Product Name

Pentostatin

CAS Number

53910-25-1

LGM Pharma is an API distributor. LGM Pharma supplies APIs as per CGMP with DMF support, subject to availability and manufacturer requirements. LGM Pharma does not sell or supply APIs or finished dosage products to individual patients, doctors, or pharmacies.

Questions? Call our customer API support number 1-(800)-881-8210

Product Name:
Pentostatin
CAS Number:
53910-25-1
Indication:
For the treatment of hairy cell leukaemia refractory to alpha interferon.
Mode of Action:

Pentostatin is a potent transition state inhibitor of adenosine deaminase (ADA), the greatest activity of which is found in cells of the lymphoid system. T-cells have higher ADA activity than B-cells, and T-cell malignancies have higher activity than B-cell malignancies. The cytotoxicity that results from prevention of catabolism of adenosine or deoxyadenosine is thought to be due to elevated intracellular levels of dATP, which can block DNA synthesis through inhibition of ribonucleotide reductase. Intracellular activation results in incorporation into DNA as a false purine base. An additional cytotoxic effect is related to its incorporation into RNA. Cytotoxicity is cell cycle phase-specific (S-phase).

Pharmacodynamics:

Pentostatin is an antineoplastic anti-metabolite used in the treatment of several forms of leukemia including acute nonlymphocytic leukemia and hairy cell leukemia. Anti-metabolites masquerade as purine or pyrimidine – which become the building blocks of DNA. They prevent these substances becoming incorporated in to DNA during the "S" phase (of the cell cycle), stopping normal development and division. It is a 6-thiopurine analogue of the naturally occurring purine bases hypoxanthine and guanine. Intracellular activation results in incorporation into DNA as a false purine base. An additional cytotoxic effect is related to its incorporation into RNA. Cytotoxicity is cell cycle phase-specific (S-phase).

Metabolism:

Primarily hepatic, but only small amounts are metabolized.

Toxicity:

LD50=128 mg/kg (mouse), side effects include lethargy, rash, fatigue, nausea and myelosuppression.

IUPAC:
(8R)-3-[(2R, 4S, 5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-3H, 6H, 7H, 8H-imidazo[4, 5-d][1, 3]diazepin-8-ol
ATC:
L01XX08
PubChem:
40926
DrugBank:
DB00552 (APRD00202)
Formula:
C18H16O3
Molecular Mass:
268.2691
Synonyms:
2'-DCF 2'-Deoxycoformycin 2'-Dexoycoformycin Deoxycoformycin
SMILES:
OC[C@H]1O[C@H](C[C@@H]1O)N1C=NC2=C1N=CNC[C@H]2O
InChi:
FPVKHBSQESCIEP-JQCXWYLXSA-N
General Reference:
General Reference:

  1. Link

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

LGM currently offers Monoclonal Antibodies (mAbs) for non-GMP/R&D use. Please inquire about Monoclonal Antibodies produced under GMP conditions.

Questions? Call our customer API support number 1-(800)-881-8210. 

Ask us about this product

API’s From Quality Manufacturers:

  • Streamlined API supply towards initial research stages as well as larger quantities of cGMP material for clinical trials and product commercialization
  • Premium quality GMP certified and fully accredited API manufacturing plants
  • Technical packages as well as access to filed DMF, ASMF or CEP (subject to availability)
  • Regulatory and technical assistance towards any submission type based on specific customer requirements

Find an API Product

Search
Generic filters