BioAssay record AID 129067 submitted by ChEMBL: Tested for body weight of CDF1 mice bearing P388 leukemia at dose of 100 mg/kg/day on day 5.
Laster, W R. Jr.; Trader, M W.; Schabel, F M. Jr.; and Griswold, T H., "5-fluorouracil (fu) Against leukemia p388 (p388/0) and ara-c- -resistant p388 (p388/ara-c). Abstr." (1982). Subject Strain Bibliography 1982. 3893 ...
BACKGROUND To investigate the antitumor effect of Inonotus obliquus Pilat, the antiproliferative effect of lanostane triterpenoids from a chloroform extract of I. obliquus sclerotia against mouse leukemia P388 cells was assessed. MATERIALS AND METHODS Cell viability was measured by MTT assay. Caspase-3/7 activity and DNA fragmentation were evaluated to analyze apoptosis induction. The in vivo antitumor effect was evaluated by the number of survival days of mouse leukemia P388-bearing female CDF1 mice. RESULTS The chloroform extract of I. obliquus sclerotia inhibited proliferation of the P388 cells. Among the triterpenoids examined, only inotodiol inhibited P388 cell proliferation. DNA fragmentation and caspase-3/7 activation were observed in the P388 cells treated with inotodiol (30 microM). A caspase-3 inhibitor, DEVD-CHO (N-acetyl-Asp-Glu-Val-Asp-al, 100 microM) partially inhibited the DNA fragmentation and growth-inhibition induced by inotodiol. The intraperitoneal administration of 10 mg/kg
BioAssay record AID 136586 submitted by ChEMBL: In vivo antitumor activity against MH 134 cell line in female BDF1 mice after oral administered dose of 50 mg/kg.
Mouse anti Feline Leukemia virus p27 antibody (7226), suitable for use in IFA, ELISA and Lateral Flow applications - The Native Antigen Company.
Chronic anthracycline administration to rabbits causes impairment of cardiac contractility and decreased gene expression of the calcium-induced calcium release channel of sarcoplasmic reticulum (SR), the ryanodine receptor (RYR2). The C-13 hydroxy me
Full Text - Human TP53 gene is characterised by a polymorphism at codon 72 leading to an Arginine-to-Proline (R/P) substitution. The two resulting p53 isoforms have a different subcellular localisation after stress (more nuclear or more mitochondrial for the P or R isoform, respectively). p53P72 variant is more efficient than p53R72 in inducing the expression of genes involved in nuclear DNA repair. Since p53 is involved also in mitochondrial DNA (mtDNA) maintenance, we wondered whether these p53 isoforms are associated with different accumulation of mtDNA damage. We observed that cells bearing p53R72 accumulate lower amount of mtDNA damage upon rotenone stress with respect to cells bearing p53P72, and that p53R72 co-localises with polymerase gamma more than p53P72. We also analysed the in vivo accumulation of heteroplasmy in a 300 bp fragment of mtDNA D-loop of 425 aged subjects. We observed that subjects with heteroplasmy higher than 5% are significantly less than expected in the p53R72/R72 group. On
The goal of this clinical research study is to learn if intensive chemotherapy (hyper-CVAD therapy) given in combination with liposomal vincristine (Marqibo),
Aim: Leukemia is characterized by uncontrolled marrow cell proliferation and metastatic foci. We investigated the antitumor potential of a nutrient mixture on
KOHNO Jun , ASAI Yasuyuki , NISHIO Maki , SAKURAI Masaaki , KAWANO Kimio , HIRAMATSU Hajime , KAMEDA Noriaki , KISHI Noboru , OKUDA Toru , KOMATSUBARA Saburo Journal of antibiotics 52(12), 1114-1123, 1999-12-25 参考文献6件 被引用文献2件 ...
Several findings have concluded the clinical importance of activating FOXO3a and its downstream genes in various anticancer therapeutics (31). TP53, a well-known tumor suppressor gene, is mutated in 50% of human cancers. These p53 mutations play an essential role in tumorigenesis and drug resistance. Different from p53, FOXO3a mutation has not yet been found in human cancer, which makes therapeutics activating FOXO3a more appealing than others. And indeed, activation of FOXO3a in p53-mutated cancer cells is sufficient for tumor suppression (12, 13). For example, doxorubicin has shown to activate FOXO3a to induce the expression of the multidrug resistance gene ABCB1 (MDR1) in K562 doxorubicin-sensitive leukemic cells (38). In chronic myeloid leukemia, inhibition of BCR-ABL by imatinib activates FOXO3a and induces Bim-dependent apoptosis (39). Imatinib also induces erythroid differentiation through repression of the ID1 gene transcription by FOXO3a (40).. Due to the potent antitumor activity of ...
