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PEPLOMYCIN SULFATE

PEPLOMYCIN SULFATE
PEPLOMYCIN SULFATE structure
CAS No.
70384-29-1
Chemical Name:
PEPLOMYCIN SULFATE
Synonyms
Pepleo;NK 631;Nsc276382;PEPLOMYCIN SULFATE;Pepleomycin Sulfate;N1-[3-[[(1S)-1-phenylethyl]aMino]propyl]bleoMycinaMide;N1-[3-[[(1S)-1-phenylethyl]amino]propyl]bleomycinamide Sulfate;Bleomycinamide, N1-[3-[(1-phenylethyl)amino]propyl]-, (S)-, sulfate (1:1) (salt)
CBNumber:
CB8413187
Molecular Formula:
C61H90N18O25S3
Formula Weight:
1571.67
MOL File:
70384-29-1.mol

PEPLOMYCIN SULFATE Properties

Melting point:
196-198°C
alpha 
25436 -2.0° (c = 1 in water)
pka
2.9, 4.8, 7.4, 9.0(at 25℃)
EWG's Food Scores
1
FDA UNII
6A668951HW
SAFETY
  • Risk and Safety Statements
Toxicity LD50 in male rats, mice (mg/kg): 234, 88 s.c.; 208, 85 i.p.; 245, 51 i.v. (Ito)

PEPLOMYCIN SULFATE Chemical Properties,Uses,Production

Chemical Properties

Pale Yellow Amorphous Powder

Originator

Pepleo, Nippon Kayaku, Co., Japan ,1981

Uses

A derivative of Bleomycin with cytostatic activity and less pulmonary toxicity than the natural Bleomycin mixture

Manufacturing Process

In 400 ml of dimethylformamide was dissolved 15.0 g of bleomycinic acid (copper-containing form). To the solution kept at 0°C by cooling were added 1.1 ml of N-methylmorpholine and 10.3 g of 6-chloro-1-pchlorobenzenesulfonyloxybenzotriazole (CCBT) as an activating compound. The mixture was stirred for 5 minutes at 0°C, then admixed with 5.3 g of N[(S)-1'-phenylethyl]-1,3-diaminopropane and further stirred for 1 hour.
After termination of the reaction by adding 200 ml of a 25% aqueous acetic acid solution, the reaction mixture was mixed with 5 liters of cold acetone to precipitate the reaction product. The precipitate was collected by filtration, washed with acetone, and dissolved in 500 ml of distilled water. The resulting aqueous solution was immediately adjusted to pH 6.0 and poured into a column containing 2 liters of CM-Sephadex C-25 (NH4+type) packed in 0.05 M aqueous ammonium chloride solution to adsorb bleomycins.
Using aqueous ammonium chloride solution, elution was performed by passing through the column 20 liters of eluent in which the concentration of ammonium chloride was continually increased from 0.05 to 1.0 M. The unreacted bleomycinic acid was found in the effluent at the ammonium chloride concentration of about 0.05 M and NK631 at the ammonium chloride concentration of about 0.45 M. Both fractions, which showed UV absorption at 292 nm;, were separately collected.
The NK631-containing fraction was poured into a resin column containing 2.6 liters of Amberlite XAD-2. The column was then washed thoroughly with water and eluted with 0.01 N hydrochloric acid in methanol-water (4:1 v/v). A total of 2.5 liters of the blue fraction, which showed UV absorption at 292 mμ, was collected. After evaporating off the methanol from the eluent fraction, the concentrate was adjusted to pH 6.0 with Dowex 44 (OH- type, an anionexchange resin composed of a copolymer of epichlorohydrin and ammonia) and was freeze-dried to obtain 16.1 g (92% yield) of NK631 dihydrochloride (copper-containing form) in the form of blue amorphous powder.
By similar treatment, 280 mg of the unreacted bleomycinic acid (coppercontaining form) were recovered.
In 200 ml of distilled water was dissolved 10.0 g of the NK631 dihydrochloride (copper-containing form). The solution was poured into a column containing 600 ml of Amberlite XAD-2 packed in distilled water. The column was washed successively with 2 liters of an aqueous solution containing 5% of EDTA-Na2, 2.5 liters of a 5% aqueous sodium sulfate solution, and 630 ml of distilled water.
The column was then eluted with 0.0025 N sulfuric acid in methanol-water mixture (1:1 v/v). A total of 900 ml of fractions containing a substance which showed UV absorption at 290 mμ was collected. After removal of methanol by distillation, the residual liquid was adjusted to pH 6.0 with Dowex 44 (OHtype) and freeze-dried to obtain 9.3 g (95% yield) of NK631 monosulfate (copper-free form) in the form of pale yellowish-white amorphous powder.

Therapeutic Function

Antineoplastic

Safety Profile

Poison by intraperitoneal, subcutaneous, and intravenous routes. Questionable carcinogen with experimental carcinogenic data. An eye irritant. When heated to decomposition it emits very toxic fumes of NOx and SOx.

PEPLOMYCIN SULFATE Preparation Products And Raw materials

Raw materials

Preparation Products


PEPLOMYCIN SULFATE Suppliers

Global( 13)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
J & K SCIENTIFIC LTD. 400-666-7788 010-82848833-
86-10-82849933 jkinfo@jkchemical.com;market6@jkchemical.com China 96500 76
Chemsky(shanghai)International Co.,Ltd. 021-50135380
shchemsky@sina.com China 32358 50
BOC Sciences 16314854226
info@bocsci.com United States 21113 65
Shenzhen Polymeri Biochemical Technology Co., Ltd. 400-002-6226
sales@biochemall.cn China 54467 58

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