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[ CAS No. 35013-72-0 ] {[proInfo.proName]}

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Chemical Structure| 35013-72-0
Chemical Structure| 35013-72-0
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Product Citations

Product Citations      Expand+

Wrobel, Konrad ; Deregowska, Anna ; Betlej, Gabriela , et al. DOI:

Abstract: Polyamidoamine (PAMAM) dendrimers are widely used as a part of drug delivery systems (DDS) to improve anticancer drug bioavailability. In the present study, monophosphates of nucleosides, anti-nucleosides (cytarabine, C and fludarabine, F) and synthetic glucocorticoid dexamethasone (D) were attached to the third generation (G3) PAMAM dendrimer via phosphamide pH-sensitive linker. Conjugates were found to be stable at neutral pH, whereas acid-triggered hydrolysis of phosphamide bond was observed at pH 5. The anticancer action of selected biotinylated mono- and di-conjugates, namely CP-, FP-, DP-CP- and DP-FP-PAMAM dendrimers was then compared to cytotoxic activity of free drugs using four cellular models of leukemia in vitro, i.e., K-562, LAMA-84, THP-1 and HL-60 cells. Ten nM DP-CP-conjugate lowered metabolic activity, caused G0/G1 cell cycle arrest and induced apoptotic cell death in HL-60 cells compared to non-cytotoxic and non-cytostatic action of free drugs when used at the same concentration 10 nM CP-, DP-FP- and FP-conjugates also promoted a decrease in metabolic activity in K-562, LAMA-84, and THP-1 and HL-60 cells, resp., however, without a sign of cytotoxicit. In conclusion, we show that the anticancer potential of CP and FP in leukemia cells may be enhanced by the conjugation with PAMAM dendrimers, especially in the presence of DP in selected exptl. settings.

Keywords: PAMAM G3 dendrimer conjugates ; Cytarabine ; Fludarabine ; Dexamethasone ; pH-cleavable linker ; Leukemia cell apoptosis

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Wrobel, Konrad ; Wolowiec, Stanislaw ; Markowicz, Joanna , et al. DOI: PubMed ID:

Abstract: Recent achievement in anticancer therapy considers the application of repurposed drugs in optimal combinations with the use of specific carriers for their targeted delivery. As a result, new optimized medications with reduced side effects can be obtained. In this study, two known anticancer drugs, celecoxib and/or simvastatin, were conjugated covalently with PAMAM G3 dendrimer and tested in vitro against human squamous carcinoma (SCC-15-15) and glioblastoma (U-118 MG) cells, as well as normal human fibroblasts (BJ). The obtained conjugates were also substituted with biotin and R-glycidol to increase their affinity for cancer cells and were characterized with NMR spectroscopy and dynamic light scattering technique. Conjugates furnished with two celecoxib and four simvastatin residues revealed the very high effectiveness and dramatically decreased the SCC-15 and U-118 MG cell viability at very low concentrations with IC50 equal to about 3 μM. Its action was 20–50-fold stronger than that of either drug alone or as a mixture. Combined conjugate revealed also additive action since it was 2–8-fold more effective than conjugates with either single drug. The combined conjugate revealed rather low specificity since it was also highly cytotoxic for BJ cells. Despite this, it may be concluded that biotinylated and R-glycidylated PAMAM G3 dendrimers substituted with both celecoxib and simvastatin can be considered as a new perspective anticancer agent, effective in therapy of malignant, incurable glioblastomas.

Keywords: drug delivery system ; biotinylated ; R-glycidylated PAMAM G3 dendrimers ; celecoxib ; simvastatin ; molecular size ; cytotoxicity ; human squamous carcinoma (SCC-15-15) ; human glioblastoma (U-118 MG) ; normal human fibroblasts (BJ)

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Product Details of [ 35013-72-0 ]

CAS No. :35013-72-0 MDL No. :
Formula : C14H19N3O5S Boiling Point : -
Linear Structure Formula :C2H4C2O2NOCO(CH2)4C5H7N2OS InChI Key :YMXHPSHLTSZXKH-RVBZMBCESA-N
M.W : 341.38 Pubchem ID :6710714
Synonyms :
Chemical Name :2,5-Dioxopyrrolidin-1-yl 5-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanoate

