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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Metabolic Enzyme & Protease > PralatrexateCAS：146464-95-1
Molecular Formula：C23H23N7O5
Molecular Weight：477.47
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Light yellow to yellow Solid
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| CAS | 146464-95-1 |
| Name | Pralatrexate |
| Molecular Formula | C23H23N7O5 |
| Molecular Weight | 477.47 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00920897 |
| SMILES | O=C(CC[C@H](NC(C1=CC=C(C=C1)C(CC#C)CC2=NC3=C(N=C(N=C3N=C2)N)N)=O)C(O)=O)O |
| Target Point | Antifolate;DHFR |
| Passage | Cell Cycle;DNA Damage/DNA Repair;Metabolic Enzyme&Protease; |
| Background | Pralatrexate is a folic acid analog |
| Biological Activity | Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment[1-4]. |
| IC50 | Ki: 13.4 pM(DHFR)[4] |
| In Vitro | Pralatrexate(100 pM-200 μM; 48-72 hours; T-lymphoma cell lines)treatment exhibits concentration- and time-dependent cytotoxicity against a broad panel of T-lymphoma cell lines. The IC50 values at 48 and 72 hours，respectively，are as follows: H9 cells，1.1 nM and 2.5 nM; P12 cells，1.7 nM and 2.4 nM; CEM cells，3.2 nM and 4.2 nM; PF-382 cells，5.5 nM and 2.7 nM; KOPT-K1 cells，1 nM and 1.7 nM; DND-41 cells，97.4 nM and 1.2 nM; and HPB-ALL cells，247.8 nM and 0.77 nM. HH cells are relatively resistant after 48 hours of exposure，with the IC50 at 72 hours being 2.8 nM[1]. |
| In Vivo | The addition of Pralatrexate(15 mg/kg; intraperitoneal injection; on days 1，4，8，and 11; SCID-beige mice)to Bortezomib(0.5 mg/kg)enhanced efficacy compared with either drug alone[1]. |
| Data Literature Source | [1]. Enrica Marchi，et al. Pralatrexate Is Synergistic With the Proteasome Inhibitor Bortezomib in in Vitro and in Vivo Models of T-cell Lymphoid Malignancies. Clin Cancer Res. 2010 Jul 15;16(14):3648-58. [2]. Francine Foss，et al. Pralatrexate Is an Effective Treatment for Relapsed or Refractory Transformed Mycosis Fungoides: A Subgroup Efficacy Analysis From the PROPEL Study. Clin Lymphoma Myeloma Leuk. 2012 Aug;12(4):238-43. [3]. Karen Kelly，et al. Randomized Phase 2b Study of Pralatrexate Versus Erlotinib in Patients With Stage IIIB/IV Non-Small-Cell Lung Cancer (NSCLC) After Failure of Prior Platinum-Based Therapy. J Thorac Oncol. 2012 Jun;7(6):1041-8. [4]. F M Sirotnak，et al. A New Analogue of 10-deazaaminopterin With Markedly Enhanced Curative Effects Against Human Tumor Xenografts in Mice. Cancer Chemother Pharmacol. 1998;42(4):313-8. |
| Unit | Bottle |
| Specification | 10mg 50mg |
是一种抗叶酸剂，也是一种有效的二氢叶酸还原酶 (DHFR) 抑制剂.具有抗肿瘤活性，可用于复发/难治性 T 细胞淋巴瘤的研究。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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