Clofarabine

Modify Date: 2024-01-02 06:04:33

Clofarabine structure	Common Name	Clofarabine
	CAS Number	123318-82-1	Molecular Weight	303.677
	Density	2.1±0.1 g/cm3	Boiling Point	599.5±60.0 °C at 760 mmHg
	Molecular Formula	C₁₀H₁₁ClFN₅O₃	Melting Point	228-2310C
	MSDS	Chinese USA	Flash Point	316.4±32.9 °C
	Symbol	GHS06	Signal Word	Danger

Use of Clofarabine

Clofarabine(Clolar; Clofarex) inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase.IC50 Value: 65 nMTarget: in vitro: Clofarabine is a second generation purine nucleoside analog with antineoplastic activity. It is phosphorylated intracellularly, which inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase, resulting in inhibition of DNA repair and synthesis of DNA and RNA. This nucleoside analog also disrupts mitochondrial function and membrane integrity, resulting in the release of pre-apoptotic factors, including cytochrome C and apoptotic-inducing factor, which activate apoptosis.in vivo: Clofarabine is used for treating relapsed or refractory acute lymphoblastic leukaemia (ALL) in children, after at least two other types of treatment have failed.

Name	clofarabine
Synonym	More Synonyms

Description	Clofarabine(Clolar; Clofarex) inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase.IC50 Value: 65 nMTarget: in vitro: Clofarabine is a second generation purine nucleoside analog with antineoplastic activity. It is phosphorylated intracellularly, which inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase, resulting in inhibition of DNA repair and synthesis of DNA and RNA. This nucleoside analog also disrupts mitochondrial function and membrane integrity, resulting in the release of pre-apoptotic factors, including cytochrome C and apoptotic-inducing factor, which activate apoptosis.in vivo: Clofarabine is used for treating relapsed or refractory acute lymphoblastic leukaemia (ALL) in children, after at least two other types of treatment have failed.
Related Catalog	Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Cell Cycle/DNA Damage >> Nucleoside Antimetabolite/Analog Research Areas >> Cancer Research Areas >> Metabolic Disease
References	[1]. Bonate et al Discovery and development of clofarabine: a nucleoside analogue for treating cancer. Nat.Rev.Drug Discov. (2006)5 855. [2]. Ghanem H, Kantarjian H, Ohanian M, Jabbour E.The Role of Clofarabine in Acute Myeloid Leukemia.Leuk Lymphoma. 2012 Sep 7. [3]. Abd Elmoneim A, Gore L, Ricklis RM, Boklan J, Cooper T, Narendran A, Rolla K, Scott T, Arceci RJ.Phase I dose-escalation trial of clofarabine followed by escalating doses of fractionated cyclophosphamide in children with relapsed or refractory acute leukemias.Pediatr Blood Cancer. 2012 Aug 8. doi: 10.1002/pbc.24264. [4]. Thudium KE, Ghoshal S, Fetterly GJ, Haese JP, Karpf AR, Wetzler M.Synergism between clofarabine and decitabine through p53R2: A pharmacodynamic drug-drug interaction modeling.Leuk Res. 2012 Aug 9. [5]. Aye Y, Brignole EJ, Long MJ, Chittuluru J, Drennan CL, Asturias FJ, Stubbe J.Clofarabine Targets the Large Subunit (α) of Human Ribonucleotide Reductase in Live Cells by Assembly into Persistent Hexamers.Chem Biol. 2012 Jul 27;19(7):799-805.

Description

Related Catalog

Signaling Pathways >> Autophagy >> Autophagy

Signaling Pathways >> Cell Cycle/DNA Damage >> Nucleoside Antimetabolite/Analog

Research Areas >> Cancer

Research Areas >> Metabolic Disease

References

[1]. Bonate et al Discovery and development of clofarabine: a nucleoside analogue for treating cancer. Nat.Rev.Drug Discov. (2006)5 855.

[2]. Ghanem H, Kantarjian H, Ohanian M, Jabbour E.The Role of Clofarabine in Acute Myeloid Leukemia.Leuk Lymphoma. 2012 Sep 7.

[3]. Abd Elmoneim A, Gore L, Ricklis RM, Boklan J, Cooper T, Narendran A, Rolla K, Scott T, Arceci RJ.Phase I dose-escalation trial of clofarabine followed by escalating doses of fractionated cyclophosphamide in children with relapsed or refractory acute leukemias.Pediatr Blood Cancer. 2012 Aug 8. doi: 10.1002/pbc.24264.

[4]. Thudium KE, Ghoshal S, Fetterly GJ, Haese JP, Karpf AR, Wetzler M.Synergism between clofarabine and decitabine through p53R2: A pharmacodynamic drug-drug interaction modeling.Leuk Res. 2012 Aug 9.

[5]. Aye Y, Brignole EJ, Long MJ, Chittuluru J, Drennan CL, Asturias FJ, Stubbe J.Clofarabine Targets the Large Subunit (α) of Human Ribonucleotide Reductase in Live Cells by Assembly into Persistent Hexamers.Chem Biol. 2012 Jul 27;19(7):799-805.

