10-Propargyl-10-deazaaminopterin
- CAS No.
- 146464-95-1
- Chemical Name:
- 10-Propargyl-10-deazaaminopterin
- Synonyms
- Pralatrexate;Pdx;Folotyn;CS-2172;Pralatrexat;Prelatrexate;Unii-A8Q8I19Q20;Pralatrexate, >=98%;FOLOTYN PRALATREXATE;Pralatrexate(Folotyn)
- CBNumber:
- CB31856065
- Molecular Formula:
- C23H23N7O5
- Molecular Weight:
- 477.47
- MOL File:
- 146464-95-1.mol
- MSDS File:
- SDS
- Modify Date:
- 2023/6/8 17:06:34
| Melting point | 215 °C(dec.) |
|---|---|
| Density | 1.471±0.06 g/cm3(Predicted) |
| storage temp. | 2-8°C |
| Water Solubility | Insoluble in water |
| solubility | ≥23.85 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| pka | 3.53±0.10(Predicted) |
| form | powder to crystal |
| color | White to Light yellow |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |   GHS07,GHS08 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H361 | |||||||||
| Precautionary statements | P201-P202-P264-P270-P280-P301+P310+P330-P308+P313-P405-P501 | |||||||||
| HS Code | 2933.59.5300 | |||||||||
| NFPA 704 |
|
10-Propargyl-10-deazaaminopterin Chemical Properties,Uses,Production
Description
Pralatrexate, an injectable DHFR inhibitor, was launched for the treatment of patients with relapsed or refractory PTCL. PTCL is an aggressive form of non-Hodgkin’s lymphoma (NHL) characterized by the proliferation of abnormal T-lymphocytes that circulate in the peripheral bloodstream. The inhibition of the folate enzymes DHFR and thymidylate synthase is a well-validated method of cancer treatment. In vitro, pralatrexate is slightly less potent than MTX in inhibiting DHFR derived from murine leukemia L1210 cells (Ki = 18.2 pM vs. 5.75 pM) and human leukemia CCRF-CEM cells (Ki = 13.4 pM vs. 5.4 pM). However, it is transported into both types of cells with 10-fold higher efficiency than MTX, thereby providing a more potent inhibition of cell growth as compared with MTX. In vivo, intraperitonally administered pralatrexate at 60 mg/ kg twice weekly for three or four doses caused complete lymphoma regressions in 89, 56, and 30% of HT, RL, and SKI-DLBCL-1 xenografted mice, respectively, whereas a similar dosing of MTX at 40 mg/kg twice weekly did not produce complete regression. The posttreatment tumor diameter was also smaller in pralatrexate-treated animals.
Uses
An antifolate with high affinity for the reduced folate carrier-type 1, produces marked complete and durable remissions in a diversity of chemotherapy refractory cases of T-cell lymphoma.
Definition
ChEBI: A pteridine that is the N-4-[1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl derivative of L-glutamic acid. Used for treatment of Peripheral T-Cell Lymphoma, an aggressive form of non-Hodgkins lymphoma.
Clinical Use
Pralatrexate, an injectable dihydrofolate reductase (DHFR) inhibitor, has a superior potency and toxicity profile compared to other DHFR inhibitors. In 2009, the compound was launched by Allos and approved in the U.S. for the treatment of patients with relapsed or refractory peripheral T-cell lymphoma (PTCL) as a single agent. It is the first drug approved for this indication.70 In 2010, orphan drug designation was received in the E.U. for the treatment of cutaneous T-cell lymphoma (CTCL).
Side effects
The most common adverse reactions associated with pralatrexate are mucositis, thrombocytopenia, nausea, and fatigue. Folic acid and vitamin B12 supplements are administered as adjunct therapies to potentially reduce pralatrexate-related hematological toxicity and mucositis.
10-Propargyl-10-deazaaminopterin Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| Laurus Labs Ltd | +91-4066594333 +91-4039804333 | Telangana, India | 50 | 58 | Inquiry |
| Apicore Pharmaceuticals Pvt Ltd | +91-2662267177 +91-2662267166 | Gujarat, India | 181 | 58 | Inquiry |
| HETERO LABS LTD | (630) 931-6800 | New Delhi, India | 97 | 58 | Inquiry |
| TCI Chemicals (India) Pvt. Ltd. | 1800 425 7889 | New Delhi, India | 6778 | 58 | Inquiry |
| Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6773 | 58 | Inquiry |
| SynZeal Research Pvt Ltd | +1 226-802-2078 | Gujarat, India | 6522 | 58 | Inquiry |
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| Shanghai Daken Advanced Materials Co.,Ltd | +86-371-66670886 | China | 16858 | 58 | Inquiry |
| Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 | China | 21669 | 55 | Inquiry |
| Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 | China | 9337 | 55 | Inquiry |
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