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CAS RN: 112887-68-0 | Product Number: R0208
Raltitrexed
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Purity: >98.0%(HPLC)
Synonyms:
- N-[[5-[[(1,4-Dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl]methylamino]-2-thienyl]carbonyl]-L-glutamic Acid
- ZD-1694
- ICI-D-1694
Product Documents:
| Size | Unit Price | Belgium | Japan* | Quantity |
|---|---|---|---|---|
| 50MG |
€146.00
|
1 | 29 |
|
| 250MG |
€466.00
|
Contact Us | 22 |
|
*Stock available in Belgium will be delivered in 1 to 3 days
*Stock available in Japan will be delivered in 1 to 2 weeks (excludes regulated items and dry ice shipments).
| Product Number | R0208 |
| Purity / Analysis Method | >98.0%(HPLC) |
| Molecular Formula / Molecular Weight | C__2__1H__2__2N__4O__6S = 458.49 |
| Physical State (20 deg.C) | Solid |
| Storage Temperature | Frozen (<0°C) |
| Condition to Avoid | Heat Sensitive |
| CAS RN | 112887-68-0 |
| Reaxys Registry Number | 4359638 |
| PubChem Substance ID | 468592784 |
| Merck Index (14) | 8099 |
| MDL Number | MFCD00864168 |
Specifications
| Appearance | White to Light yellow powder to crystal |
| Purity(HPLC) | min. 98.0 area% |
| Purity(Neutralization titration) | min. 97.0 % |
| Specific rotation [a]20/D | -15.0 to -20.0 deg(C=1,MeOH) |
| NMR | confirm to structure |
Properties (reference)
| Melting Point | 176 °C(dec.) |
| Specific Rotation | -17° (C=1,MeOH) |
| Solubility in water | Soluble |
GHS
| Pictogram |
|
| Signal Word | Danger |
| Hazard Statements | H301 : Toxic if swallowed. H360 : May damage fertility or the unborn child. |
| Precautionary Statements | P501 : Dispose of contents/ container to an approved waste disposal plant. P201 : Obtain special instructions before use. P264 : Wash skin thoroughly after handling. P280 : Wear protective gloves/ protective clothing/ eye protection/ face protection/ hearing protection. P308 + P313 : IF exposed or concerned: Get medical advice/ attention. P301 + P310 + P330 : IF SWALLOWED: Immediately call a POISON CENTER/doctor. Rinse mouth. |
Related Laws:
| RTECS# | MA1253250 |
Transport Information:
| UN Number | UN2811 |
| Class | 6.1 |
| Packing Group | III |
| HS Number | 2934999090 |
Application
Raltitrexed: A Thymidylate Synthase (TS) Inhibitor
Raltitrexed (or ZD1694) is a quinazoline-based folate analogue that selectively inhibits thymidylate synthase (TS). TS is a folate [F0043]-dependent enzyme that catalyzes the reductive methylation of 2'-deoxyuridine-5'-monophosphate (dUMP) [D3673] to 2'-deoxythymidine-5'-monophosphate (dTMP) [T0845, Na salt]. This pathway is crucial for DNA synthesis, because TS is a key enzyme in the synthesis of thymidine-5’-triphosphate (dTTP) which is required exclusively for DNA synthesis. The inhibition of TS leads to DNA fragmentation and cell death. Therefore, TS represents a critical target in cancer chemotherapy. In clinical studies, raltitrexed is also used in combination with other antitumor agents. (The product is for research purpose only.)
References
- ZD1694 (Tomudex): a new thymidylate synthase inhibitor with activity in colorectal cancer
- Mechanisms of acquired resistance to the quinazoline thymidylate synthase inhibitor ZD1694 (Tomudex) in one mouse and three human cell lines
- Raltitrexed: a review of its pharmacological properties and clinical efficacy in the management of advanced colorectal cancer
- Raltitrexed in mesothelioma (a review)
- Determination of raltitrexed in human plasma by high performance liquid chromatography-electrospray ionization-mass spectrometry
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