Cladribine

Research use only, not for human use.

Cladribine is an adenosine deaminase inhibitor used to treat hairy cell leukemia and multiple sclerosis.

Cladribine is an adenosine deaminase inhibitor used to treat hairy cell leukemia and multiple sclerosis.(In Vitro):Cladribine (0.25-4 μM; 24-48 hours) inhibits human DLBCL cells proliferation.Cladribine (1-4 μM; 24 hours) induces G1 phase arrest via decreasing the expressions of Cyclin D1 and Cyclin E, and increasing the expressions of p21 and p27 in DLBCL cells.Cladribine (1-4 μM; 24 hours) induces apoptosis and activates extrinsic and intrinsic signaling pathways in human DLBCL cells.Cladribine (1-4 μM; 24 hours) activates endoplasmic reticulum stress.Cladribine inhibits cell proliferation of multiple myeloma (MM) cells in a dose-dependent manner; with IC50s of approximately 2.43 μM, 0.75 μM and 0.18 μM for U266, RPMI8226 and MM1.S cells, respectively. (In Vivo):Cladribine (10 μg/kg; i.p.; 3 times/week; for 2 weeks) may have benefits in the treatment of ischemia/reperfusion injury to the biochemical and histopathologic parameters.Cladribine (0.5 mg/kg; i.p.; daily; for 60 days) increases amyloid beta peptide generation and plaque burden in APdE9 mice.Cladribine exhibits Cmax (rat 4.9 ng/mL) following intra-arterial injection.Cladribine exhibits Cmax (rat 1.1 ng/mL) following subcutaneous injection.Cladribine exhibits elimination half-lives (rat 3.5 h) and plasma clearance (rat 2.8 L/h/kg) following intra-arterial injection.Cladribine exhibits elimination half-lives (rat 4.5 h) and plasma clearance (rat 2.3 L/h/kg) following subcutaneous injection.Cladribine administration with s.c. injection may produce more favourable pharmacokinetic profiles than i.a. injection following a single dose.

Cladribine (0.25-4 μM; 24-48 hours) inhibits human DLBCL cells proliferation.Cladribine (1-4 μM; 24 hours) induces G1 phase arrest via decreasing the expressions of Cyclin D1 and Cyclin E, and increasing the expressions of p21 and p27 in DLBCL cells.?Cladribine (1-4 μM; 24 hours) induces apoptosis and activates extrinsic and intrinsic signaling pathways in human DLBCL cells.Cladribine (1-4 μM; 24 hours) activates endoplasmic reticulum stress.Cladribine inhibits cell proliferation of multiple myeloma (MM) cells in a dose-dependent manner; with IC50s of approximately 2.43 μM, 0.75 μM and 0.18 μM for U266, RPMI8226 and MM1.S cells, respectively. Cell Proliferation AssayCell Line:The human DLBCL cell lines (U2932, OCI-LY10, SUDHL2, WSU-DLCL2, DB) Concentration:0 μM, 0.25 μM, 0.5 μM, 1 μM, 2 μM, 4 μM Incubation Time:24 hours, 48 hours Result:Exhibited notable suppression of cell proliferation in five DLBCL cells.Western Blot Analysis Cell Line:U2932 cells, WSU-DLCL2 cells Concentration:0 μM, 1 μM, 2 μM, 4 μM Incubation Time:24 hours Result:Decreased the expressions of Cyclin D1 and Cyclin E, and increased the expressions of p21 and p27.Apoptosis Analysis Cell Line:U2932 cells, WSU-DLCL2 cells Concentration:0 μM, 1 μM, 2 μM, 4 μM Incubation Time:24 hours Result:Induced apoptosis and activates exogenous and endogenous apoptotic signaling pathways.Cell Cycle Analysis Cell Line:U2932 cells, WSU-DLCL2 cells Concentration:0 μM, 1 μM, 2 μM, 4 μM Incubation Time:24 hours Result:Caused G1 phase arrest.RT-PCR Cell Line:U2932 cells, WSU-DLCL2 cells Concentration:0 μM, 1 μM, 2 μM, 4 μM Incubation Time:24 hours Result:Activated ER stress.

Cladribine (10 μg/kg; i.p.; 3 times/week; for 2 weeks) may have benefits in the treatment of ischemia/reperfusion injury to the biochemical and histopathologic parameters.?Cladribine (0.5 mg/kg; i.p.; daily; for 60 days) increases amyloid beta peptide generation and plaque burden in APdE9 mice.Cladribine exhibits Cmax (rat 4.9 ng/mL) following intra-arterial injection.Cladribine exhibits Cmax (rat 1.1 ng/mL) following subcutaneous injection.Cladribine exhibits elimination half-lives (rat 3.5 h) and plasma clearance (rat 2.8 L/h/kg) following intra-arterial injection.Cladribine exhibits elimination half-lives (rat 4.5 h) and plasma clearance (rat 2.3 L/h/kg) following subcutaneous injection.Cladribine administration with s.c. injection may produce more favourable pharmacokinetic profiles than i.a. injection following a single dose. Animal Model:Male Sprague-Dawley rats, ischemic injury model Dosage:10 μg/kg Administration:Intraperitoneal injection, 3 times/week, for 2 weeks Result:Might increase expression of Sphk1 and consecutively SphK1 suppressed HIF-1α.Animal Model:Male Sprague Dawley rats (350-450 g) Dosage:2 mg/kg for s.c., 1 mg/kg for i.a. (Pharmacokinetic Analysis) Administration:Subcutaneous injection, intra-arterial Result:Cmax (4.9 ng/mL i.a.; 1.1 ng/mL s.c.), T1/2 β (3.5 h i.a.; 4.5 s.c.).

Biodribin | ?2-Chlorodeoxyadenosine | Jk 6251 | Leustatin | NSC 105014 | RWJ 26251

Endocrinology/Hormones

AChR

Adenosine deaminase (MM1.S cells)| Adenosine deaminase (RPMI8226 cells)| Adenosine deaminase (U266 cells)

Cancer

——

4291-63-8

285.69

C10H12ClN5O3

>98% (HPLC)

DMSO: 57 mg/mL (199.51 mM)

O[C@@H]1[C@@H](CO)O[C@@H](N2C=NC3=C(N)N=C(Cl)N=C23)C1

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

(-20℃)

With Ice Pack

≥ 2 years