Sun, L. R., Zhong, J. L., Cui, S. X., Li, X., Ward, S. G., Shi, Y. Q., Zhang, X. F., Cheng, Y. N., Gao, J. J. and Qu, X. J., 2010. Modulation of P-glycoprotein activity by the substituted quinoxalinone compound QA3 in adriamycin-resistant K562/A02 cells. Pharmacological Reports ...
Get if set to true, this profile will be active unless another profile in this pom is activated using the command line -P option or by one of that profiles activators ...
TY - JOUR. T1 - A reduced folate carrier mutation produces substrate-dependent alterations in carrier mobility in murine leukemia cells and methotrexate resistance with conservation of growth in 5-formyltetrahydrofolate. AU - Zhao, Rongbao. AU - Assaraf, Yehuda G.. AU - Goldman, I. David. PY - 1998/4/3. Y1 - 1998/4/3. N2 - With 5-formyltetrahydrofolate (5-CHO-THF) as the folate source a methotrexate (MTX) transport-deficient murine leukemia cell line, L1210-G1a, was isolated after chemical mutagenesis and MTX selection. This cell line was 10-fold resistant to MTX in comparison to parental L1210 cells, yet the EC50 for 5-CHO-THF was increased by a factor of only 2. The initial uptake of MTX, at a concentration of 1 μM, was decreased by a factor of 40, whereas influx of 5-CHO-THF dropped by a factor of only 8. This difference in initial uptake rates was attributed solely to changes in influx V(max) without a significant change in K(m). Whereas the RFC1 mRNA level in L1210-G1a cells was ...
Marqibo (liposomal vincristine) is a form of vincristine preparation. Vincristine is designed to interfere with the multiplication of cancer cells, which may slow or stop their growing and spreading throughout the body. This may cause the cancer cells to die. Liposomal vincristine is formed when vincristine is placed inside of oil droplets called liposomes, which may help to improve the delivery of drug to the tumor site. The liposomal formulation results in a slow, steady release of vincristine in the tumor metastasis, exposing the cancer cells to vincristine continuously.. The goal of this clinical research study is to learn if Marqibo (liposomal vincristine) can help to control metastatic uveal melanoma. The safety of liposomal vincristine will also be studied.. Approximately 50 patients will take part in this study. ...
Koshy, J.; Ansary, A.; Lo, K.M.; Das, V.G. (2001) Evaluation of antibacterial properties of triorganotin carboxylates containing functionalised ester groups in tests against some pathogenic bacteria. Metal-based drugs, 8 (2). pp. 107-11. ISSN 0793-0291. Koshy, J.; Das, V.G.; Balabaskaran, S.; Ng, S.W.; Wahab, N. (2000) High In-Vitro Antitumour Activity of Triphenyltin Coumarin 3-Carboxylate and its Coordination Complexes With Monodentate Oxygen Donor Ligands Against the Epstein Barr Virus (EBV)-DNA Positive Raji and the P-388 Murine Leukaemia Cell Lines, and Evidence for the Suppression by Organotin of the Early Antigen Complex in the EBV Lytic Cycle. Metal-based drugs, 7 (5). pp. 245-51. ISSN 0793-0291. ...
HOUSTON, TX -- (Marketwired) -- 08/29/17 -- Moleculin Biotech, Inc., (NASDAQ: MBRX) ("Moleculin" or the "Company"), a preclinical pharmaceutical company focused on the development of anti-cancer drug candidates, some of which are based on license agreements with The University of Texas System on behalf of the M.D. Anderson Cancer Center, today announced it has filed with the Food and Drug Administration (FDA) an Investigational New Drug (IND) application to study Annamycin in the treatment of relapsed or refractory acute myeloid leukemia (AML).. Submitting this revised IND marks a significant milestone for Moleculin. FDA allowing the IND to go into effect -- which is the anticipated next step and normally would occur within 30 days -- will allow the Company to begin additional clinical trials as part of demonstrating the safety and effectiveness of Annamycin. The current plan is to seek approval for treating relapsed or refractory acute myeloid leukemia. If the IND goes into effect as planned, ...
New antitumor agents designated MA 144-M.sub.1 and MA 144-M.sub.2, which are anthracycline glycosides and inhibit the growth of gram-positive bacteria, e.g. Staphyococcus aureus, Bacillus subtilis and
Carter, S K. and Friedman, M A., "5-(3,3-dimethyl-1-triazeno)-imidazole-4-carboxamide (dtic, Dic, nsc- -45388)-a new antitumor agent with activity against malignant melanoma." (1972). Subject Strain Bibliography 1972. 568 ...