Calculated chemistry of [ 35013-72-0 ]      Expand+

Physicochemical Properties

Num. heavy atoms : 23
Num. arom. heavy atoms : 0
Fraction Csp3 : 0.71
Num. rotatable bonds : 7
Num. H-bond acceptors : 5.0
Num. H-bond donors : 2.0
Molar Refractivity : 93.18
TPSA : 130.11 ?2

Pharmacokinetics

GI absorption : High
BBB permeant : No
P-gp substrate : Yes
CYP1A2 inhibitor : No
CYP2C19 inhibitor : No
CYP2C9 inhibitor : No
CYP2D6 inhibitor : No
CYP3A4 inhibitor : No
Log Kp (skin permeation) : -8.55 cm/s

Lipophilicity

Log Po/w (iLOGP) : 1.7
Log Po/w (XLOGP3) : -0.23
Log Po/w (WLOGP) : -0.82
Log Po/w (MLOGP) : 1.29
Log Po/w (SILICOS-IT) : 0.48
Consensus Log Po/w : 0.48

Druglikeness

Lipinski : 0.0
Ghose : None
Veber : 0.0
Egan : 0.0
Muegge : 0.0
Bioavailability Score : 0.55

Water Solubility

Log S (ESOL) : -1.35
Solubility : 15.3 mg/ml ; 0.0447 mol/l
Class : Very soluble
Log S (Ali) : -2.04
Solubility : 3.08 mg/ml ; 0.00902 mol/l
Class : Soluble
Log S (SILICOS-IT) : -2.17
Solubility : 2.3 mg/ml ; 0.00675 mol/l
Class : Soluble

Medicinal Chemistry

PAINS : 0.0 alert
Brenk : 2.0 alert
Leadlikeness : 0.0
Synthetic accessibility : 4.07

Safety of [ 35013-72-0 ]

Signal Word:Warning Class:N/A
Precautionary Statements:P261-P280-P305+P351+P338 UN#:N/A
Hazard Statements:H302+H312+H332-H315-H319-H335 Packing Group:N/A
GHS Pictogram:

Application In Synthesis of [ 35013-72-0 ]

* All experimental methods are cited from the reference, please refer to the original source for details. We do not guarantee the accuracy of the content in the reference.

  • Downstream synthetic route of [ 35013-72-0 ]

