research use only
Cat.No.S1497
| Related Targets | Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism |
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| Other DHFR Inhibitors | Calcium Folinate Aminopterin Diaveridine |
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | PMID |
|---|---|---|---|---|---|---|
| human KB cells | Growth inhibition assay | 96 h | Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay, IC50=0.47 nM | |||
| Chinese hamster R2 cells | Growth inhibition assay | 96 h | Growth inhibition of Chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTiter-blue assay, IC50=0.057 μM | |||
| Click to View More Cell Line Experimental Data | ||||||
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In vitro |
DMSO
: 28 mg/mL
(58.64 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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| Molecular Weight | 477.47 | Formula | C23H23N7O5 |
Storage (From the date of receipt) | |
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| CAS No. | 146464-95-1 | Download SDF | Storage of Stock Solutions |
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| Synonyms | NSC 754230 | 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 | ||
Read more about storage stability stock solution CAS number SMILES
| Targets/IC50/Ki |
DHFR
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| In vitro |
Pralatrexate and bortezomib exhibits concentration- and time-dependent cytotoxicity against a broad panel of T-lymphoma cell lines. This compound shows synergism when combined with bortezomib in all cell lines studied. It also induces potent apoptosis and caspase activation when combined with bortezomib across the panel. The agent significantly modulates the expression of p27, NOXA, HH3, and RFC-1 as assessed by Western blot assays. This compound is rationally designed for improved cellular transport via RFC-1, and to have greater intracellular drug retention through the enhanced formation of polyglutamylated conjugates. It is thought to exert its pharmacological effect primarily through inhibition of DHFR, having an IC50 in the picomolar range. This chemical demonstrates superior intracellular transport via the reduced folate carrier, and increased accumulation within cells by enhanced polyglutamylation. It exhibits antitumor activity that is superior to the activity of other antifolates. Its enhanced activity relative to methotrexate (MTX) is due to its much more rapid rate of transport and polyglutamation, the former less important when the carrier is saturated.
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| In vivo |
Pralatrexate treatment results in treatment-related toxicity in MV522 mice models, as determined by significant weight loss in some animals prior to death; however, remaining mice regains all lost weight by Day 35.
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References |
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(data from https://clinicaltrials.gov, updated on 2026-05-11)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT07225985 | RECRUITING | Recurrent T-Cell Non-Hodgkin Lymphoma; Refractory T-Cell Non-Hodgkin Lymphoma |
Fred Hutchinson Cancer Center |
2026-04-27 | PHASE1; PHASE2 |
| NCT06072131 | RECRUITING | Peripheral T Cell Lymphoma |
Acrotech Biopharma Inc. |
2023-10-04 | PHASE3 |
| NCT07691450 | NOT_YET_RECRUITING | Recurrent Anaplastic Large Cell Lymphoma; Recurrent Enteropathy-Associated T-Cell Lymphoma; Recurrent Follicular Helper T-Cell Lymphoma; Recurrent Follicular Helper T-Cell Lymphoma, Angioimmunoblastic-Type; Recurrent Follicular Helper T-Cell Lymphoma, Follicular-Type; Recurrent Follicular Helper T-Cell Lymphoma, Not Otherwise Specified; Recurrent Hepatosplenic T-Cell Lymphoma; Recurrent Mature T-Cell and NK-Cell Non-Hodgkin Lymphoma; Recurrent Monomorphic Epitheliotropic Intestinal T-cell Lymphoma; Recurrent Peripheral T-Cell Lymphoma, Not Otherwise Specified; Recurrent Primary Cutaneous CD8-Positive Aggressive Epidermotropic Cytotoxic T-Cell Lymphoma; Recurrent Primary Cutaneous Gamma-Delta T-Cell Lymphoma; Recurrent Subcutaneous Panniculitis-Like T-Cell Lymphoma; Refractory Anaplastic Large Cell Lymphoma; Refractory Enteropathy-Associated T-Cell Lymphoma; Refractory Follicular Helper T-Cell Lymphoma; Refractory Follicular Helper T-Cell Lymphoma, Angioimmunoblastic-Type; Refractory Follicular Helper T-Cell Lymphoma, Follicular-Type; Refractory Follicular Helper T-Cell Lymphoma, Not Otherwise Specified; Refractory Hepatosplenic T-Cell Lymphoma; Refractory Mature T-Cell and NK-Cell Non-Hodgkin Lymphoma; Refractory Monomorphic Epitheliotropic Intestinal T-cell Lymphoma; Refractory Peripheral T-Cell Lymphoma, Not Otherwise Specified; Refractory Primary Cutaneous CD8-Positive Aggressive Epidermotropic Cytotoxic T-Cell Lymphoma; Refractory Primary Cutaneous Gamma-Delta T-Cell Lymphoma; Refractory Subcutaneous Panniculitis-Like T-Cell Lymphoma |
City of Hope Medical Center |
2027-01-03 | PHASE1 |
| NCT04747236 | RECRUITING | PTCL |
University of Virginia |
2021-02-19 | PHASE2 |
| NCT06561048 | RECRUITING | Peripheral T-Cell Lymphoma, Not Otherwise Specified; Angioimmunoblastic T-cell Lymphoma; Follicular T-Cell Lymphoma; Nodal Peripheral T-Cell Lymphoma With TFH Phenotype; Systemic Anaplastic Large Cell Lymphoma; Lymphoma, T-Cell, Peripheral; Lymphoma, T-Cell |
Corvus Pharmaceuticals, Inc. |
2024-10-02 | PHASE3 |
| NCT06671717 | NOT_YET_RECRUITING | Relapsed Peripheral T-Cell Lymphoma; Refractory Peripheral T-Cell Lymphoma |
Peking University People's Hospital |
2024-12 |
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Question 1:
We are just wondering if it is a racemic mixture or a monomer? Will you please let us know?
Answer:
It is the S enantiomer.