| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Tubublin; microtubule depolymerization
|
|---|---|
| References | |
| Additional Infomation |
Stimulation-triggered drug release and increased drug loading are two key prerequisites for the fabrication of nanomedicine delivery systems. This paper presents the first Pluronic P123-d-hyd-DTX/DTX complex micelles that integrate a high pH sensitivity strategy and a dual drug loading mode into a single platform. We synthesized the Pluronic P123-d-hyd-DTX conjugate (P123-d-hyd-DTX) for the first time by linking DTX to the PEO chain of P123 via two hydrazone bonds on the main chain. Increasing the number of hydrazone bonds in the unimolecular conjugate enhances the pH sensitivity of the conjugate micelles. Furthermore, to improve drug loading, a dual drug loading strategy (chemical coupling and physical encapsulation) was employed. Specifically, P123-d-hyd-DTX/DTX composite micelles were prepared by further encapsulating DTX using pH-sensitive P123-d-hyd-DTX as a carrier. The resulting P123-d-hyd-DTX/DTX micelles were perfectly spherical with a uniform particle size distribution (110.37 nm) and a high drug loading (12.64%). In vitro release experiments confirmed that both the P123-d-hyd-DTX/DTX micelles and the P123-d-hyd-DTX micelles (as a control) exhibited highly pH-responsive release characteristics. Especially at pH 6.5, the release rates of DTX within 48 hours were approximately 90.9% and 75%, respectively. Compared with P123-d-hyd-DTX micelles, P123-d-hyd-DTX/DTX complex micelles showed stronger inhibitory effects on the proliferation of B16F10 cells (p < 0.01), but their cytotoxicity was slightly lower than that of free DTX (p < 0.05). In the B16F10 melanoma xenograft model, P123-d-hyd-DTX/DTX complex micelles were superior to Duopafei® (p < 0.01) and P123-d-hyd-DTX micelles (p < 0.05) in inhibiting tumor growth, and no significant adverse reactions were observed. In summary, this novel polymer complex micelle based on dual hydrazone bonds and a dual drug loading strategy is a promising drug delivery platform that is expected to improve the efficacy of cancer treatment and reduce side effects. [1]
|
| Molecular Formula |
C48H59NO16
|
|---|---|
| Exact Mass |
905.383
|
| CAS # |
1234218-62-2
|
| PubChem CID |
161734498
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
1.8
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
16
|
| Rotatable Bond Count |
18
|
| Heavy Atom Count |
65
|
| Complexity |
1910
|
| Defined Atom Stereocenter Count |
11
|
| SMILES |
CC1=C2[C@H](C(=O)[C@@]3([C@H](C[C@@H]4[C@]([C@H]3[C@@H]([C@@](C2(C)C)(C[C@@H]1OC(=O)[C@@H]([C@H](C5=CC=CC=C5)NC(=O)OC(C)(C)C)OC(=O)CCC(=O)C)O)OC(=O)C6=CC=CC=C6)(CO4)OC(=O)C)O)C)O
|
| InChi Key |
XKHDVNYIFGGXRE-LEPVCIIKSA-N
|
| InChi Code |
InChI=1S/C48H59NO16/c1-25(50)20-21-33(53)62-37(35(28-16-12-10-13-17-28)49-43(58)65-44(4,5)6)42(57)61-30-23-48(59)40(63-41(56)29-18-14-11-15-19-29)38-46(9,39(55)36(54)34(26(30)2)45(48,7)8)31(52)22-32-47(38,24-60-32)64-27(3)51/h10-19,30-32,35-38,40,52,54,59H,20-24H2,1-9H3,(H,49,58)/t30-,31-,32+,35-,36+,37+,38-,40-,46+,47-,48+/m0/s1
|
| Chemical Name |
[(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4-acetyloxy-1,9,12-trihydroxy-10,14,17,17-tetramethyl-15-[(2R,3S)-3-[(2-methylpropan-2-yl)oxycarbonylamino]-2-(4-oxopentanoyloxy)-3-phenylpropanoyl]oxy-11-oxo-6-oxatetracyclo[11.3.1.03,10.04,7]heptadec-13-en-2-yl] benzoate
|
| Synonyms |
Sudocetaxel; 1234218-62-2; [(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4-Acetyloxy-1,9,12-trihydroxy-10,14,17,17-tetramethyl-15-[(2R,3S)-3-[(2-methylpropan-2-yl)oxycarbonylamino]-2-(4-oxopentanoyloxy)-3-phenylpropanoyl]oxy-11-oxo-6-oxatetracyclo[11.3.1.03,10.04,7]heptadec-13-en-2-yl] benzoate;
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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