Cladribine

ArtNr	S1199-25
Hersteller	Selleckchem
CAS-Nr.	4291-63-8
Menge	25 mg
Quantity options	100 mg 1 g 10 g 10 mM/1 mL 200 mg 25 mg 50 mg 5 g
Kategorie	Oncology Neuroscience Neural Lineage Markers Neuroinflammation Neural Transcription Factors Aging & Neurological Disorders Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Bladder Cancer Colorectal Cancer Breast Cancer Heart & Blood Cancer Testicular & Prostate Cancer
Typ	Inhibitors
Specific against	other
Smiles	C1C(C(OC1N2C=NC3=C(N=C(N=C32)Cl)N)CO)O
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	2-CdA,2-Chloro-2′-deoxyadenosine,CldAdo,Jk 6251,NSC 105014,RWJ 26251
Similar products	Cladribine
Lieferbar
Storage Conditions	2 years -80 in solvent
Molecular Weight	285, 69
Administration	Administered via i.p.
Animal Models	Adult wild-type (AB) zebrafish
Cell lines	U266, RPMI8226 and MM1.S
Clinical Trials	Cladribine plus Rituximab has entered in a phase II clinical trial in the treatment of leukemia.
Concentrations	0 uM - 32 uM
Dosages	0.7 mM - 3.5 mM
Formulation	Saline
IC50	2.43 uM, 2.43 uM, 2.43 uM, 2.43 uM, 2.43 uM, 2.43 uM
In vitro	Cladribine exerts remarkable activity in hairy cell leukemia (HCL), a chronic B-cell lymphoproliferative disorder, producing prolonged complete remissions. Cladribine induces accumulation of DNA strand breaks, and subsequently activates the tumor suppressor p53 in lymphocytes. Cladribine may modulate STAT3 activity in MM cells. Cladribine inhibits proliferation/survival of U266, RPMI8226 and MM1.S cells in a dose-dependent manner. While U266 is the least sensitive cell line, MM1.S is the most sensitive one to cladribine. Treatment with cladribine gradually increases the percentage of cells in the G1 phase of the cell cycle and reduces the percentage of cells in S phase. Cladribine appears to increase G2-M phase in U266 cells upon 24 hour-treatment. A dose-dependent increase in apoptosis induced by cladribine is seen in both RPMI8226 and MM1.S cells. Treatment with cladribine at 0.2 uM dramatically induces activation of caspase-3, -8, and -9 and PARP cleavage in a time-dependent manner in MM1.S. Cladribine significantly decreases the phospho-STAT3 (P-STAT3) levels in a dose-dependent manner, but has no effect on the total STAT3 protein levels. [1] Cladribine possesses concentration-dependent apoptosis-inducing potential in the HSB2 cells. [2] Cladribine inhibits growth of primary mast cell (MC) and the MC line HMC-1 in a dose-dependent manner, with lower IC50 values recorded in HMC-1.2 cells harboring KIT D816V compared to HMC-1.1 cells lacking KIT D816V. [3] Cladribine decreases the migratory capacity of CD14+ monocytes, as well as of CD4+ and CD8+ T lymphocytes. [4]
In vivo	Cladribine (0.7-3.5 mM) and/or diltiazem (2.4 mM), is injected intraperitoneally into adult zebrafish and red blood cell (RBC) lysates are assayed by HPLC for levels of purine nucleotides (e.g. ATP), potential biomarkers of cardiovascular health. Diltiazem increased RBC ATP concentrations, which are inhibited by co-injection of cladribine. [5] Plasma concentrations of Cladribine decreases rapidly following a biphasic decline after both ia and s.c. administrations. The AUC and t 1/2 beta after a single 1 mg/kg ia and 2 mg/kg s.c. injection of Cladribine are 0.66 vs 1.2 ug, h/mL and 3.5 vs 4.5 hours, respectively. [6]
Incubation Time	72 hours
Method	The non-radioactive cell proliferation kit is used to determine cell viability. In brief, Human MM cell line U266, RPMI8226 and MM1.S are seeded onto 96-well plates with either 0.1 mL complete medium (5% FBS) as control, or 0.1 mL of the same medium containing a series of doses of cladribine, and incubated for 72 hours. After reading all wells at 490 nm with a micro-plate reader, the percentages of surviving cells from each group relative to controls, defined as 100% survival, are determined by reduction of MTS.
Solubility (25C)	DMSO 57 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	Cladribine is an adenosine deaminase inhibitor for U266, RPMI8226, and MM1.S cells with IC50 of approximately 2.43 μM, 0.75 μM, and 0.18 μM, respectively.
Chemical Name	(2R, 3S, 5R)-5-(6-amino-2-chloro-9H-purin-9-yl)-2-(hydroxymethyl)-tetrahydrofuran-3-ol
Features	Cladribine is primarily active in lymphoid tissues.

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