Nelarabine
Modify Date: 2024-01-02 10:19:41
Nelarabine structure
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Common Name | Nelarabine | ||
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| CAS Number | 121032-29-9 | Molecular Weight | 297.267 | |
| Density | 2.0±0.1 g/cm3 | Boiling Point | 721.0±70.0 °C at 760 mmHg | |
| Molecular Formula | C11H15N5O5 | Melting Point | 209-217ºC | |
| MSDS | N/A | Flash Point | 389.9±35.7 °C | |
Use of NelarabineNelarabine (Arranon, 506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells. Nelarabine is a chemotherapy drug used in T-cell acute lymphoblastic leukemia. IC50 Value: 0.44 uM (HSB2 cell lines); 1.24 μM(ALL-SIL cell lines); 2.15 μM(JURKAT cell lines); 0.067 uM (PER-255 cell lines) [1]Target: Nucleoside antimetabolite/analogin vitro: The IC50 of Nelarabine is 25-fold and 113-fold higher than ARAC in T- and B-lineage, respectively. T-ALL cells are eightfold more sensitive to Nelarabine than B-lineage but there is considerable overlap. The efficacy of NEL in T-lineage and B-lineage cell lines is 25-fold and 113-fold less than ARAC, respectively [1].in vivo: The median age was 34 years (range, 16-66 years); 32 (82%) patients were male. The rate of complete remission was 31% (95% confidence interval [CI], 17%, 48%) and the overall response rate was 41% (95% CI, 26%, 58%). The principal toxicity was grade 3 or 4 neutropenia and thrombocytopenia, occurring in 37% and 26% of patients, respectively [2]. Nelarabine has activity in T-cell malignancies, as evaluated in 2 Phase I and 5 Phase II studies. It received accelerated approval from the FDA based on the resuits of 2 Phase II trials, one in pediatric patients (PGAA 2001) and the other in adults (CALGB 19801)Toxicity: The principal toxicity was grade 3 or 4 neutropenia and thrombocytopenia, occurring in 37% and 26% of patients, respectively [2].Clinical trial: Drug Use Investigation for Arranon G (Nelarabine) Injection 250 mg. |
| Name | nelarabine |
|---|---|
| Synonym | More Synonyms |
| Description | Nelarabine (Arranon, 506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells. Nelarabine is a chemotherapy drug used in T-cell acute lymphoblastic leukemia. IC50 Value: 0.44 uM (HSB2 cell lines); 1.24 μM(ALL-SIL cell lines); 2.15 μM(JURKAT cell lines); 0.067 uM (PER-255 cell lines) [1]Target: Nucleoside antimetabolite/analogin vitro: The IC50 of Nelarabine is 25-fold and 113-fold higher than ARAC in T- and B-lineage, respectively. T-ALL cells are eightfold more sensitive to Nelarabine than B-lineage but there is considerable overlap. The efficacy of NEL in T-lineage and B-lineage cell lines is 25-fold and 113-fold less than ARAC, respectively [1].in vivo: The median age was 34 years (range, 16-66 years); 32 (82%) patients were male. The rate of complete remission was 31% (95% confidence interval [CI], 17%, 48%) and the overall response rate was 41% (95% CI, 26%, 58%). The principal toxicity was grade 3 or 4 neutropenia and thrombocytopenia, occurring in 37% and 26% of patients, respectively [2]. Nelarabine has activity in T-cell malignancies, as evaluated in 2 Phase I and 5 Phase II studies. It received accelerated approval from the FDA based on the resuits of 2 Phase II trials, one in pediatric patients (PGAA 2001) and the other in adults (CALGB 19801)Toxicity: The principal toxicity was grade 3 or 4 neutropenia and thrombocytopenia, occurring in 37% and 26% of patients, respectively [2].Clinical trial: Drug Use Investigation for Arranon G (Nelarabine) Injection 250 mg. |
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| Related Catalog | |
| References |
| Density | 2.0±0.1 g/cm3 |
|---|---|
| Boiling Point | 721.0±70.0 °C at 760 mmHg |
| Melting Point | 209-217ºC |
| Molecular Formula | C11H15N5O5 |
| Molecular Weight | 297.267 |
| Flash Point | 389.9±35.7 °C |
| Exact Mass | 297.107330 |
| PSA | 148.77000 |
| LogP | -0.58 |
| Vapour Pressure | 0.0±2.4 mmHg at 25°C |
| Index of Refraction | 1.829 |
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Material Safety Data Sheet
