(R)-BAY1238097
目录号 : GC34443(R)-BAY1238097是BAY1238097的低活性R型异构体。BAY1238097是一种有效的、BET与组蛋白结合的选择性抑制剂,通过下调c-Myc水平及下游转录组,在AML(急性髓性白血病)和MM(多发性骨髓瘤)模型中表现出较强的抗增殖活性。
Cas No.:1564269-85-7
Sample solution is provided at 25 µL, 10mM.
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(R)-BAY1238097 is the R-isomer with lower activity of BAY1238097. BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome[1][2]. BET[1].
[1]. Lejeune, P., et al. (2015) Abstract 3524: BAY 1238097, a novel BET inhibitor with strong efficacy in hematological tumor models. Cancer Research, 75(15 Suppl), 884. [2]. Bernasconi E, et al. Preclinical evaluation of the BET bromodomain inhibitor BAY 1238097 for the treatment of lymphoma. Br J Haematol. 2017 Sep;178(6):936-948.
Cas No. | 1564269-85-7 | SDF | |
Canonical SMILES | O=C(N1N=C(C2=CC=C(N3CCN(C)CC3)C=C2)C4=CC(OC)=C(OC)C=C4C[C@H]1C)NC | ||
分子式 | C25H33N5O3 | 分子量 | 451.56 |
溶解度 | DMSO : 150 mg/mL (332.18 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.2145 mL | 11.0727 mL | 22.1455 mL |
5 mM | 0.4429 mL | 2.2145 mL | 4.4291 mL |
10 mM | 0.2215 mL | 1.1073 mL | 2.2145 mL |
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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 | |||
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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。
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Linking big five personality traits to sexuality and sexual health: A meta-analytic review
Psychol Bull 2018 Oct;144(10):1081-1110.PMID:29878796DOI:10.1037/bul0000157.
This meta-analytic review addresses whether the major dimensions of trait personality relate to components of human sexuality. A comprehensive literature search identified 137 studies that met inclusion criteria (761 effect sizes; total n = 420,595). Pooled mean effects were computed using inverse-variance weighted random effects meta-analysis. Mean effect sizes from 100 separate meta-analyses provided evidence that personality relates to theoretically predicted components of sexuality and sexual health. Neuroticism was positively related to sexual dissatisfaction (R+ = .18), negative emotions (R+ = .42), and symptoms of sexual dysfunction (R+ = .16). Extraversion was positively related to sexual activity (R+ = .17) and risky sexual behavior (R+ = .18), and negatively related to symptoms of sexual dysfunction (R+ = -.17). Openness was positively related to homosexual orientation (R+ = .16) and liberal attitudes toward sex (R+ = .19). Agreeableness and conscientiousness were negatively related to sexually aggressive behavior (R+ = -.20; R+ = -.14) and sexual infidelity (R+ = -.18; R+ = -.17). Less robust evidence indicated that extraversion related negatively, and neuroticism positively, to child sexual abuse, and that openness related negatively to homophobic attitudes. Random effects metaregression identified age, gender, and study quality as important moderators of pooled mean effects. These findings might be of interest to health care professionals developing health care services that aim to promote sexually healthy societies. (PsycINFO Database Record
Management of thyroid cancer: United Kingdom National Multidisciplinary Guidelines
J Laryngol Otol 2016 May;130(S2):S150-S160.PMID:27841128DOI:10.1017/S0022215116000578.
This is the official guideline endorsed by the specialty associations involved in the care of head and neck cancer patients in the UK. This paper provides recommendations on the management of thyroid cancer in adults and is based on the 2014 British Thyroid Association guidelines. Recommendations • Ultrasound scanning (USS) of the nodule or goitre is a crucial investigation in guiding the need for fine needle aspiration cytology (FNAC). (R) • FNAC should be considered for all nodules with suspicious ultrasound features (U3-U5). If a nodule is smaller than 10 mm in diameter, USS guided FNAC is not recommended unless clinically suspicious lymph nodes on USS are also present. (R) • Cytological analysis and categorisation should be reported according to the current British Thyroid Association Guidance. (R) • Ultrasound scanning assessment of cervical nodes should be done in FNAC-proven cancer. (R) • Magnetic resonance imaging (MRI) or computed tomography (CT) should be done in suspected cases of retrosternal extension, fixed tumours (local invasion with or without vocal cord paralysis) or when haemoptysis is reported. When CT with contrast is used pre-operatively, there should be a two-month delay between the use of iodinated contrast media and subsequent radioactive iodine (I131) therapy. (R) • Fluoro-deoxy-glucose positron emission tomography imaging is not recommended for routine evaluation. (G) • In patients with thyroid cancer, assessment of extrathyroidal extension and lymph node disease in the central and lateral neck compartments should be undertaken pre-operatively by USS and cross-sectional imaging (CT or MRI) if indicated. (R) • For patients with Thy 3f or Thy 4 FNAC a diagnostic hemithyroidectomy is recommended. (R) • Total thyroidectomy is recommended for patients with tumours greater than 4 cm in diameter or tumours of any size in association with any of the following characteristics: multifocal disease, bilateral disease, extrathyroidal spread (pT3 and pT4a), familial disease and those with clinically or radiologically involved nodes and/or distant metastases. (R) • Subtotal thyroidectomy should not be used in the management of thyroid cancer. (G) • Central compartment neck dissection is not routinely recommended for patients with papillary thyroid cancer without clinical or radiological evidence of lymph node involvement, provided they meet all of the following criteria: classical type papillary thyroid cancer, patient less than 45 years old, unifocal tumour, less than 4 cm, no extrathyroidal extension on ultrasound. (R) • Patients with metastases in the lateral compartment should undergo therapeutic lateral and central compartment neck dissection. (R) • Patients with follicular cancer with greater than 4 cm tumours should be