Anthracycline-formaldehyde conjugates: Cellular uptake, localization, toxicity, and circumvention of multidrug resistance. Journal Article ...
Cyclopentenyl methyl piperidinedione-13C4 - Internal standard , HPLC-MS method validation, LC-MS-MS method validation, Clinical diagnostic, Analytical method development, Alsachim
These samples are collected at the following pressures: 5, 10, 25, 50, 75, 100, 125, 150, 175, 200, 250, 300, 400, 600, 800, 1000, 1250, 1500, 2000, 2500, 3000, 3500, 4000 dbar and 10 m above the ocean floor ...
Line p2h3-18-3. Expressed in all tissues. Expression is weak in the outer tissues in the mature part of the root but it remains high in the vascular tissues.. ...
Siz-le-ri bil-mem ama be-nim yaz ay-la-rında par-mak-la-rı-mı kı-pır-da-ta-cak ha-lim ol-maz sev-gi-li okur-la-rım. Şez-lon-gu-ma uzan-dı-ğım-da, kar-şım-da de-niz ol-ma-sa göz-le-ri-mi bi-le aç-mak is-te-mem. Göz-ka-pak-la-rı-nı kal-dı-ra-cak-sın da... Devamını okumak için başlığı tıklayınız.
Hana Biosciences, a biopharmaceutical company focused on advancing cancer care, recently announced that the US Food and Drug Administration (FDA) has granted orphan drug designation for vincristine sulfate liposomes injection (Marqibo) in the treatment of adult patients with acute lymphoblastic leukemia (ALL). 1
HOUSTON, TX -- (Marketwired) -- 10/03/17 -- Moleculin Biotech, Inc., (NASDAQ: MBRX) ("Moleculin" or the "Company"), a clinical stage pharmaceutical company focused on the development of anti-cancer drug candidates, some of which are based on license agreements with The University of Texas System on behalf of the M.D. Anderson Cancer Center, today announced that it has entered into an agreement to conduct its clinical trial to study Annamycin for the treatment of acute myeloid leukemia (AML) with the first of several hospitals desiring to be treatment centers.. "Now that our IND (investigational new drug) application is approved, the race is on to open treatment centers and begin recruiting patients," commented Walter Klemp, Chairman and CEO of Moleculin. "We have identified 14 treatment sites that meet our criteria and have expressed an interest in participating, so there will be much more of this to come.". "This first facility is a hematology clinic in a major hospital in Poland," continued ...
The preparation of a series of pironetin analogues with simplified structure is described. Their cytotoxic activity and their interactions with tubulin have been investigated. It has been found that, while less active than the parent molecule, the pironetin analogues still share the mechanism of action of the latter and compete for the same binding site to α-tubulin. Variations in the configurations of their stereocenters do not translate into relevant differences between biological activities [-] ...
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The oxazaphosphorines including cyclophosphamide (CPA), ifosfamide (IFO), and trofosfamide represent an important group of therapeutic agents due to their substantial antitumor and immuno-modulating activity. CPA is widely used as an anticancer drug, an immunosuppressant, and for the mobilization of hematopoetic progenitor cells from the bone marrow into peripheral blood prior to bone marrow transplantation for aplastic anemia, leukemia, and other malignancies. New oxazaphosphorines derivatives have been developed in an attempt to improve selectivity and response with reduced toxicity. These derivatives include mafosfamide (NSC 345842), glufosfamide (D19575, β-D-glucosylisophosphoramide mustard), NSC 612567 (aldophosphamide perhydrothiazine), and NSC 613060 (aldophosphamide thiazolidine). This review highlights the metabolism and transport of these oxazaphosphorines (mainly CPA and IFO, as these two oxazaphosphorine drugs are the most widely used alkylating agents) and the clinical ...
In another example of chemists replacing carbon in monomers, John D. Protasiewicz of Case Western Reserve University has been preparing π-conjugated multiring scaffolds bearing P=C double bonds known as benzoxaphospholes. "We want to replace carbon atoms, maybe all of them, with other elements," Protasiewicz said. He explained that P=C bonds like those in benzoxaphospholes can mimic C=C bonds-phosphorus is coming to be known among chemists as a "carbon copy," he pointed out. A bonus is that the P=C bonds can lower the energy of the lowest unoccupied molecular orbital of the molecules to alter their electronic properties. Protasiewiczs team has shown these compounds have a high degree of luminescence. In related work presented at the symposium, Thomas Baumgartner of York University described modifying viologens to make phosphole derivatives. Viologens are bipyridine compounds often used to build electrochromic properties into polymeric materials.. ...
