- Pemetrexed disodium hemipenta hydrate
- Methotrexate
- Pyrimethamine
- Pemetrexed
| PralatrexateAntifolate,a folate analog |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Cell experiment [1,2]: | |
Cell lines | Cancer cell lines, NCI-H460 human NSCLC cells, MV522 human metastatic human NSCLC cells |
Preparation method | The solubility of this compound in DMSO is > 23.9 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 72h |
Applications | Pralatrexate showed antiproliferative activity against 15 cancer cell lines with the IC50 values ranged from 0.01 ± 0.002 μM for the prostate cancer cell line PC3 to > 350 μM for the MDA-MB-435 cell line. Pralatrexate dose-dependently inhibited the activity of DHFR. In NCI-H460 cells, treatment with pralatrexate for 15 or 60 min resulted in a short-term uptake of radiolabeled antifolates. |
| Animal experiment [1]: | |
Animal models | Female nude mice (nu/nu) bearing NCI-H460 or MV522 tumor cells |
Dosage form | Intraperitoneal injection, 1 and 2 mg/kg, every day×5, for two cycles of 5 days |
Application | In MV522 human non-small cell lung cancer (NSCLC) xenograft, pralatrexate showed increased antitumor activity. In the 2 mg/kg pralatrexate-treated group, the 38% tumor growth inhibition (TGI) was observed. In NCI-H460 NSCLC xenograft, pralatrexate showed antitumor activity in a dose-dependent way. TGI of 1 mg/kg and 2 mg/kg pralatrexate-treated groups was 34% and 52%, respectively. In NCI-H460 and MV522 human tumor xenografts, pralatrexate resulted in dose-dependent weight loss, which suggested its toxicity. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Izbicka E, Diaz A, Streeper R, et al. Distinct mechanistic activity profile of pralatrexate in comparison to other antifolates in in vitro and in vivo models of human cancers[J]. Cancer chemotherapy and pharmacology, 2009, 64(5): 993-999. [2]. Serova M, Bieche I, Sablin M P, et al. Single agent and combination studies of pralatrexate and molecular correlates of sensitivity[J]. British journal of cancer, 2011, 104(2): 272. | |
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| Cas No. | 146464-95-1 | SDF | Download SDF |
| Chemical Name | (2S)-2-[[4-[1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl]amino]pentanedioic acid | ||
| Canonical SMILES | C#CCC(CC1=CN=C2C(=N1)C(=NC(=N2)N)N)C3=CC=C(C=C3)C(=O)NC(CCC(=O)O)C(=O)O | ||
| Formula | C23H23N7O5 | M.Wt | 477.47 |
| Solubility | ≥23.85 mg/mL in DMSO, <2.4 mg/ml="" in="" etoh,=""><2.29 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Pralatrexate is an inhibitor of DHFR with Ki value of 45 nM [1].
Dihydrofolate reductase (DHFR) is an enzyme that reduces dihydrofolic acid to tetrahydrofolic acid, a methyl group shuttle required for the synthesis of purines, thymidylic acid, and certain amino acids.
Pralatrexate is a DHFR inhibitor with high affinity for folylpolyglutamate synthetase (FPGS) and reduced folate carrier 1 (RFC-1), resulting in extensive internalization and accumulation in tumour cells. In 15 human cancer cell lines, pralatrexate showed antiproliferative effects with IC50 < 0.1="" μm="" in="" pc3,="" scc61,="" du145,="" ht29,="" hop62,="" sq20b,="" hop92,="" hep2="" and="" igrov1="" cells.="" while="" it="" showed="" antiproliferative="" effects="" with="" ic50≥="" 9="" μm="" in="" colo205,="" hcc2998,="" mcf7,="" hct116,="" ovcar3="" and="" mda-mb-435="" cells="">
In MV522 human non-small cell lung cancer (NSCLC) xenograft, pralatrexate showed increased antitumor activity. In the 2 mg/kg pralatrexate-treated group, the 38% tumor growth inhibition (TGI) was observed. In NCI-H460 NSCLC xenograft, pralatrexate showed antitumor activity in a dose-dependent way. TGI of 1 mg/kg and 2 mg/kg pralatrexate-treated groups was 34% and 52%, respectively. In the two xenografts, pralatrexate resulted in weight loss, which suggested its toxicity [1].
References:[1]. Izbicka E, Diaz A, Streeper R, et al. Distinct mechanistic activity profile of pralatrexate in comparison to other antifolates in in vitro and in vivo models of human cancers. Cancer Chemother Pharmacol, 2009, 64(5): 993-999. [2]. Serova M, Bieche I, Sablin MP, et al. Single agent and combination studies of pralatrexate and molecular correlates of sensitivity. Br J Cancer, 2011, 104(2): 272-280.
