| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
ABT-751 hydrochloride (2 μM; 4, 8, 24h) disrupts mitosis, disrupts mitochondrial membrane potential, induces ROS generation and DNA damage in hepatocellular carcinoma-derived Hep-3B cells[9]. ABT-751 hydrochloride (2 μM; 4, 8, 24h) can cause DNA damage, inhibit cell proliferation and induce G2/M cell cycle arrest in Hep-3B cells[9]. ABT-751 hydrochloride (2 μM; 4, 8, 24h) induces autophagy in TP53-deficient Hep-3B cells by inhibiting the AKT/MTOR signaling pathway, and induces apoptosis through caspase-dependent, extrinsic and intrinsic pathways. When the TP53 gene is exogenously expressed, the autophagy and apoptosis of these cells induced by ABT-751 are further increased[9].
|
|---|---|
| ln Vivo |
ABT-751 hydrochloride (100 mg/kg/day, oral, 5 days on, 5 days off x2, 21 days) has a significant inhibitory effect in neuroblastoma models. In rhabdomyosarcoma and Wilms tumor models, Can induce significant reduction or regression of tumor size. ABT-751 has a synergistic effect on Vincristine and Paclitaxel (HY-B0015) [7]. ABT-751 hydrochloride (100 mg/kg/day, oral, 5 days on, 5 days off x2) is synergistic with Docetaxel (HY-B0011) in mouse prostate, non-small cell lung cancer, and breast tumor xenograft models , improve the inhibitory effect on tumors [8].
|
| Animal Protocol |
Animal/Disease Models:xenograft models of neuroblastoma, osteosarcoma, Ewing sarcoma rhabdomyosarcoma, medulloblastoma and eight kidney cancer lines (six Wilms tumors, two rhabdoid)[7]
Doses: 100 mg/kg Route of Administration: Oral gavage (p.o.) Experimental Results: Had obvious inhibitory effect in neuroblastoma model. Induced significant reduction or regression of tumor volume in rhabdomyosarcoma and nephroblastoma models. Had a synergistic effect on vincristine or Paclitaxel (HY-B0015). |
| References |
|
| Molecular Formula |
C18H18CLN3O4S
|
|---|---|
| Molecular Weight |
407.87
|
| Exact Mass |
407.071
|
| CAS # |
141450-48-8
|
| PubChem CID |
11983308
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
5.369
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
27
|
| Complexity |
523
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
KWQWWUXRGIIBAS-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C18H17N3O4S.ClH/c1-25-15-8-10-16(11-9-15)26(23,24)21-17-3-2-12-19-18(17)20-13-4-6-14(22)7-5-13;/h2-12,21-22H,1H3,(H,19,20);1H
|
| Chemical Name |
N-[2-(4-hydroxyanilino)pyridin-3-yl]-4-methoxybenzenesulfonamide;hydrochloride
|
| Synonyms |
E7010 hydrochloride
|
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4518 mL | 12.2588 mL | 24.5176 mL | |
| 5 mM | 0.4904 mL | 2.4518 mL | 4.9035 mL | |
| 10 mM | 0.2452 mL | 1.2259 mL | 2.4518 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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