So far GSK3B has been described to be involved in modulating biological processes as opposite as proliferation or apoptosis, depending on the cellular, molecular, and developmental context (28-37). In fact, GSK3B is known to play an antiproliferative role by promoting APC-dependent phosphorylation-and hence proteosome-mediated degradation-of β-catenin, a transcription factor positively regulating Myc and cyclin D1 expression (14). In HCT116 colon carcinoma cell line it has been showed that GSK3B inhibition leads to apoptosis via p53 activation (38, 39). Here we present a novel role for GSK3B in colon carcinomas showing that its inhibition resensitizes drug-resistant p53-null colon cancer cells to chemotherapy both in vitro and in vivo and that GSK3B negatively regulates RIP1-independent necroptosis in response to chemotherapy. Moreover, in accordance with in vitro and in vivo data, we showed that GSK3B is activated in a high percentage (63.6%) of samples from 5FU-treated stage II colon ...
Creative Peptides offers H-beta-(1-Cyclopentenyl)-DL-Ala-OH for your research. We also provide custom peptide synthesis, process development, GMP manufacturing.
MacDowell, Edwin Carleton (January 1955) Mouse leukemia. XV. Resistance to spontaneous cases in hybrids, induced by milk. Cancer Research, 15 (1). pp. 19-22. MacDowell, Edwin Carleton (January 1955) Mouse leukemia. XVI. Spontaneous cases in strain C58 resisted by milk of old STOLI foster nurses. Cancer Research, 15 (1). pp. 23-25. Bhaskar, Surindar Nath, Schour, Isaac, MacDowell, Edwin Carleton, Weinmann, Joseph Peter (June 1951) The skull and the dentition of screw tail mice. The Anatomical Record, 110 (2). pp. 199-229. MacDowell, E. Carleton (February 1950) "Light"- a new mouse color. The Journal of Heredity, 41 (2). pp. 35-36. Taylor, Martha J., MacDowell, E. Carleton (March 1949) Mouse leukemia. XIV. Freeing transplanted line I from a contaminating virus. Cancer Research, 9 (3). pp. 144-149. MacDowell, Edwin Carleton, Taylor, Martha J. (1948) Mouse leukemia. XIII. A maternal influence that lowers the incidence of spontaneous cases. Proceedings of the Society for Experimental Biology and ...
siRNA E6AP transfection efficiency varied for CaSki and HeLa cell lines from 28% to 47%. In both cell lines p53 and p21 expression levels increased.. - G Anton, D Socolov, Z Sgarburã, F. Cornitescu, C D Goia, I V. Iancu, A Plesa, S. Teleman, DNA versus RNA methods for human papillomavirus detection in cervical samples, Gineco.ro -a Journal of Obstetrics and Gynecology 2009, 5, ISSN:1841-4435 ...
A novel approach to circumvent multidrug resistance is hybridization of natural products in dimers. We analyzed homodimers of two artesunic acid molecules and heterohybrids of artesunic acid and betulin in human CCRF-CEM and multidrug-resistant P-glycoprotein-overexpressing CEM/ADR5000 leukemia cells. Multidrug-resistant cells were not cross-resistant to the novel compounds. Collateral sensitivity was observed for artesunic acid homodimer. Artesunic acid and artesunic acid homodimer induced G0/G1 cell cycle arrest, apoptosis, and formation of reactive oxygen species. ...
Consumer Medicine InformationConsumer Medicine InformationWhat is in this leaflet?This leaflet answers some common questions about PEXSIG (perhexiline maleate) tablets.It does not contain all of the available information about PEXSIG tablets.It does not replace talking to your doctor or pharmacist.All medicines have risks and benefits. Your doctor has weighed the risks of you taking PEXSIG tablets against the expected benefits.If you have any concerns about taking this medicine, ask your doctor or..
