Busulfan
- CAS No.
- 55-98-1
- Chemical Name:
- Busulfan
- Synonyms
- myleran;busulfex;busulphan;1,4-BUTANEDIOL DIMETHANESULFONATE;Butane-1,4-diyl dimethanesulfonate;gt41;x149;mablin;Mylera;an33501
- CBNumber:
- CB2105891
- Molecular Formula:
- C6H14O6S2
- Molecular Weight:
- 246.3
- MOL File:
- 55-98-1.mol
- Modify Date:
- 2025/2/24 16:12:34
| Melting point | 114-117 °C(lit.) |
|---|---|
| Boiling point | 359.3°C (rough estimate) |
| Density | 1.305 (estimate) |
| refractive index | 1.5630 (estimate) |
| Flash point | 9℃ |
| storage temp. | Inert atmosphere,Room Temperature |
| solubility | Very slightly soluble in water, freely soluble in acetone and in acetonitrile, very slightly soluble in ethanol (96 per cent). |
| form | Crystalline Powder |
| color | Pale Brown |
| Water Solubility | Decomposes |
| Merck | 14,1505 |
| BRN | 1791786 |
| Stability | Moisture Sensitive |
| CAS DataBase Reference | 55-98-1(CAS DataBase Reference) |
| IARC | 1 (Vol. 4, Sup 7, 100A) 2012 |
| EPA Substance Registry System | Busulfan (55-98-1) |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |   GHS06,GHS08 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Danger | |||||||||
| Hazard statements | H301-H340-H350-H360FD | |||||||||
| Precautionary statements | P202-P264-P270-P280-P301+P310-P405 | |||||||||
| Hazard Codes | T+,T,F | |||||||||
| Risk Statements | 45-26/27/28-63-46-36/37/38-23/24/25-39/23/24/25-11 | |||||||||
| Safety Statements | 53-36/37/39-45-28A-36/37-16-7 | |||||||||
| RIDADR | UN 2811 6.1/PG 1 | |||||||||
| WGK Germany | 3 | |||||||||
| RTECS | EK1750000 | |||||||||
| HazardClass | 6.1(b) | |||||||||
| PackingGroup | III | |||||||||
| HS Code | 29053990 | |||||||||
| Hazardous Substances Data | 55-98-1(Hazardous Substances Data) | |||||||||
| Toxicity | LD50 i.v. in rats: 1.8 mg/kg (Scherf) | |||||||||
| NFPA 704 |
|
Busulfan price More Price(4)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich(India) | B2635 | Busulfan analytical standard, for drug analysis | 55-98-1 | 10G | ₹5001.15 | 2022-06-14 | Buy |
| Sigma-Aldrich(India) | B2635 | Busulfan analytical standard, for drug analysis | 55-98-1 | 25G | ₹7945.55 | 2022-06-14 | Buy |
| Sigma-Aldrich(India) | B-094 | Busulfan solution 1?mg/mL in acetonitrile, certified reference material, ampule of 1?mL, Cerilliant? | 55-98-1 | 1ML | ₹28608.3 | 2022-06-14 | Buy |
| TCI Chemicals (India) | B1022 | 1,4-Butanediol Dimethanesulfonate | 55-98-1 | 25G | ₹4800 | 2022-05-26 | Buy |
Busulfan Chemical Properties,Uses,Production
Description
Chemically, busulfan is classified as an alkyl sulfonate. One or both of the methylsulfonate ester moieties can be displaced by the nucleophilic N7 of guanine, leading to monoalkylated and cross-linked DNA. The extent of alkyl sulfonate–mediated DNA interstrand cross-linking has been shown to vary with the length of the alkyl chain between sulfonate esters, with the tetramethylene-containing busulfan showing less interstrand cross-linking capability than hexamethylene, methylene, or octamethylene analogues. Intrastrand cross-linking also occurs, preferentially at 5′-GA-3′ but also at 5′-GG-3′ sequences. Alkylation of Cys sulfhydryl groups is yet another mechanism of cytotoxicity.
Chemical Properties
White Crystalline Solid
Uses
Busulfan USP (Myleran) is used to treat Chronic granulocytic leukemia; other myeloproliferative disorders.
Indications
Busulfan (Myleran) is a bifunctional methanesulfonic
ester that forms intrastrand cross-linkages with DNA.
The drug is well absorbed after oral administration and
has a plasma half-life of less than 5 minutes. Metabolites
and degradation products are excreted primarily in the
urine.
Busulfan is used in the palliative treatment of
chronic granulocytic leukemia. Daily oral therapy results
in decreased peripheral white blood cells and improved
symptoms in almost all patients during the
chronic phase of the disease. Excessive uric acid production
from rapid tumor cell lysis should be prevented
by coadministration of allopurinol.
At usual therapeutic dosages, busulfan is selectively
toxic to granulocyte precursors rather than lymphocytes.
