In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml
Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
Biological Activity
Description
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.
Targets
Adenosine deaminase (MM1.S cells)
Adenosine deaminase (RPMI8226 cells)
Adenosine deaminase (U266 cells)
0.18 μM
0.75 μM
2.43 μM
In vitro
Cladribine exerts remarkable activity in hairy cell leukaemia (HCL), a chronic B-cell lymphoproliferative disorder, producing prolonged complete remissions. This compound induces accumulation of DNA strand breaks, and subsequently activates the tumour suppressor p53 in lymphocytes. It may modulate STAT3 activity in MM cells. This chemical 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 this compound gradually increases the percentage of cells in the G1 phase of the cell cycle and reduces the percentage of cells in S phase. It appears to increase G2-M phase in U266 cells upon 24 hour-treatment. A dose-dependent increase in apoptosis induced by this agent is seen in both RPMI8226 and MM1.S cells. Treatment with it at 0.2 μM dramatically induces activation of caspase-3, -8, and -9 and PARP cleavage in a time-dependent manner in MM1.S. This compound significantly decreases the phospho-STAT3 (P-STAT3) levels in a dose-dependent manner, but has no effect on the total STAT3 protein levels. It possesses concentration-dependent apoptosis-inducing potential in the HSB2 cells. This chemical 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 harbouring KIT D816V compared to HMC-1.1 cells lacking KIT D816V. It decreases the migratory capacity of CD14+ monocytes, as well as of CD4+ and CD8+ T lymphocytes.
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 this compound. Plasma concentrations of this chemical decrease 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 this compound are 0.66 vs 1.2 μg × h/mL and 3.5 vs 4.5 hours, respectively.
Features
Cladribine is primarily active in lymphoid tissues.
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.
ABT199/venetoclax synergism with thiotepa enhances the cytotoxicity of fludarabine, cladribine and busulfan in AML cells
[ Oncotarget, 2024, 15:220-231]
Synergistic effect of HDAC inhibitor Chidamide with Cladribine on cell cycle arrest and apoptosis by targeting HDAC2/c-Myc/RCC1 axis in acute myeloid leukemia
[ Exp Hematol Oncol, 2023, 12(1):23]
Antineoplastic efficacy profiles of avapritinib and nintedanib in KIT D816V+ systemic mastocytosis: a preclinical study
[ Am J Cancer Res, 2023, 13(2):355-378]
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei
[ J Pers Med, 2022, 12(2)258]
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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