MS 209
- CAS No.
- 158681-49-3
- Chemical Name:
- MS 209
- Synonyms
- MS 209;MS-209 fumarate;Dofequidar fumarate;Dofequidar (sesquifumarate);Dofequidar fumarate >=98% (HPLC);4-(Diphenylacetyl)-a-[(5-quinolinyloxy)methyl]-1-Piperazineethanol (E)-2-butenedioate fumarate (1:1.5);4-(Diphenylacetyl)-alpha-((5-quinolinyloxy)methyl)-1-piperazineethanol (E)-2-butenedioate (2:3) (salt);1-Piperazineethanol, 4-(diphenylacetyl)-alpha-((5-quinolinyloxy)methyl)-, (E)-2-butenedioate (2:3) (salt)
- CBNumber:
- CB81390656
- Molecular Formula:
- C30H31N3O3.C4H4O4
- Molecular Weight:
- 597.664
- MDL Number:
- MOL File:
- 158681-49-3.mol
| storage temp. | -20°C |
|---|---|
| solubility | DMSO: soluble20mg/mL, clear |
| form | powder |
| color | white to beige |
| NCI Dictionary of Cancer Terms | MS 209 |
| FDA UNII | 3DM793MFSE |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |   GHS07,GHS08 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H361-H412 |
| Precautionary statements | P264-P270-P301+P312-P330-P501-P201-P202-P281-P308+P313-P405-P501-P273-P501 |
| WGK Germany | 3 |
MS 209 Chemical Properties,Uses,Production
Uses
Dofequidar (MS-209) sesquifumarate is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar sesquifumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar sesquifumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect[1][2].
in vivo
Dofequidar (200 mg/kg; orally administered; starting from days 10 or 14 after tumor cell inoculation, 4 doses) sesquifumarate in NK cell-depleted SCID mice inoculated with SBC-3/ADM or SBC-3 cells significantly inhibits the metastasis of SBC-3/ADM cells to multiple organs when combined with Etoposide (VP-16) (HY-13629) or Adriamycin[1].
Dofequidar (200 mg/kg; orally administered; given 30 minutes before Irinotecan (CPT-11) (HY-16562) injection, and both are administered on days 0, 4, and 8; throughout the experiment) sesquifumarate in nude mice inoculated with HeLa SP cells significantly reduces the tumor volume when combined with Irinotecan[2].
| Animal Model: | 6- to 8-week-old male severe combined immunodeficiency (SCID) mice, depleted of natural killer (NK) cells by intraperitoneal injection of TM-β1 Ab (1 mg/mouse) 2 days before tumor inoculation, and then inoculated intravenously with SBC-3 or SBC-3/ADM cells[1] |
| Dosage: | 200 mg/kg |
| Administration: | Orally administered; the mice inoculated with SBC-3 cells were treated on days 14, 15, 21, and 22; the mice inoculated with SBC-3/ADM cells were treated on days 10, 11, 17, and 18. |
| Result: | Combined use with Etoposide (VP-16) (HY-13629) or Adriamycin can significantly inhibit metastasis formation by SBC-3/ADM cells to the liver, kidneys, and lymph nodes, and the weight of the liver of the treated mice was significantly less than that of other groups. |
| Animal Model: | 5- to 6-week-old female BALB/c-nu/nu (nude) mice, inoculated subcutaneously with HeLa SP cells[2] |
| Dosage: | 200 mg/kg |
| Administration: | Orally administered 30 minutes before intravenous injection of Irinotecan (67 mg/kg); on days 0, 4, and 8. |
| Result: | Co-treatment with Irinotecan drastically decreased the tumor volume. |
References
[1] Nokihara H, et al. A new quinoline derivative MS-209 reverses multidrug resistance and inhibits multiorgan metastases by P-glycoprotein-expressing human small cell lung cancer cells. Jpn J Cancer Res. 2001 Jul;92(7):785-92. DOI:10.1111/j.1349-7006.2001.tb01162.x
[2] Katayama R, et al. Dofequidar fumarate sensitizes cancer stem-like side population cells to chemotherapeutic drugs by inhibiting ABCG2/BCRP-mediated drug export. Cancer Sci. 2009 Nov;100(11):2060-8. DOI:10.1111/j.1349-7006.2009.01288.x
MS 209 Preparation Products And Raw materials
Raw materials
Preparation Products
MS 209 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49734 | 58 |
| Shanghai Zeye Biotechnology Co., Ltd. | 021-021-61998551 13122364865 | sale1@shzysw.net | China | 9778 | 58 |
| Energy Chemical | 021-58432009 400-005-6266 | marketing@energy-chemical.com | China | 44918 | 58 |
| Biosynth Biological Technology (Suzhou) Co Ltd | 51288865780 | sales@biosynth.com | China | 6051 | 58 |
| Jinan Dingguo Biotechnology Co., Ltd. | 053181181593 | CHINA | 155 | 58 | |
| Guangzhou Junuo Biotechnology Co., Ltd. | 13432975901 | CHINA | 132 | 58 | |
| Guangzhou Squirrel Biotechnology Co., Ltd. | 17765276361 | CHINA | 109 | 58 |