[ 35013-72-0 ] Synthesis Path-Downstream   1~6

  • 1
  • [ 35013-72-0 ]
  • [ 576-19-2 ]
YieldReaction ConditionsOperation in experiment
D-Biotin (1 gm) was dissolved at 48.8 mg/ml in DW. NHS (0.5 gm) was dissolved at 92 mg/ml in DMF and added to the biotin. Solid EDAC at ~ 4-fold excess (3.1 gm) was added as powder to the NHS/Biotin mix, while stirring rapidly. The reaction was allowed to proceed for 20 mins. At this stage complexes of Lysyl-Copper-Lysine at 100 mg/ml in 1% NaHCCbeta (5.8 gm in 58 ml) was added to Biotin-NHS and reacted overnight. The reaction mix was precipitated with acetone to 70% and then the pellet was dissolved in 100 ml 50 mM EDTA. The soluble material was loaded onto Dowex 1 X 2 resin. All of the Lys-C-Lys stuck to the column. The biocytin in the flow through was loaded onto XAD- 16 resin and washed with DW. Residual Lys-Cu-Lys washed through. The biocytin was eluted with 4 x 100 ml 75% MeOH. After which the product was rotary evaporated, resuspended in distilled water and lyophilized. Mass spectral analysis of biocytin showed a Molecular ion of 373.
  • 3
  • [ 35013-72-0 ]
  • [ 60-32-2 ]
  • [ 72040-64-3 ]
YieldReaction ConditionsOperation in experiment
75% In N,N-dimethyl-formamide; at 20℃; biotin-NHS (1 eq., 388 mg, 1.14 mmol) was dissolved in the anhydrous DMF (8.54 mL). To the resulting solution was added 6-aminocaproic acid (1 eq., 149 mg, 1.14 mmol) andthe mixture was stirred at r.t. overnight and then concentrated to yield 1:1 mixture of the product and NHS. To the product was then added 95:1 :4 mixture of EtOH-AcOH-H20. The resulting suspension was heated to boiling, filtered, and left to crystallize to yield compound 9 (305 mg, 0.854 mmol, 75 percent) as a white fluffy solid. The structure of 9 was confirmed by ESI-MS analysis (Method 1).ESI-MS m/z: 358.3 [M+H]
1.455 g With sodium hydrogencarbonate; In water; N,N-dimethyl-formamide; at 20℃; for 16h; epsilon-Aminocaproic acid (966mg, 8.4mmol) was dissolved in 30mL 1M aqueous NaHCO3 solution. Then N-hydroxysuccinimidobiotin (3.09g) in 35mL DMF was added dropwise to the solution and the mixture was stirred at room temperature for 16h. The solution was concentrated under reduced pressure to remove partial solvent and 150mL aqueous citric acid (100g/L) was then added and stirred at 60°C for 30min. The precipitate was collected by filtration and washed with distilled water. The precipitate was dissolved in a mixture of isopropanol and water (8:2, v/v) and kept at 4°C to give pure 3 (1.455g, 50percent) as a yellowish crystal; IR cm?1 (KBr): 3200?3500, 3070, 2932, 2859, 1696, 1644, 1543, 1475, 1391, 1324, 1265, 1118; 1H NMR (600MHz, DMSO-d6): delta 7.75 (1H, t, J=5.4Hz, C6?NH), 6.45 (1H, s, C13?NH), 6.38 (1H, s, C14?NH), 4.35?4.27 (1H, m, H-14), 4.12 (1H, m, H-13), 3.09 (1H, m, H-12), 3.00 (1H, m, H-6) 2.82 (1H, dd, J=12.4, 5.1Hz, H-15a), 2.57 (1H, d, J=12.4Hz, H-15b), 2.19 (2H, t, J=7.4Hz, H-2), 2.04 (2H, t, J=7.3Hz, H-8), 1.20?1.67 (14H, m). 13C NMR (150MHz, DMSO-d6): delta 171.84 (C-1, C-7), 162.74 (C-16), 61.06 (C-13), 59.20 (C-14), 55.44 (C-12), 39.68 (C-15), 38.25 (C-6), 35.21 (C-8), 29.05 (C-2), 28.92, 28.21, 28.04, 26.04, 25.73, 25.36.
368.3 mg With sodium hydrogencarbonate; In water; acetone; at 20℃; for 12h; General procedure: Biotin-NHS was ammonolyzed withlinkers to afford biotin-linker products [Biotin-AAn-COOH (n = 1, 3, 5, and 7) orBiotin-PEG(n+1)-COOH (n = 1, 2 and 3)]. The linker [AAn (n = 1, 3, 5, and 7) orNH2-PEG(n+1)-COOH (n = 1, 2 and 3), 1 eq.] was dissolved in 4 mL water solutionrespectively, and 240.0 mg NaHCO3 was added to the solution. The reaction mixturewas stirred and the Biotin-NHS (1 eq.) and acetone (500 ul) were added subsequently.After stirring for 12h at room temperature, the solvent was removed by vacuum, andthe crude was dispersed in water, adjusting the pH by 2M HCl to pH=3. The mixturesolution was filtered, washed by water and concentrated under reduced pressure toachieved Biotin-linker products [Biotin-AAn-COOH (n = 1, 3, 5, and 7) orBiotin-PEG(n+1)-COOH (n = 1, 2 and 3)]2, 3.
  • 4
  • [ 67107-87-3 ]
  • [ 35013-72-0 ]
  • [ 1393360-95-6 ]
  • 5
  • [ 29390-67-8 ]
  • [ 35013-72-0 ]
  • [ 1118755-11-5 ]
YieldReaction ConditionsOperation in experiment
72% With triethylamine; In N,N-dimethyl-formamide; at 20℃; for 24h; Biotin succinimidyl ester (7.2 mg, 21.6 mmol) and 6-amino-6-deoxy-beta-CD (20 mg, 17.6 mmol) were dissolved in dry DMF (4 ml), TEA (3 ml, d 0.72) was added, and the reaction mixture was stirred at room temperature for 24 h. The solvent was evaporated to dryness in vacuo. The product was freeze-dried to afford pure product as a white powder. Yield: 72percent.
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