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[CAS NO. 152946-68-4] Nolatrexed dihydrochloride
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-108474 |
| Brand: | MCE |
| CAS: | 152946-68-4 |
Overview
| MDL | MFCD00917041 |
|---|---|
| Molecular Weight | 357.26 |
| Molecular Formula | C14H14Cl2N4OS |
| SMILES | [H]Cl.O=C1N=C(N)NC2=C1C(SC3=CC=NC=C3)=C(C)C=C2.[H]Cl |
1 Publications Citing Use of MCE
Summary
Nolatrexed dihydrochloride (AG 337) is a non-competitive lipophilic inhibitor of thymidylate synthase , interacts at the folate cofactor binding site of the enzyme, with a K i of 11 nM for human thymidylate synthase [1] . Nolatrexed dihydrochloride (AG 337) induces cell cycle arrest in S phase of cancer cells. Anti-cancer activity [2] .
IC50 & Target
Ki: 11 nM (Human Thymidylate Synthase) [1]
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00012324 | Eximias Pharmaceutical|National Cancer Institute (NCI) |
Liver Cancer
|
September 2000 | Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 50 mg/mL ( 139.95 mM ; Need ultrasonic)
DMSO : 41.67 mg/mL ( 116.64 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.7991 mL | 13.9954 mL | 27.9908 mL |
| 5 mM | 0.5598 mL | 2.7991 mL | 5.5982 mL |
| 10 mM | 0.2799 mL | 1.3995 mL | 2.7991 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 25 mg/mL (69.98 mM); Clear solution; Need ultrasonic and warming
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution
References
- [1] Webber S, et al. AG337, a novel lipophilic thymidylate synthase inhibitor: in vitro and in vivo preclinical studies. Cancer Chemother Pharmacol. 1996;37(6):509-17.
- [2] McGuire JJ, et al. Characterization of the effect of AG337, a novel lipophilic thymidylate synthase inhibitor, on human head and neck and human leukemia cell lines.
Synonyms
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