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PENTOSTATIN

CAS No.
53910-25-1
Chemical Name:
PENTOSTATIN
Synonyms
dcf;Nipent;deoxycoformycin;Co-V;2’dcf;ci-825;yk-176;Cl 825;PD-ADI;Coforin
CBNumber:
CB4746489
Molecular Formula:
C11H16N4O4
Molecular Weight:
268.27
MDL Number:
MFCD00078802
MOL File:
53910-25-1.mol
MSDS File:
SDS
Last updated:2024-03-18 17:29:40

PENTOSTATIN Properties

Melting point 154-157?C
alpha D25 +76.4° (c = 1 in water); D23 +73.0° (c = 1, pH 7 buffer)
Boiling point 411.43°C (rough estimate)
Density 1.2576 (rough estimate)
refractive index 1.6081 (estimate)
storage temp. -20°C
solubility H2O: soluble10mg/mL, clear
pka 5.2(at 25℃)
form White solid
color white to beige
optical activity [α]/D +70 to +80°, c = 1 in H2O
NCI Dictionary of Cancer Terms DCF; Nipent; pentostatin
FDA UNII 395575MZO7
NCI Drug Dictionary Nipent
ATC code L01XX08
Proposition 65 List Pentostatin

Pharmacokinetic data

Protein binding 4%
Excreted unchanged in urine 50-96%
Volume of distribution 36.1 Litres
Biological half-life 2.6-10 / 18

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS06
Signal word  Danger
Hazard statements  H301
Precautionary statements  P301+P310
Hazard Codes  Xn
Risk Statements  22
RIDADR  UN 2811 6.1 / PGIII
WGK Germany  3
HS Code  2933998090
Toxicity LD50 oral in mouse: 227mg/kg
NFPA 704
0
2 0

PENTOSTATIN price More Price(40)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich SML0508 Pentostatin ≥95% (HPLC) 53910-25-1 5mg $94.1 2024-03-01 Buy
Sigma-Aldrich 116860 Adenosine Deaminase Inhibitor, DCF 53910-25-1 10mg $172 2024-03-01 Buy
Cayman Chemical 14878 Pentostatin ≥98% 53910-25-1 1mg $38 2024-03-01 Buy
Cayman Chemical 14878 Pentostatin ≥98% 53910-25-1 5mg $85 2024-03-01 Buy
Sigma-Aldrich SML0508 Pentostatin ≥95% (HPLC) 53910-25-1 25mg $400 2024-03-01 Buy
Product number Packaging Price Buy
SML0508 5mg $94.1 Buy
116860 10mg $172 Buy
14878 1mg $38 Buy
14878 5mg $85 Buy
SML0508 25mg $400 Buy

PENTOSTATIN Chemical Properties,Uses,Production

Description

Pentostatin, an adenosine deaminase inhibitor, is an orphan drug introduced for the treatment of hairy cell leukemia. The agent is considered a significant advance over alpha-interferon, the only other drug available for this indication. The majority of patients treated with pentostatin have been reported to remain in remission for at least four years. It is also under investigation for the treatment of other kinds of leukemia and in transplant rejection.

Description

Because of their antitumor activity via inhibition of DNA synthesis, purine nucleoside derivatives resistant to deamination have been developed for the treatment of various leukemias. Pentostatin is a purine nucleoside analog that irreversibly inhibits adenosine deaminase (Ki = 0.9 pM) and thus interrupts DNA synthesis in dividing cells. Pentostatin has been reported to display strong efficacy in the clinical treatment of hairy cell leukemia as well as relapsed chronic lymphocytic leukemia.

Chemical Properties

White Solid

Originator

Warner-Lambert (Parke-Davis) (U.S.A.)

Uses

Pentostatin is a potent antitumor antibiotic isolated from a Streptomyces species. Pentostatin is a potent inhibitor of adenine deaminase and has been used therapeutically as an antitumor agent.

Uses

An adenosine deaminase inhibitor used as an anti-cancer therapeutic drug. Shown to be effective in the treatment of hairy cell leukemia as well as having use in the treatment of other types of cancer such as chronic lymphocytic leukemia.

Uses

Pentostatin is a potent antitumour antibiotic isolated from a Streptomyces species. Pentostatin is a potent inhibitor of adenine deaminase and has been used therapeutically as an antitumour agent.

