MS 209
- Product Name
- 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
- Formula Weight
- 597.664
- MOL File
- 158681-49-3.mol
MS 209 Property
- storage temp.
- -20°C
- solubility
- DMSO: soluble20mg/mL, clear
- form
- powder
- color
- white to beige
Safety
- WGK Germany
- 3
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H361Suspected of damaging fertility or the unborn child
H412Harmful to aquatic life with long lasting effects
- Precautionary statements
-
P201Obtain special instructions before use.
P202Do not handle until all safety precautions have been read and understood.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P273Avoid release to the environment.
P281Use personal protective equipment as required.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P308+P313IF exposed or concerned: Get medical advice/attention.
P330Rinse mouth.
P405Store locked up.
P501Dispose of contents/container to..…
MS 209 Chemical Properties,Usage,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
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