toxicity. Conclusions: The findings of this study show that HDR-BT 13.5 Gy × 2 as monotherapy was safe and effective for prostate cancer patients with low-intermediate risk.
Visibility of microcalcification clusters and masses in breast tomosynthesis image volumes and digital mammography: a 4AFC human observer study
Purpose: To investigate the visibility of simulated lesions in digital breast tomosynthesis (BT) image volumes compared with 2D digital mammography (DM).
Methods: Simulated lesions (masses and microcalcifications) were added to images of the same women acquired on a DM system (Mammomat Novation, Siemens) and a BT prototype. The same beam quality was used for the DM and BT acquisitions. The total absorbed dose resulting from a 25-projection BT acquisition and reconstruction (BT(25)) was approximately twice that of a single DM view. By excluding every other projection image from the reconstruction (BT(13)), approximately the same dose as in DM was effected. Simulated microcalcifications were digitally added with varying contrast to the DM and BT images. Simulated masses with 8 mm diameter were also added to BT images. A series of 4-alternative forced choice (4AFC) human observer experiments were conducted. Four medical physicists participated in all experiments, each consisting of 60 trials per experimental condition. The observers interpreted the BT image volumes in cine-mode at a fixed image sequence speed. The required threshold contrast (S(t)) to achieve a detectability index (d') of 2.5 (i.e., 92.5% correct decisions) was determined.
Results: The S(t) for mass detection in DM was approximately a factor of 2 higher than required in BT indicating that the detection of masses was improved under BT conditions compared to DM. S(t) for microcalcification detection was higher for BT than for DM at both BT dose levels (BT(25) and BT(13)), with a statistically significant difference in S(t) between DM and BT(13). These results indicate a dose-dependent decrease in detection performance in BT for detection of microcalcifications.
Conclusions: In agreement with previous investigations, masses of size 8 mm can be detected with less contrast in BT than in DM indicating improved detection performance for BT. However, for the investigated microcalcifications, the results of this study indicate potentially worse performance for BT than for DM at the same dose level.
Characterization of combined intracavitary/interstitial brachytherapy including oblique needles in locally advanced cervix cancer
Purpose: To characterize and report on dosimetric outcomes of image guided adaptive brachytherapy (IGABT) using intracavitary and interstitial (IC/IS) applicators including oblique needles (O-needles) in locally advanced cervical cancer (LACC).
Methods and materials: Twenty LACC patients treated with radio-chemotherapy and offered IC/IS-IGABT including O-needles were analyzed. An in-house 3D-printed vaginal template was used to steer the needles parallel and obliquely in relation to the tandem, supplemented with free-hand needles if needed. Implant characteristics and loading patterns were analyzed. Using the equivalent dose in 2Gy-fractions (EQD2) concept, cumulative (EBRT+BT) V85, V75, V60Gy, targets/OARs doses and high dose volumes (150%, 200% and 300% (100% = 85 Gy EQD210)) were evaluated.
Results: Median(range) tumor width at diagnosis was 5.5(3.6; 7.5)cm; CTVHR volume was 45(23; 136)cm3 with maximum distance from tandem to CTVHR border of 3.4(2.5; 4.8)cm. T-stage distribution was IIB/III/IVA in 6(30%)/9(45%)/5(25%) of patients. At BT, 13(65%) patients had distal parametrial/pelvic wall infiltration. Median(range) number of needles per patient was 11(8-18). Average distribution of intrauterine, vaginal and interstitial dwell times were 31%, 25% and 44%, respectively. Median(range) dwell-time per dwell position was 11(2-127)% of average point-A based standard loading. Median V85Gy/V150%/V200%/V300% were 85(38; 171)/41(21; 93)/22(12; 41)/7(4; 19) cm3; CTVHR D90% was 93(83; 97)Gy EQD210; bladder/rectum/sigmoid/bowel D2cm3 were 78(64; 104)/65(52; 76)/59(53; 69)/61(47; 76)Gy EQD23.
Conclusions: The use of O-needles in patients with large and/or unfavorable tumors resulted in excellent target coverage and OARs sparing. Intrauterine and vaginal loadings were reduced compared to standard loading and almost half of the loading was shifted into IS needles. This was achieved with gentle loading in the majority of dwell positions.
Advantage and validation of vendor-independent software for myocardial strain analysis compared to vendor-specific software
Introduction: One of the main limitations incorporating strain imaging into widespread clinical practice is inter-vendor incompatibility. This poses a problem when serial strain measurements are required in a multi-vendor echocardiography laboratory.
Methods: This study sought to compare the variability of two-dimensional speckle-tracking global and regional longitudinal strain using vendor-specific software and vendor-independent software from images acquired by two different commercially available ultrasound systems. Forty subjects underwent two sequential echocardiographic acquisitions using different ultrasound systems (GE Vivid E9 and Philips iE33). Global longitudinal strain and regional peak longitudinal strain were derived using vendor-specific software (EchoPAC BT 13 v201 and QLAB version 10.3) and vendor-independent software (TomTec Image Arena version 4.6). Agreement and reproducibility of global and regional strain between vendor-specific and vendor-independent software were assessed by independent blinded observers.
Results: Global longitudinal strain derived from vendor-independent software was comparable to global longitudinal strain derived from vendor-specific software, whilst regional strain was lower in agreement compared to global longitudinal strain. There was good overall agreement and high inter- and intra-observer reproducibility using vendor-independent software for global longitudinal strain and regional strain.
Conclusions: Vendor-independent software provides good agreement with vendor-specific software for global longitudinal strain. However, minor variability exists for regional strain measurements between vendor-independent and vendor-specific software. Good agreement of strain measurements derived by vendor-independent software suggests vendor-independent software could potentially be useful for serial follow-up of global longitudinal strain.
Redox responsive Pluronic micelle mediated delivery of functional siRNA: a modular nano-assembly for targeted delivery
There is an unmet need to develop strategies that allow site-specific delivery of short interfering RNA (siRNA) without any associated toxicity. To address this challenge, we have developed a novel siRNA delivery platform using chemically modified pluronic F108 as an amphiphilic polymer with a releasable bioactive disulfide functionality. The micelles exhibited thermoresponsive properties and showed a hydrodynamic size of ?291 nm in DLS and ?200-250 nm in SEM at 37 °C. The grafting of free disulfide pyridyl groups enhanced the transfection efficiency and was successfully demonstrated in human colon carcinoma (HCT116; 88%) and glioma cell lines (U87; 90%), non-cancerous human dermal fibroblast (HDF; 90%) cells as well as in mouse embryonic stem (mES; 54%) cells. To demonstrate the versatility of our modular nanocarrier design, we conjugated the MDGI receptor targeting COOP peptide on the particle surface that allowed the targeted delivery of the cargo molecules to human patent-derived primary BT-13 gliospheres. Transfection experiments with this design resulted in ?65% silencing of STAT3 mRNA in BT-13 gliospheres, while only ?20% of gene silencing was observed in the absence of the peptide. We believe that our delivery method solves current problems related to the targeted delivery of RNAi drugs for potential in vivo applications.