Busulfex
Busulfan
CAS: 55-98-1
Molecular Formula: C6H14O6S2
Busulfex - Names and Identifiers
| Name | Busulfan |
| Synonyms | Myleran myleran BUSULFAN Busulfex busulfex Busulfan busulphan Busulphan 1,4-dimethanesulfonoxybutane 1,4-Dimethanesulfonoxybutane 1,4-BUTANEDIOL DIMETHANESULFONATE 1,4-Butanediol dimethanesulfonate tetramethylene bis(methanesulfonate) Tetramethylene bis(methanesulfonate) |
| CAS | 55-98-1 |
| EINECS | 200-250-2 |
| InChI | InChI=1/C6H14O6S2/c1-13(7,8)11-5-3-4-6-12-14(2,9)10/h3-6H2,1-2H3 |
Busulfex - Physico-chemical Properties
| Molecular Formula | C6H14O6S2 |
| Molar Mass | 246.3 |
| Density | 1.305 (estimate) |
| Melting Point | 114-117°C(lit.) |
| Boling Point | 359.3°C (rough estimate) |
| Flash Point | 9℃ |
| Water Solubility | Decomposes |
| Solubility | Very slightly soluble in water, freely soluble in acetone and in acetonitrile, very slightly soluble in ethanol (96 per cent). |
| Appearance | Crystalline Powder |
| Color | Pale Brown |
| Merck | 14,1505 |
| BRN | 1791786 |
| Storage Condition | Inert atmosphere,Room Temperature |
| Stability | Moisture Sensitive |
| Refractive Index | 1.5630 (estimate) |
| MDL | MFCD00007562 |
| Physical and Chemical Properties | White crystalline powder. Melting Point 119 °c. Do not dissolve in water, but can dissolve slowly, while the hydrolysis. In 25 ° C acetone solubility of 2.4g/100ml, in ethanol solubility of 0.1g/100ml, almost odorless. |
| Use | Antineoplastic drugs. The product for the cell cycle non-specific drugs, mainly for the G1 phase and M phase. The low dose of the product inhibited the production of bone marrow granulocytes and had little effect on red blood cells and lymphocytes. High dose had little effect on red blood cells and lymphocytes. In large doses, the production of red blood cells and lymphocytes was inhibited. Due to the selective effect, the effect of chronic myeloid leukemia is significant. Busulfan is the main drug for the treatment of chronic myeloid leukemia, and its remission rate can reach 80-90%. But should be discontinued in the event of acute lesions. |
| In vitro study | Busulfan inhibits the frequency of cell formation in the cobblestone region, but does not cause a significant increase in apoptosis of hematopoietic stem cell-like cells and progenitor cells. Busulfan inhibits the hematopoietic function of HSC-like cells and progenitor cells through an apoptosis-dependent mechanism. Busulfan induces bone marrow hematopoietic cell senescence in a time-dependent manner, which is similar to p16 in normal human diploid fibroblast WI38, Busulfan (alkylating agent) causes DNA damage by cross-linking DNA and protein, senescence is independently induced by extracellular signal-regulated kinase (ERK) and p38 mitogen-activated protein kinase (p38 protein) cascades. Busulfan induced a transient decrease in glutathione but not a sustained increase in ROS production. In testicular cells, Busulfan prevents apoptosis of spermatogonial stem cells by inhibiting the expression of PCNA and inducing Rb hypophosphorylation. |
| In vivo study | The Busulfan-treated mice showed a marked increase in apoptosis and a decrease in testicular weight. Busulfan(40 mg/kg) induced apoptosis in the maximum number of cells while reducing the number of necrotic cells. In NOD/SCID mice, Busulfan treatment and irradiation resulted in similar detection sensitivity of HSC by limiting dilution analysis. The Busulfan transplanted mice had slow and incomplete lymphatic engraftment. Busulfan(20 mg/kg to 100 mg/kg) dose-dependently provided homotypic lymphoid recombination in mice. |
Busulfex - Risk and Safety
| Risk Codes | R45 - May cause cancer R26/27/28 - Very toxic by inhalation, in contact with skin and if swallowed. R63 - Possible risk of harm to the unborn child R46 - May cause heritable genetic damage R36/37/38 - Irritating to eyes, respiratory system and skin. R23/24/25 - Toxic by inhalation, in contact with skin and if swallowed. R39/23/24/25 - R11 - Highly Flammable |
| Safety Description | S53 - Avoid exposure - obtain special instructions before use. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S28A - S36/37 - Wear suitable protective clothing and gloves. S16 - Keep away from sources of ignition. S7 - Keep container tightly closed. |
| UN IDs | UN 2811 6.1/PG 1 |
| WGK Germany | 3 |
| RTECS | EK1750000 |
| HS Code | 29053990 |
| Hazard Class | 6.1(b) |
| Packing Group | III |
| Toxicity | LD50 i.v. in rats: 1.8 mg/kg (Scherf) |
Busulfex - Standard
Authoritative Data Verified Data
This product is 1, 4-butanediol dimesylate. Calculated as dried product, the content of C6H14O6S2 shall not be less than 98.5%.
Last Update：2024-01-02 23:10:35
Busulfex - Trait
Authoritative Data Verified Data
- This product is white crystalline powder; Almost odorless.
- This product is dissolved in acetone, slightly soluble in water or ethanol.
melting point
The melting point of this product (General 0612) is 114~118°C.
