CAS 121032-29-9|Nelarabine

Introduction：Basic information about CAS 121032-29-9|Nelarabine, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Nelarabine BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Synonyms

Common Name	Nelarabine
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	/	Flash Point	389.9±35.7 °C

Names

Name	nelarabine
Synonym	More Synonyms

Nelarabine BiologicalActivity

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.
Related Catalog	Signaling Pathways >>Cell Cycle/DNA Damage >>Nucleoside Antimetabolite/AnalogResearch Areas >>Cancer
References	[1]. Beesley AH, et al. In vitro cytotoxicity of nelarabine, clofarabine and flavopiridol in paediatric acute lymphoblastic leukaemia. Br J Haematol. 2007 Apr;137(2):109-16. [2]. DeAngelo DJ, et al. Nelarabine induces complete remissions in adults with relapsed or refractory T-lineage acute lymphoblastic leukemia or lymphoblastic lymphoma: Cancer and Leukemia Group B study 19801. Blood. 2007 Jun 15;109(12):5136-42.

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.

Related Catalog

Signaling Pathways >>Cell Cycle/DNA Damage >>Nucleoside Antimetabolite/AnalogResearch Areas >>Cancer

References

[1]. Beesley AH, et al. In vitro cytotoxicity of nelarabine, clofarabine and flavopiridol in paediatric acute lymphoblastic leukaemia. Br J Haematol. 2007 Apr;137(2):109-16.

[2]. DeAngelo DJ, et al. Nelarabine induces complete remissions in adults with relapsed or refractory T-lineage acute lymphoblastic leukemia or lymphoblastic lymphoma: Cancer and Leukemia Group B study 19801. Blood. 2007 Jun 15;109(12):5136-42.

Chemical & Physical Properties

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
InChIKey	IXOXBSCIXZEQEQ-UHTZMRCNSA-N
SMILES	COc1nc(N)nc2c1ncn2C1OC(CO)C(O)C1O

Safety Information

Hazard Codes	Xi

Synonyms

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

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