위는 이진 분류 (binary classification)의 PR 그래프의 예입니다. 그래프가 위쪽으로 갈수록 정확도가 높은 모델이고, ROC와 마찬가지로 PR 그래프의 AUC (면적)값을 이용하여 모델의 정확도를 평가할 수 있습니다.. (출처 : http://scikit-learn.org/stable/auto_examples/model_selection/plot_precision_recall.html). 그러면 모델이 쓸만한 모델인지 아닌지는 어떤 기준을 사용할까요? ROC 그래프의 경우에는 Y=X 그래프를 기준으로 그래프 윗쪽에 있는 경우 쓸만한 모델로 판단을 했는데, PR 그래프의 경우 Base line이라는 것을 사용합니다.. Base line = P / (P+N) 으로 정하는데, P는 데이타에서 Positive 레이블의 수, N 은 전체 데이타의 수입니다. 예를 들어 암 데이타에서 암 양성이 300개 이고, 전체 데이타가 700이면 Base line은 300/(700+300) = 0.3 이 됩니다.. ...
Tephrosin is a natural rotenoid which has potent antitumor activities. Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors. - Mechanism of Action & Protocol.
വിവരങ്ങൾ ക്രിയേറ്റീവ് കോമൺസ് ആട്രിബ്യൂഷൻ-ഷെയർഎലൈക്ക് അനുമതിപത്ര പ്രകാരം ലഭ്യമാണ്; മേൽ നിബന്ധനകൾ ഉണ്ടായേക്കാം. കൂടുതൽ വിവരങ്ങൾക്ക് ഉപയോഗനിബന്ധനകൾ കാണുക ...
TY - JOUR. T1 - Transforming growth factor β1 inhibits expression of the gene products for steel factor and its receptor (c-kit). AU - Heinrich, Michael C.. AU - Dooley, Douglas C.. AU - Keeble, Winifred W.. PY - 1995/4/1. Y1 - 1995/4/1. N2 - Transforming growth factor β1 (TGF-β1), a product of marrow stromal cells, inhibits the proliferation and differentiation of hematopoietic progenitor cells within the hematopoietic microenvironment. Steel factor (SF), also a product of marrow stromal cells, is an essential positive regulator of hematopoiesis in vivo. TGF-β1 has been shown to repress human and murine leukemic cell and murine lin- bone marrow mononuclear cell expression of the receptor for SF (c-kit). We speculated that TGF-β1 might exert its inhibitory effect on hematopoiesis in part by decreasing SF/c-kit interactions. Therefore, we tested the hypothesis that TGF-β1 inhibits both stromal cell expression of SF and hematopoietic progenitor cell expression of c-kit. We measured stromal ...
Approach and Results-Using both rat balloon injury and mouse wire injury models, we identified CTP synthase 1 (CTPS1) as one of the potential targets that may be used for developing therapeutics for treating neointima-related disorders. CTPS1 was induced in proliferative SMCs in vitro and neointima SMCs in vivo. Blockade of CTPS1 expression by small hairpin RNA or activity by cyclopentenyl cytosine suppressed SMC proliferation and neointima formation. Surprisingly, cyclopentenyl cytosine had much less effect on EC proliferation. Of importance, blockade of CTPS1 in vivo sustained the re-endothelialization as a result of induction of CTP synthesis salvage pathway enzymes nucleoside-diphosphate kinase A and B in ECs. Diphosphate kinase B seemed to preserve EC proliferation via use of extracellular cytidine to synthesize CTP. Indeed, blockade of both CTPS1 and diphosphate kinase B suppressed EC proliferation in vitro and the re-endothelialization in vivo.. ...
Septacin, a new antitumor and antifungal antibiotic produced by Streptomyces fimbriatus Antimicrob Agents Chemother 1963, 83-88, ...
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A series of amidoximes was prepared and evaluated for possible antitumor activity against L1210 leukemia. Three of the most active compounds in the L1210 system, formamidoxime, acetamidoxime, and 2-aminoacetamidoxime hydrochloride, were also active against P388 leukemia. Acetamidoxime was marginally active against Lewis lung carcinoma. The active amidoximes showed best activity against L1210 leukemia when given two times daily, 5 hours apart, for 8 days. Most of the amidoximes produced excessive central nervous system stimulation.
In conclusion, the present results suggest that SP could be effective in treatment against the erythrocytic stages of vivax malaria in Iran; however, the increased frequency of mutant haplotypes in Iran since 2006 is worrying and indicates the emergence of drug-tolerant/resistant P. vivax isolates in Iran in near future.. ...
The presence of the glucocorticoid (GC) receptor is required for GC-evoked apoptosis. However, the explicit mechanism of involvement of this receptor continues to be debated. Employing the murine (S-49) and human (CCRF-CEM) lymphoid cell lines, we demonstrated that this response requires a specializ …
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... is an indolocarbazole isolated from Lechevalieria aerocolonigenes. Rebeccamycin displays selective antitumor activity against several cell lines. Analogues of rebeccamycin have been tested in clinical trials for cancer therapy ...