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Anifostine trihydrate

Anifostine trihydrate structure

CAS No:
112901-68-5
Formula:
C5H17N2O4PS
Chemical Name:
Anifostine trihydrate
Synonyms:
Amifostine (150 mg);Anifostine trihydrate;Ethanethiol,2-[(3-aMinopropyl)aMino]-, 1-(dihydrogen phosphate), hydrate (1:3);Amifostine trihydrate, >=98%;Aminopropylamino)ethylsulfanylphosphonic acid trihydrate;S-2-(3-AMINOPROPYLAMINO)ETHYL O,O-DIHYDROGEN PHOSPHOROTHIOATE;WR2721;Amifostine
Categories:
Active Pharmaceutical Ingredients > Specialty Drugs

Description

Amifostine is the trihydrate form of a phosphorylated aminosulfhydryl compound. After dephosphorylation of amifostine by alkaline phosphatase to an active free sulfhydryl (thiol) metabolite, the thiol metabolite binds to and detoxifies cytotoxic platinum-containing metabolites of cisplatin and scavenges free radicals induced by cisplatin and ionizing radiation. The elevated activity of this agent in normal tissues results from both the relative abundance of alkaline phosphatase in normal tissues and the greater vascularity of normal tissues compared to tumor tissues.|A phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia.

Amifostine is a broad-spectrum cytoprotective agent, once used as a military anti-radiation agent, and now used as a protective drug for radiotherapy and chemotherapy. It has significantly effective in reducing the side effects of anticancer drugs such as cyclophosphamide, ciplatin, doxorubicin, and anti-HIV drugs such as 3-azido-3-deoxythymidine, without affecting the efficacy of anticancer or anti-HIV drugs curative effect. At present, the commercially available amifostine products include freeze-dried powder injection（ETHYOL ）produced by American Life Sciences Co., Ltd. It is only available as a lyophilized powder for injection, but is thermally unstable.

Anifostine trihydrate Basic Attributes

Molecular Weight：

232.23

Exact Mass：

268.085785

UNII：

M487QF2F4V

DSSTox ID：

DTXSID40150210

NCI Thesaurus Code：

C488

Color/Form：

White to off-white

HScode：

2930909165

Characteristics

PSA：

124

XLogP3：

0.64900

Appearance：

powder

Density：

1.367g/cm3

Boiling Point：

441.7°C at 760 mmHg

Flash Point：

220.9ºC

Storage Conditions：

2-8°C

PKA：

pKa1 <2.0; pKa2 4.2; pKa3 9.0; pKa4 11.7(at 25℃)

Critical Temperature & Pressure：

2-8°C

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

hazard class code：

safety instructions：

26-36

RTECS Number：

TE6491000

Marks：

Precautionary statement(s)：

P301 + P312 + P330

Hazard Statements：

GHS Classification：

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P301+P312, P330, and P501|Aggregated GHS information provided by 39 companies from 1 notifications to the ECHA C&L Inventory.

Drug Information

MeSH：

Drugs used to protect against ionizing radiation. They are usually of interest for use in radiation therapy but have been considered for other purposes, e.g. military. (See all compounds classified as Radiation-Protective Agents.)

MeSH Entry Terms：

Amifostine

Anifostine trihydrate Use and Manufacturing

Protectant (topical); radioprotector.

Amifostine may provide renal protection during PRRT using somatostatin analogs by mitigating radiation damage and reducing the absorbed kidney radiation dose. Amifostine remediates the degenerative effects of radiation on the mineralization capacity of the murine mandible.

Computed Properties

Molecular Weight:268.27
Hydrogen Bond Donor Count:7
Hydrogen Bond Acceptor Count:9
Rotatable Bond Count:7
Exact Mass:268.08579457
Monoisotopic Mass:268.08579457
Topological Polar Surface Area:124
Heavy Atom Count:15
Complexity:152
Covalently-Bonded Unit Count:4
Compound Is Canonicalized:Yes

Drug Function and Efficacy

This product is an organic thiophosphate compound. After being hydrolyzed and dephosphorylated by alkaline phosphatase bound to the cell membrane in the tissue, it becomes an active metabolite WR-1065, whose chemical structure is H2N-(CH2)3-NH-(CH2)2-SH. Because the sulfhydryl group has the function of scavenging free radicals in the tissue, it can reduce the toxicity of cisplatin, cyclophosphamide and mitomycin.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Amifostine for injection
Ingredients	Main ingredient: Amifostine Chemical name: S-2-[3-aminopropylamine]ethylthiophosphoric acid Molecular formula: C5H15N2O3PS Molecular weight: 214.22
Indication	Not yet clear.
Specifications	0.4 g
Manufacturer	Merro Pharmaceutical Co., Ltd.

Amifostine
Specifications	－－－－

Amifostine
Manufacturer	Merro Pharmaceutical Co., Ltd.

See More Related Drugs

Registered Holders

Tianjin Zhongrui Pharmaceutical Co., Ltd.

China
Active
Kaifeng MINGREN Pharmaceuticals Co., Ltd.

China
Active
Sichuan Huiyu Pharmaceutical Co., Ltd.

China
Active

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Recommended Suppliers of Anifostine trihydrate

Hangzhou Dawn Ray Pharmaceutical Co.,Ltd Contact Supplier

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Amifostine

CAS No.: 112901-68-5

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Tianjin Zhongrui Pharmaceutical Co.,Ltd Contact Supplier

CN
8 YRS

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Amifostine 82%

CAS No.: 112901-68-5

Grade: Pharmaceutical Grade

Content: 82%

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