Section1. Identification of the substance Product Name: Nelarabine Synonyms: Section2. Hazards identification Harmful by inhalation, in contact with skin, and if swallowed. Section3. Composition/information on ingredients. Ingredient name:Nelarabine CAS number:121032-29-9 Section4. First aid measures Skin contact:Immediately wash skin with copious amounts of water for at least 15 minutes while removing contaminated clothing and shoes. If irritation persists, seek medical attention. Eye contact:Immediately wash skin with copious amounts of water for at least 15 minutes. Assure adequate flushing of the eyes by separating the eyelids with fingers. If irritation persists, seek medical attention. Inhalation:Remove to fresh air. In severe cases or if symptoms persist, seek medical attention. Ingestion:Wash out mouth with copious amounts of water for at least 15 minutes. Seek medical attention. Section5. Fire fighting measures In the event of a fire involving this material, alone or in combination with other materials, use dry powder or carbon dioxide extinguishers. Protective clothing and self-contained breathing apparatus should be worn. Section6. Accidental release measures Personal precautions: Wear suitable personal protective equipment which performs satisfactorily and meets local/state/national standards. Respiratory precaution:Wear approved mask/respirator Hand precaution:Wear suitable gloves/gauntlets Skin protection:Wear suitable protective clothing Eye protection:Wear suitable eye protection Methods for cleaning up: Mix with sand or similar inert absorbent material, sweep up and keep in a tightly closed container for disposal. See section 12. Environmental precautions: Do not allow material to enter drains or water courses. Section7. Handling and storage Handling:This product should be handled only by, or under the close supervision of, those properly qualified in the handling and use of potentially hazardous chemicals, who should take into account the fire, health and chemical hazard data given on this sheet. Store in closed vessels, refrigerated. Storage: Section8. Exposure Controls / Personal protection Engineering Controls: Use only in a chemical fume hood. Personal protective equipment: Wear laboratory clothing, chemical-resistant gloves and safety goggles. General hydiene measures: Wash thoroughly after handling. Wash contaminated clothing before reuse. Section9. Physical and chemical properties Appearance:Not specified Boiling point:No data No data Melting point: Flash point:No data Density:No data Molecular formula:C11H15N5O5 Molecular weight:297.3 Section10. Stability and reactivity Conditions to avoid: Heat, flames and sparks. Materials to avoid: Oxidizing agents. Possible hazardous combustion products: Carbon monoxide, nitrogen oxides. Section11. Toxicological information No data. Section12. Ecological information No data. Section13. Disposal consideration Arrange disposal as special waste, by licensed disposal company, in consultation with local waste disposal authority, in accordance with national and regional regulations. Section14. Transportation information Non-harzardous for air and ground transportation. Section15. Regulatory information No chemicals in this material are subject to the reporting requirements of SARA Title III, Section 302, or have known CAS numbers that exceed the threshold reporting levels established by SARA Title III, Section 313. SECTION 16 - ADDITIONAL INFORMATION N/A |
| Hazard Codes | Xi |
|---|
| 2-Amino-9-b-D-arabinofuranosyl-6-methoxy-9H-purine |
| 2-Amino-6-methoxypurinribonucleosid |
| 506u |
| MAY |
| 9-(β-D-Arabinofuranosyl)-6-methoxy-9H-purin-2-amine |
| 9-b-D-Arabinofuranosyl-6-methoxy-9H-purin-2-amine |
| (2R,3S,4S,5R)-2-(2-Amino-6-methoxy-9H-purin-9-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol |
| 9-β-D-Arabinofuranosyl-6-methoxy-9H-purin-2-amine |
| (2R,3S,4S,5R)-2-(2-amino-6-méthoxy-9H-purin-9-yl)-5-(hydroxyméthyl)tétrahydrofurane-3,4-diol |
| Nelzarabine |
| 9beta-D-Arabinofuranosyl-6-methoxy-9H-purin-2-amine |
| 9H-Purin-2-amine, 9-β-D-arabinofuranosyl-6-methoxy- |
| Nelarabine |
| O6-methyl-guanosine |
| Arranon |
| GW 506U78 |