A1412-1ml | Clofarabine [123318-82-1] Clinisciences

Background

Clofarabine is a DNA synthesis inhibitor and a substrate of Deoxycytidine kinase (dCK).
DCK is a key cytosolic enzyme in the DNA-synthesis salvage pathway and is responsible for the phosphorylation of clofarabine.
Clofarabine is phosphorylated to form clofarabine triphosphate, which competes with dATP for DNA polymerase-α and -ε. At the same time, clofarabine-monophosphate is incorporated into internal and terminal DNA sites, which impaired DNA elongation and repair. Clofarabine triphosphate inhibits ribonucleotide reductase with IC50 value of 65 nM, which then reduced dCTP and dATP. Clofarabine is efficiently transported into cells through nucleoside transporters hENT1, hENT2, and hCNT2. Clofarabine results in release of cytochrome c, apoptosis protease-activating factor 1 (APAF1), apoptotic-inducing factor (AIF) and caspase 9 into the cytosol. In both rapidly growing and quiescent tumours, clofarabine has anticancer activity because of its inhibition of DNA synthesis and induction of apoptosis.
Implanted human tumour xenografts in athymic nude or severe combined immune deficiency mice, Clofarabine administered intraperitoneally had significant antitumor activity.
References:
[1]. Bonate PL, Arthaud L, Cantrell WR Jr, et al. Discovery and development of clofarabine: a nucleoside analogue for treating cancer. Nat Rev Drug Discov, 2006, 5(10): 855-863.

Chemical Properties

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	303.68
Cas No.	123318-82-1
Formula	C₁₀H₁₁ClFN₅O₃
Solubility	insoluble in H2O; insoluble in EtOH; ≥15.18 mg/mL in DMSO
Chemical Name	(2R,3R,4S,5R)-5-(6-amino-2-chloropurin-9-yl)-4-fluoro-2-(hydroxymethyl)oxolan-3-ol
SDF	Download SDF
Canonical SMILES	C1=NC2=C(N1C3C(C(C(O3)CO)O)F)N=C(N=C2N)Cl
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Purity = 99.41%

Chemical structure

Clofarabine [123318-82-1]

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Background

Chemical Properties

Quality Control

Chemical structure

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