Density	2.1±0.1 g/cm3
Boiling Point	599.5±60.0 °C at 760 mmHg
Melting Point	228-2310C
Molecular Formula	C₁₀H₁₁ClFN₅O₃
Molecular Weight	303.677
Flash Point	316.4±32.9 °C
Exact Mass	303.053436
PSA	119.31000
LogP	0.24
Vapour Pressure	0.0±1.8 mmHg at 25°C
Index of Refraction	1.844

Clofarabine MSDS(Chinese)

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UD7473000

CHEMICAL NAME :: 9H-Purin-6-amine, 2-chloro-9-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl) -

CAS REGISTRY NUMBER :: 123318-82-1

LAST UPDATED :: 199706

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C10-H11-Cl-F-N5-O3

MOLECULAR WEIGHT :: 303.71

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

TYPE OF TEST :: DNA inhibition

TEST SYSTEM :: Human Leukocyte

DOSE/DURATION :: 50 nmol/L

REFERENCE :: CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 51,2386,1991

Symbol	GHS06
Signal Word	Danger
Hazard Statements	H300
Precautionary Statements	P264-P301 + P310
Personal Protective Equipment	Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges
Hazard Codes	Xi,C
Risk Phrases	R36/37/38:Irritating to eyes, respiratory system and skin . R20/21/22:Harmful by inhalation, in contact with skin and if swallowed .
Safety Phrases	S26-S36-S45-S36/37/39
RIDADR	UN 2735 8/PG 3
WGK Germany	3
RTECS	DP5550000
Packaging Group	III
Hazard Class	8

Precursor 9
CAS#:355138-50-0 2-Chloro-9-(2-d... CAS#:97614-43-2 2-Deoxy-2-fluor... CAS#:97614-44-3 2-Deoxy-2-fluor... CAS#:6974-32-9 b-D-Ribofuranos...
CAS#:1839-18-5 2-chloroadenine CAS#:1055168-98-3 2',3',5'-tri-O-... CAS#:1353040-42-2 2-chloro-9-(3',... CAS#:103884-99-7 9H-Purine, 9-(3...
CAS#:75788-35-1 benzyl 2-acetam...
DownStream 2
CAS#:1839-18-5 2-chloroadenine CAS#:850883-62-4 α-2d2F-Ara-1-P

The potential of clofarabine in MLL-rearranged infant acute lymphoblastic leukaemia.

Eur. J. Cancer 51 , 2008-21, (2015)

MLL-rearranged acute lymphoblastic leukaemia (ALL) in infants is the most difficult-to-treat type of childhood ALL, displaying a chemotherapy-resistant phenotype, and unique histone modifications, gen...

Preclinical examination of clofarabine in pediatric ependymoma: intratumoral concentrations insufficient to warrant further study.

Cancer Chemother. Pharmacol. 75 , 897-906, (2015)

Clofarabine, a deoxyadenosine analog, was an active anticancer drug in our in vitro high-throughput screening against mouse ependymoma neurospheres. To characterize the clofarabine disposition in mice...

Knockdown of Bcl-xL enhances growth-inhibiting and apoptosis-inducing effects of resveratrol and clofarabine in malignant mesothelioma H-2452 cells.

J. Korean Med. Sci. 29(11) , 1464-72, (2014)

Mcl-1 and Bcl-xL, key anti-apoptotic proteins of the Bcl-2 family, have attracted attention as important molecules in the cell survival and drug resistance. In this study, we investigated whether inhi...

Clofarex

(2R,3R,4S,5R)-5-(6-amino-2-chloropurin-9-yl)-4-fluoro-2-(hydroxymethyl)oxolan-3-ol

(2R,3R,4S,5R)-5-(6-amino-2-chloro-9H-purin-9-yl)-4-fluoro-2-(hydroxyméthyl)tétrahydrofuran-3-ol

9H-Purin-6-amine, 2-chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-

2-Chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)adenine

(2R,3R,4S,5R)-5-(6-Amino-2-chlor-9H-purin-9-yl)-4-fluor-2-(hydroxymethyl)tetrahydrofuran-3-ol

(2R,3R,4S,5R)-5-(6-amino-2-chloro-9H-purin-9-yl)-4-fluoro-2-(hydroxymethyl)tetrahydrofuran-3-ol

2-chloro-2'-arabino-fluoro-2'-deoxyadenosine

Cl-F-Ara-A

Clofarabine

Clofarabine [USAN]

Clolar

2-Chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-9H-purin-6-amine

MFCD00871077

Shanghai Jizhi Biochemical Technology Co., Ltd
China
Product Name: Clofarabine
Price: ￥288.0/5mg ￥4008.0/100mg ￥13418.0/500mg ￥878.0/25mg
Purity: 99.0%
Stocking Period: 2 Day
Contact: Liu jia

DC Chemicals Limited
China
Product Name: Clofarabine
Price: $250.0/100mg $500.0/250mg $1000.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: Clofarabine
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

Zhejiang Hangyu API Co., Ltd
China
Product Name: Clofarabine
Price: ￥Inquiry/1kg
Purity: 99.5%
Stocking Period: Inquiry
Contact: Vinnie

Henan Tianfu Chemical Co., Ltd.
China
Product Name: 6-Amino-2-chloro-9-(2'-deoxy-2'-fluoro-b-D-arabinofuranosyl)purine
Price: $Inquiry/1kg $Inquiry/25kg $Inquiry/1000kg $Inquiry/10ton
Purity: 99.0%
Stocking Period: Inquiry
Contact: Anson

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Price: $73/10mM*1mLinDMSO

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Clofarabine

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