Thrombocytopenia and anemia and less commonly,
nausea, alopecia, mucositis, and sterility also may
occur. Unusual side effects of busulfan include gynecomastia,
a general increase in skin pigmentation, and interstitial
pulmonary fibrosis.
Definition
ChEBI: A methanesulfonate ester that is butane-1,4-diol in which the hydrogens of the hydroxy groups are replaced by methanesulfonyl groups. An alkylating antineoplastic agent, it is used for the treatment of chronic myeloid leukemia (although it has been largely replaced by newer drugs). It is also used as an insect sterilant.
General Description
As an alternative to utilizing aziridines as electrophilic species,it was found that simply utilizing a carbon chain terminated atboth ends by leaving groups gave compounds capable of actingas cross-linking agents.Busulfan utilizestwo sulfonate functionalities as leaving groups separated by afour-carbon chain that reacts with DNA to primarily form intrastrandcross-link at 5'-GA-3' sequences.The sulfonatesare also subject to displacement by the sulfhydryl functionsfound in cysteine and glutathione, and metabolic products areformed as a result of nucleophilic attack by these groups togenerate sulfonium species along with methane sulfonicacid.This is followed by conversion to tetrahydrothiophene,and further oxidation products are subsequently produced togive the sulfoxide and sulfone. The cyclic sulfone known assulfolane may be further oxidized to give 3-hydroxysulfolane.
Air & Water Reactions
Busulfan is an alkylating agent which hydrolyzes in water. .
Reactivity Profile
Busulfan is an alkylating agent which hydrolyzes in water. . Strong reducers may yield hydrogen sulfide.
Hazard
Extremely toxic, carcinogen, clastogenic, teratogenic, immunosuppressive, delayed bone marrow aplasia, cataracts, pigmentation, pulmonary thrombosis, cardiotoxic effects, thrombocytopenia.
Fire Hazard
Flash point data for Busulfan are not available. Busulfan is probably combustible.
Clinical Use
Busulfan is used in the treatment of chronic myelogenous leukemia and can be administered either orally or by IV infusion.
Side effects
Serious bone marrow hypoplasia and myelosuppression are possible with this agent, and recovery from busulfaninduced pancytopenia can take up to 2 years.
Safety Profile
Confirmed carcinogen producing leukemia, kidney, and uterine tumors. Experimental neoplastigenic and tumorigenic data. Poison by ingestion, subcutaneous, intraperitoneal, intravenous, and possibly other routes. Ingestion by pregnant women can cause cancer of the reproductive system of the fetus includtng the uterus. Human teratogenic effects by ingestion and possibly other routes include developmental abnormaltties of the eye, ear, craniofacial area including the nose and tongue, gastrointestinal system, endocrine system, urogenital system, and other unspecified areas. Other human reproductive effects by ingestion and possibly other routes include: impotence, changes in the uterus, cervix, and vagina, and menstrual-cycle dtsorders. Experimental reproductive effects. Human systemic effects by ingestion: general arteriolar or venous ddation of the eye, changes in structure or function of salivary glands. When heated to decomposition it emits toxic fumes of SOx. See also SULFONATES.
Carcinogenicity
1,4-Butanediol dimethanesulfonate is known to be a human carcinogen based on sufficient evidence of carcinogenicity from studies in humans.
Busulfan Preparation Products And Raw materials
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| KARPSCHEM LABORATORIES | +91-7249203006 +91-7249203006 | Maharashtra, India | 786 | 58 | Inquiry |
| Basil Drugs AND Pharmaceuticals Pvt Ltd | +91-2249700250 +91-9619320820 | Mumbai, India | 108 | 58 | Inquiry |
| Triveni Interchem Private Limited | +91-02606618618 +91-7574814001 | Gujarat, India | 42 | 58 | Inquiry |
| NATCO Pharma Limited | +91-9849511345 +91-9866005199 | Hyderabad, India | 24 | 58 | Inquiry |
| Kekule Pharma Limited | +919849798889 | Hyderabad, India | 59 | 58 | Inquiry |
| Ralington Pharma | +91-7948911722 +91-9687771722 | Gujarat, India | 1350 | 58 | Inquiry |
| Shivalik Rasayan Ltd | +91-1147589500 +91-9811043611 | New Delhi, India | 12 | 58 | Inquiry |
| Surajlok Chemicals Pvt Ltd (Neon Laboratories Ltd) | +91-2268107000 +91-9987232509 | Maharashtra, India | 30 | 58 | Inquiry |
| Apicore Pharmaceuticals Pvt Ltd | +91-2662267177 +91-2662267166 | Gujarat, India | 181 | 58 | Inquiry |
| Fresenius Kabi Oncology Limited | +91-1243325000 +91-1244885000 | Haryana, India | 22 | 58 | Inquiry |
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