Indications

Pentostatin (Nipent, deoxycoformycin) is a purine isolated from fermentation cultures of the microbe Streptomyces antibioticus. Its mechanism of action involves inhibition of the enzyme adenosine deaminase, which plays an important role in purine salvage pathways and DNA synthesis.The resulting accumulation of deoxyadenosine triphosphate (dATP) is highly toxic to lymphocytes.
Pentostatin is effective in the therapy of hairy cell leukemia, producing remissions in 80 to 90% of patients and complete remissions in more than 50%. The major toxic effects of the drug include myelosuppression, nausea, and skin rashes.

brand name

Nipent (SuperGen), Coforin (Katetsuken).

General Description

The drug is available in 10-mg vials for IV use. The drug isused to treat leukemias such as hairy cell leukemia, chroniclymphocytic leukemia, and lymphoblastic leukemia. Themechanism of action involves inhibition of the enzymeadenosine deaminase yielding increased cellular levels ofdeoxyadenosine and deoxyadenosine triphosphate (dATP).The increased levels of dATP are cytotoxic to lymphocytes.Pentostatin is a fermentation product of Streptomyces antibioticus.Resistance appears to involve decreased cellulartransport or increased expression of catabolic enzymes.Acid instability prevents oral administration, and the drug isonly administered by IV. The drug is distributed in totalbody water but does not enter the CNS. The majority of thedosage is excreted unchanged in the urine. Fatal pulmonary toxicity has occurred when pentostatin and fludarabine areused in combination. Toxicities include myelosuppression,immunosuppression, nausea, vomiting, headache, lethargy,and fatigue.

Biological Activity

Irreversible inhibitor of adenosine deaminase (K i = 2.5 pM). Anticancer agent.

Biochem/physiol Actions

Pentostatin/2′-deoxycoformycin is used to treat patients with Waldenstr?m′s macroglobulinemia.

Mechanism of action

Pentostatin is the most potent inhibitor of adenosine deaminase, an important and ubiquitous cellular enzyme. Inhibition of this enzyme leads to the accumulation of dATP, which inhibits ribonucleotide reductase and thus DNA synthesis.

Clinical Use

Pentostatin is a ring-expanded purine ribonucleoside that inhibits adenosine deaminase and is used in the treatment of hairy cell leukemia. The elevated levels of deoxyadenosine triphosphate that result from inhibition of this degradative enzyme inhibit the action of ribonucleotide reductase (the enzyme that converts ribose diphosphate to deoxyribose diphosphate), thus halting DNA synthesis within the tumor cell.

Safety Profile

Poison by intravenous route. An experimental teratogen. Human mutation data reported. When heated to decomposition it emits toxic fumes of NOx.

Drug interactions

Potentially hazardous interactions with other drugs
Antipsychotics: avoid with clozapine (increased risk of agranulocytosis).
Cytotoxics: increased risk of toxicity with high-dose cyclophosphamide - avoid; increased pulmonary toxicity with fludarabine (unacceptably high incidence of fatalities).

Metabolism

Only a small amount is metabolised via the liver.
It is primarily excreted unchanged by the kidneys (30-90% excreted by kidneys within 24 hours).

storage

Store at +4°C

PENTOSTATIN Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 197)Suppliers
Supplier Tel Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795 ivan@atkchemical.com China 32480 60
Biochempartner
0086-13720134139 candy@biochempartner.com CHINA 967 58
Hubei xin bonus chemical co. LTD
86-13657291602 linda@hubeijusheng.com CHINA 22968 58
Shenzhen Excellent Biotech Co., Ltd.
13480692018 ramyan@ex-biotech.com CHINA 954 58
Jurong Coupling Biotechnology Co., Ltd.
13656108824 coupling278191416@hotmail.com CHINA 184 58
career henan chemical co
+86-0371-86658258 15093356674; factory@coreychem.com China 29826 58
Shaanxi Dideu Medichem Co. Ltd
+86-29-87569266 15319487004 1015@dideu.com China 2263 58
Fuxin Pharmaceutical
+86-021-021-50872116 +8613122107989 contact@fuxinpharm.com China 10297 58
Hubei Ipure Biology Co., Ltd
+8613367258412 ada@ipurechemical.com China 10326 58
ANHUI WITOP BIOTECH CO., LTD
+8615255079626 eric@witopchemical.com China 23556 58

