(S)-Pralatrexate
(S)-Pralatrexate is an orally active anticancer compound. (S)-Pralatrexate exhibits cytotoxic activity against cancer cells and possesses anti-inflammatory activity. (S)-Pralatrexate can be used in research related to prostate cancer, breast cancer, rheumatoid arthritis, etc.
For research use only. We do not sell to patients.
- CAS No.: 1320211-69-5
- Formula: C23H23N7O5
- Molecular Weight:477.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SK-BR-3 | IC50 |
11.9 nM
|
Inhibition of cell growth against human SKBR-3 breast cancer cells assessed via MTS assay, following 3-hour treatment with (S)-Pralatrexate and additional 72-hour incubation in growth medium.
Inhibition of cell growth against human SKBR-3 breast cancer cells assessed via MTS assay, following 3-hour treatment with (S)-Pralatrexate and additional 72-hour incubation in growth medium.
|
US20110190305A1 |
| MDA-MB-435 | IC50 |
100 nM
|
Inhibition of cell growth against human MDA-MB-435 melanoma cells assessed via MTS assay, following 3-hour treatment with (S)-Pralatrexate and additional 72-hour incubation in growth medium.
Inhibition of cell growth against human MDA-MB-435 melanoma cells assessed via MTS assay, following 3-hour treatment with (S)-Pralatrexate and additional 72-hour incubation in growth medium.
|
US20110190305A1 |
| NCI-H460 | IC50 |
289 nM
|
Inhibition of cell growth against human NCI-H460 lung cancer cells assessed via MTS assay, following 3-hour treatment with (S)-Pralatrexate and additional 72-hour incubation in growth medium (first assay).
Inhibition of cell growth against human NCI-H460 lung cancer cells assessed via MTS assay, following 3-hour treatment with (S)-Pralatrexate and additional 72-hour incubation in growth medium (first assay).
|
US20110190305A1 |
| NCI-H460 | IC50 |
169.3 nM
|
Inhibition of cell growth against human NCI-H460 lung cancer cells assessed via MTS assay, following 3-hour treatment with (S)-Pralatrexate and additional 72-hour incubation in growth medium (repeat assay).
Inhibition of cell growth against human NCI-H460 lung cancer cells assessed via MTS assay, following 3-hour treatment with (S)-Pralatrexate and additional 72-hour incubation in growth medium (repeat assay).
|
US20110190305A1 |
| CWR22R | IC50 |
13.3 nM
|
Inhibition of cell growth against human CWR22-RV1 prostate cancer cells assessed via MTS assay, following 3-hour treatment with (S)-Pralatrexate and additional 72-hour incubation in growth medium.
Inhibition of cell growth against human CWR22-RV1 prostate cancer cells assessed via MTS assay, following 3-hour treatment with (S)-Pralatrexate and additional 72-hour incubation in growth medium.
|
US20110190305A1 |
In Vitro
(S)-Pralatrexate (PDX-10a) (3 pM-10 μM; 3 h) potently inhibits growth of SKBR-3 human breast cancer cells (IC50 = 11.9 nM), MDA-MB-435 human melanoma cells (IC50 = 100 nM), NCI-H460 human lung cancer cells (IC50 = 289 nM, 169.3 nM), and CWR22-RV1 human prostate cancer cells (IC50 = 13.3 nM) in a dose-dependent manner in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SKBR-3 human breast cancer cells, MDA-MB-435 human melanoma cells, NCI-H460 human lung cancer cells, CWR22-RV1 human prostate cancer cells
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Concentration:3 pM-10 μM
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Incubation Time:3 h
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Result:Inhibited cell growth in SKBR-3 breast cancer cells with an IC50 of 11.9 nM.
Inhibited cell growth in MDA-MB-435 melanoma cells with an IC50 of 100 nM.
Inhibited cell growth in NCI-H460 lung cancer cells with an IC50 of 289 nM in the first assay and 169 nM in the repeat assay.
Inhibited cell growth in CWR22-RV1 prostate cancer cells with an IC50 of 13.3 nM.
Exhibited dose-dependent responses across all cell lines.
In Vivo
(S)-Pralatrexate exhibits enhanced prophylactic antiarthritic efficacy relative to racemic PDX and/or PDX-10b in a Type II collagen-induced rheumatoid arthritis model in DBA/1 mice[1].
(S)-Pralatrexate (0.025-0.075 mg/kg; p.o.; daily; 17 days) exhibits enhanced antiarthritic efficacy relative to racemic PDX and/or PDX-10b in a type II collagen-induced rheumatoid arthritis model in female Lewis rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Lewis rats[1]
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Dosage:0.025 mg/kg; 0.05 mg/kg; 0.075 mg/kg
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Administration:p.o.; daily; 17 days
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Result:Showed increased antiarthritic activity relative to racemic PDX and/or PDX-10b for some aspects of arthritis (reduced ankle diameter AUC, reduced final paw weight).
Chemical Information
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CAS No. 1320211-69-5
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Molecular Weight 477.48
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Formula C23H23N7O5
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SMILES
NC=1C2=C(N=CC(C[C@H](CC#C)C3=CC=C(C(N[C@@H](CCC(O)=O)C(O)=O)=O)C=C3)=N2)N=C(N)N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)