research use only
Cat.No.S7930
| Related Targets | Akt Wnt/beta-catenin PKC HSP ROCK Integrin Bcr-Abl Actin FAK Kinesin |
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| Other Microtubule Associated Inhibitors | Nocodazole MMAF Patupilone (Epothilone B) Lexibulin (CYT997) CW069 Combretastatin A4 Epothilone A ABT-751 (E7010) TAI-1 Cucurbitacin B |
| Molecular Weight | 506.70 | Formula | C27H42N2O5S |
Storage (From the date of receipt) | |
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| CAS No. | 219989-84-1 | Download SDF | Storage of Stock Solutions |
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| Synonyms | Azaepothilone B, BMS-247550, Aza-epothilone B | Smiles | CC1CCCC2(C(O2)CC(NC(=O)CC(C(C(=O)C(C1O)C)(C)C)O)C(=CC3=CSC(=N3)C)C)C | ||
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In vitro |
DMSO
: 100 mg/mL
(197.35 mM)
Ethanol : 47 mg/mL Water : Insoluble |
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In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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| Targets/IC50/Ki |
microtubule(tubulin stabilising)
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| In vitro |
BMS-247550 is a highly potent cytotoxic agent capable of killing cancer cells at low nanomolar concentrations and retains its antineoplastic activity against human cancers that are naturally insensitive to paclitaxel or that have developed resistance to paclitaxel. |
| In vivo |
In vivo, BMS-247550 has clearly demonstrated antitumor activity that is superior to paclitaxel in both paclitaxel-resistant and -sensitive tumours. BMS-247550 is more efficacious than paclitaxel in all five paclitaxel-resistant tumours evaluated in this study (four human and one murine): i.e., the clinically derived paclitaxel resistant Pat-7 ovarian carcinoma, the A2780Tax ovarian carcinoma that is resistant to paclitaxel because of tubulin mutations, the HCT116/VM46 MDR colon carcinoma, the clinically derived paclitaxel-resistant Pat-21 breast carcinoma, and the murine fibrosarcoma M5076. Against three paclitaxel-sensitive human tumour xenografts, BMS-247550 produces antitumor activity equivalent to paclitaxel: i.e., A2780 human ovarian carcinoma, HCT116, and LS174T human colon carcinoma. |
References |
(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03093155 | Completed | Epithelial Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Cancer |
Yale University|R-Pharm-US LLC |
April 3 2017 | Phase 2 |
| NCT01454479 | Unknown status | Recurrent Endometrial Cancer |
Hung-Hsueh Chou|GlaxoSmithKline|Bristol-Myers Squibb|Chang Gung Memorial Hospital |
March 2011 | Phase 1 |
| NCT01012362 | Terminated | Breast Cancer|Lung Cancer|Colon Cancer|Pancreatic Cancer|Head and Neck Cancer|Kidney Cancer|Sarcoma|Hepatocellular Cancer |
Masonic Cancer Center University of Minnesota|GlaxoSmithKline |
December 2009 | Phase 1 |
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