View Lastest Price from PENTOSTATIN manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Pentostatin pictures 2021-12-14 Pentostatin
53910-25-1
US $10.00 / g/Bag 10g 99 100KG Wuhan Demeikai Biotechnology Co., Ltd
PENTOSTATIN pictures 2021-07-13 PENTOSTATIN
53910-25-1
US $15.00-10.00 / KG 1KG 99%+ HPLC Monthly supply of 1 ton Zhuozhou Wenxi import and Export Co., Ltd
PENTOSTATIN USP/EP/BP pictures 2021-07-02 PENTOSTATIN USP/EP/BP
53910-25-1
US $1.10 / g 1g 99.9% 100 Tons Min Dideu Industries Group Limited
  • Pentostatin pictures
  • Pentostatin
    53910-25-1
  • US $10.00 / g/Bag
  • 99
  • Wuhan Demeikai Biotechnology Co., Ltd
  • PENTOSTATIN pictures
  • PENTOSTATIN
    53910-25-1
  • US $15.00-10.00 / KG
  • 99%+ HPLC
  • Zhuozhou Wenxi import and Export Co., Ltd

PENTOSTATIN Spectrum

2’-deoxycoformycin CL-67310465:NSC-218321 (8R)-3-(2-Deoxy-β-D-erythro-pentofuranosyl)-3,4,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol Pentostatin(Deoxycoformycin) Pentostatin, >=99% ci-825 cl67310465 co-vidarabine iazepin-8-ol imidazo(4,5-d)(1,3)diazepin-8-ol,3-(2-deoxy-beta-d-pentofuranosyl)-3,6,7,8-tet (8R)-3-(2-Deoxy-β-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8β-ol Coforin 2'-DeoxycoforMycin, Covidaribine, ADAI, CI 825, d-Cof, NSC 218321, PD-ADI, YK 176 nsc-218321 yk-176 Imidazo4,5-d1,3diazepin-8-ol, 3-(2-deoxy-.beta.-D-erythro-pentofuranosyl)-3,4,7,8-tetrahydro-, (8R)- Imidazo[4,5-d][1,3]diazepin-8-ol, 3-(2-deoxy-b-D-erythro-pentofuranosyl)-3,4,7,8-tetrahydro-, (8R)- 2'-Dexoycoformycin Cl 825 Co-V Deaminase inhibitor Imidazo[4,5-d][1,3]diazepin-8-ol, 3-(2-deoxy-b-D-erythro-pentofuranosyl)-3,4,7,8-tetrahydro-, (8R)- (9CI) Imidazo[4,5-d][1,3]diazepin-8-ol, 3-(2-deoxy-b-D-erythro-pentofuranosyl)-3,4,7,8-tetrahydro-, (R)- NSC 247520 PD-ADI Vira A deaminase inhibitor 2''-DEOXYCOFORMYCIN (2''-DCF: NIPENT) -3-(2-Deoxy-β-D-erythro-pentofuranosyl)-3,6,7,8-te-trahydroimidazo[4,5-d][1,3]diazepin-8-ol (R)-3-((2S,4S,5R)-4-Hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-3,4,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol Adenosine Deaminase Inhibitor, DCF PENTOSTATIN (r)-3-(2-deoxy-beta-d-erythro-pento-furanosyl)-3,6,7,8-tetrahydroimidazo[4,5-d (r)-3-(2-deoxy-beta-d-pentofuranosyl)-3,6,7,8-tetrahydroimidazo(4,5-d)(1,3)d (r)-deoxycoformycin (r)-rahydro 2’dcf Vira A Deaminase Inhibito Imidazo[4,5-d][1,3]diazepin-8-ol, 3-(2-deoxy-β-D-erythro-pentofuranosyl)-3,4,7,8-tetrahydro-, (8R)- (R)-3-((2R,4S,5R)-4-Hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-3,4,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol PENTOSTATIN USP/EP/BP Pentostatin (CI825 Pentostatin, 98%(HPLC) Adenosine Deaminase Inhibitor, DCF - CAS 53910-25-1 - Calbiochem (8R)-3-(2-Deoxy-b-D-erythro-pentofuranosyl)-3,4,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol dcf deoxycoformycin Nipent Reliable quality 53910-25-1 PENTOSTATIN (8R)-3-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-7,8-dihydro-4H-imidazo[4,5-d][1,3]diazepin-8-ol PD-81565 PD 81565 PD81565 (8R)-3-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-7,8-dihydro-4H-imidazo[4,5-d][1,3]diazepin-8-ol 53910-25-1 Chiral Reagents Heterocycles Intermediates & Fine Chemicals Pharmaceuticals