Last Update：2022-01-01 11:39:09
Busulfex - Differential diagnosis
Authoritative Data Verified Data
- take this product about 0.1g, add potassium nitrate 0.lg and 0.25g of potassium hydroxide were heated and melted, cooled, and dissolved with 5ml of water. Dilute hydrochloric acid was added to make the solution acidic.
- take about 0.lg of this product, add 10ml of water and 5ml of sodium hydroxide solution. After heating and dissolving, special odor will occur. Cool, divide the solution into 2 parts, 1 drop of potassium permanganate test solution was added in 1 part, and the color of the solution was gradually changed from purple to blue, and finally to Alexandrite. In the other part, dilute sulfuric acid was added to make it acidic, and 1 drop of potassium permanganate test solution was added, and the purple color of the solution remained unchanged.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 935).
Last Update：2022-01-01 11:39:09
Busulfex - Exam
Authoritative Data Verified Data
acidity
take 0.20g of this product, add 50ml of anhydrous ethanol (neutral to methyl red indicator solution), heat and dissolve, add 3 drops of Methyl red indicator solution, and use sodium hydroxide titration solution (0.lmol/L) titration, not over 0.05.
loss on drying
take this product, put it in a phosphorus pentoxide dryer, and dry it under reduced pressure at 60°C to constant weight, and the weight loss shall not exceed 0.5% (General rule 0831).
ignition residue
not more than 0.1% (General rule 0841).
Last Update：2022-01-01 11:39:10
Busulfex - Content determination
Authoritative Data Verified Data
take about 0.2g of this product, accurately weigh it, put it in a 200ml Erlenmeyer flask, add 40ml of water, attach a reflux condenser, slowly reflux for 30 minutes, cool, add several drops of phenolphthalein indicator liquid, with sodium hydroxide titration solution (0.lmol/L) titration. Each 1 ml of sodium hydroxide titration solution (0.1 mol /L) corresponds to 12.32mg of C6H14O6S2.
Last Update：2022-01-01 11:39:11
Busulfex - Category
Authoritative Data Verified Data
antineoplastic agents.
Last Update：2022-01-01 11:39:11
Busulfex - Storage
Authoritative Data Verified Data
sealed storage.
Last Update：2022-01-01 11:39:11
Busulfex - Myleran（Busulfan Tablets）
Authoritative Data Verified Data
This product contains busulfan (C6H14O6S2) should be labeled the amount of 90.0% to 110.0%.
trait
This product is sugar-coated tablets, White after removing the coating.
identification
take an appropriate amount of fine powder of this product (about 5mg equivalent to busulfan), add 25ml of acetone, shake to dissolve busulfan, filter, evaporate the filtrate, and determine it according to law (General rule 0612), the melting point was 113 to 118°C.
examination
should be in accordance with the relevant provisions under The tablet item (General rule 0101).
Content determination
Take 20 tablets (2mg specification) or 80 tablets (0.5 mg specification) of this product, place the mortar in the mortar to grind, pay attention to avoid loss, move the beaker, wash the mortar with 20ml of acetone, the whole powder was washed in a beaker and stirred at a slight temperature. After precipitation, the supernatant was filtered through a conical flask with absorbent cotton moistened with acetone, and the residue was extracted with acetone for 3 times, 20ml each time, the extract was filtered into a human conical flask, distilled off acetone on a water bath, the residue was added with 30ml of water, reflux condenser tube was attached, and the mixture was slowly refluxed for 30 minutes, allowed to cool, and several drops of phenolphthalein indicator liquid were added, titration with sodium hydroxide titration solution (0.05mol/L). Each 1 ml of sodium hydroxide titration solution (0.05 mol/L) is equivalent to 6.158mg of C6H14O6S2.
category
Same as busulfan.
specification
(1)0.5mg (2)2mg
storage
sealed and stored in a dry place.
Last Update：2022-01-01 11:39:12
Busulfex - Reference Information
| (IARC) carcinogen classification | 1 (vol. 4, sup 7, 100a) 2012 |
| EPA chemical information | Information provided by: ofmpub.epa.gov (external link) |
| biological activity | Busulfan is a cell cycle non-specific alkylating agent anti-tumor drug. Busulfan can induce apoptosis. |
| use | antineoplastic drugs. This product is a cell cycle non-specific drug, mainly used in G1 phase and M phase. The low dose of the product inhibits the production of bone marrow granulocytes and has almost no effect on red blood cells and lymphocytes. At large doses, there was little effect on red blood cells and lymphocytes. In large doses, it inhibits the production of red blood cells and lymphocytes. Due to the selective effect, it has a significant effect on chronic myeloid leukemia. BaiXiaoan is currently the main drug for the treatment of chronic myeloid leukemia, and its remission rate can reach 80-90%. But once acute changes occur, the drug should be stopped. |
| Production method | It is obtained by condensation of methyl sulfonyl chloride with 1,4-butanediol. |
| category | toxic substances |
| toxicity classification | highly toxic |
| acute toxicity | abdominal cavity-rat LD50: 22 mg/kg; Oral administration-mouse LD50: 110 mg/kg |
| flammability hazard characteristics | thermal decomposition discharges toxic sulfur oxide smoke |
| storage and transportation characteristics | warehouse ventilation and low temperature drying; Store separately from oxidants and acids; Not easy to store for a long time to prevent polymerization |
| fire extinguishing agent | water, dry powder, dry sand, carbon dioxide, foam, 1211 fire extinguishing agent |
| toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |
Last Update：2024-04-09 02:00:09
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