treated with total thyroidectomy. (R) • I131 ablation should be carried out only in centres with appropriate facilities. (R) • Serum thyroglobulin (Tg) should be checked in all post-operative patients with differentiated thyroid cancer (DTC), but not sooner than six weeks after surgery. (R) • Patients who have undergone total or near total thyroidectomy should be started on levothyroxine 2 µg per kg or liothyronine 20 mcg tds after surgery. (R) • The majority of patients with a tumour more than 1 cm in diameter, who have undergone total or near-total thyroidectomy, should have I131 ablation. (R) • A post-ablation scan should be performed 3-10 days after I131 ablation. (R) • Post-therapy dynamic risk stratification at 9-12 months is used to guide further management. (G) • Potentially resectable recurrent or persistent disease should be managed with surgery whenever possible. (R) • Distant metastases and sites not amenable to surgery which are iodine avid should be treated with I131 therapy. (R) • Long-term follow-up for patients with differentiated thyroid cancer (DTC) is recommended. (G) • Follow-up should be based on clinical examination, serum Tg and thyroid-stimulating hormone assessments. (R) • Patients with suspected medullary thyroid cancer (MTC) should be investigated with calcitonin and carcino-embryonic antigen levels (CEA), 24 hour catecholamine and nor metanephrine urine estimation (or plasma free nor metanephrine estimation), serum calcium and parathyroid hormone. (R) • Relevant imaging studies are advisable to guide the extent of surgery. (R) • RET (Proto-oncogene tyrosine-protein kinase receptor) proto-oncogene analysis should be performed after surgery. (R) • All patients with known or suspected MTC should have serum calcitonin and biochemical screening for phaeochromocytoma pre-operatively. (R) • All patients with proven MTC greater than 5 mm should undergo total thyroidectomy and central compartment neck dissection. (R) • Patients with MTC with lateral nodal involvement should undergo selective neck dissection (IIa-Vb). (R) • Patients with MTC with central node metastases should undergo ipsilateral prophylactic lateral node dissection. (R) • Prophylactic thyroidectomy should be offered to RET-positive family members. (R) • All patients with proven MTC should have genetic screening. (R) • Radiotherapy may be useful in controlling local symptoms in patients with inoperable disease. (R) • Chemotherapy with tyrosine kinase inhibitors may help in controlling local symptoms. (R) • For individuals with anaplastic thyroid carcinoma, initial assessment should focus on identifying the small proportion of patients with localised disease and good performance status, which may benefit from surgical resection and other adjuvant therapies. (G) • The surgical intent should be gross tumour resection and not merely an attempt at debulking. (G).
Relationship between core stability, functional movement, and performance
J Strength Cond Res 2011 Jan;25(1):252-61.PMID:20179652DOI:10.1519/JSC.0b013e3181b22b3e.
The purpose of this study was to determine the relationship between core stability, functional movement, and performance. Twenty-eight healthy individuals (age = 24.4 ± 3.9 yr, height = 168.8 ± 12.5 cm, mass = 70.2 ± 14.9 kg) performed several tests in 3 categories: core stability (flexion [FLEX], extension [EXT], right and left lateral [LATr/LATl]), functional movement screen (FMS) (deep squat [DS], trunk-stability push-up [PU], right and left hurdle step [HSr/HSl], in-line lunge [ILLr/ILLl], shoulder mobility [SMr/SMl], active straight leg raise [ASLRr/ASLRl], and rotary stability [RSr/RSl]), and performance tests (backward medicine ball throw [BOMB], T-run [TR], and single leg squat [SLS]). Statistical significance was set at p ≤ 0.05. There were significant correlations between SLS and FLEX (R = 0.500), LATr (R = 0.495), and LATl (R = 0.498). The TR correlated significantly with both LATr (R = 0.383) and LATl (R = 0.448). Of the FMS, BOMB was significantly correlated with HSr (R = 0.415), SMr (R = 0.388), PU (R = 0.407), and RSr (R = 0.391). The TR was significantly related with HSr (R = 0.518), ILLl (R = 0.462) and SMr (R = 0.392). The SLS only correlated significantly with SMr (R = 0.446). There were no significant correlations between core stability and FMS. Moderate to weak correlations identified suggest core stability and FMS are not strong predictors of performance. In addition, existent assessments do not satisfactorily confirm the importance of core stability on functional movement. Despite the emphasis fitness professionals have placed on functional movement and core training for increased performance, our results suggest otherwise. Although training for core and functional movement are important to include in a fitness program, especially for injury prevention, they should not be the primary emphasis of any training program.
Evidence for the distinction between "consonantal-/R/" and "vocalic-/R/" in American English
Clin Linguist Phon 2015;29(8-10):613-22.PMID:26172586DOI:10.3109/02699206.2015.1047962.
We examine the distinction between "consonantal-r" and "vocalic-r" in American English, terms encountered in the speech pathology literature but rarely in phonetic studies. We review evidence from phonetics, phonology and therapy, and describe our own study which measured percentage rhoticity in pre- and post-vocalic /R/. We suggest that the evidence supports a view that there is no more variation between pre-vocalic and post-vocalic /R/ than found in many other consonants. We also evaluate the different transcription traditions for post-vocalic /R/ in American English (as a consonant or a vowel), and describe a preliminary study demonstrating that these transcriptions are not equivalent, and denote different realisations.
Fragrance material review on dihydrocarveol (R,R,R)
Food Chem Toxicol 2008 Nov;46 Suppl 11:S121-2.PMID:18640226DOI:10.1016/j.fct.2008.06.041.
A toxicologic and dermatologic review of dihydrocarveol (R,R,R) when used as a fragrance ingredient is presented.