4291-63-8 Cladribine CAS NO.4291-63-8
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- Min.Order: 1 Kilogram
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A(10-150)Kilogram
- Product Details
Keywords
- 4291-63-8 Cladribine
- 4291-63-8 Cladribine
- 4291-63-8 Cladribine
Quick Details
- ProName: 4291-63-8 Cladribine
- CasNo: 4291-63-8
- Molecular Formula: C10H12ClN5O3
- Appearance: White powder
- Application: Organic Chemicals
- DeliveryTime: according to client's demand quantity
- PackAge: as requested
- Port: SHANGHAI
- ProductionCapacity: 100 Metric Ton/Year
- Purity: 99%
- Storage: room temperature
- Transportation: by Sea
- LimitNum: 1 Kilogram
- Heavy metal: 0.01
- Grade: Industrial Grade,Pharma Grade
- Transportation: LCL
Superiority
Product Name: Cladribine
Synonyms: CDA;CLADRIBINE;CLADRIBINE CDA;LABOTEST-BB LT01147851;2-CHLORO-2'-DEOXYADENOSINE;2CDA;2-CL-DADO;2-chloro-2’-deoxy-adenosin
CAS: 4291-63-8
MF: C10H12ClN5O3
MW: 285.69
EINECS: 636-978-6
Product Categories: API;Anti-cancer&immunity;Inhibitors;Bases & Related Reagents;Nucleotides;Pharmaceuticals
Mol File: 4291-63-8.mol
Cladribine Chemical Properties
Melting point 181-185 °C(lit.)
alpha D25 -18.8° (c = 1 in DMF)
Boiling point 547.6±60.0 °C(Predicted)
density 2.03±0.1 g/cm3(Predicted)
storage temp. 2-8°C
solubility Slightly soluble in water, soluble in dimethyl sulfoxide, slightly soluble in methanol, practically insoluble in acetonitrile. It shows polymorphism (5.9).
form White solid
pka 13.75±0.60(Predicted)
λmax 265nm(EtOH aq.)(lit.)
Merck 14,2337
Stability: Store in Freezer
InChIKey PTOAARAWEBMLNO-HSUXUTPPSA-N
CAS DataBase Reference 4291-63-8(CAS DataBase Reference)
Safety Information
Hazard Codes T
Risk Statements 36/37/38-23/24/25
Safety Statements 26-37/39-45-36-22
RIDADR UN 2811 6.1 / PGIII
WGK Germany 3
RTECS AU7357560
HS Code 29349990
Hazardous Substances Data 4291-63-8(Hazardous Substances Data)
Toxicity LD50 intraperitoneal in mouse: 150mg/kg
Details
Cladribine Usage And Synthesis
Description Cladribine (2-chloro-2′-deoxyadenosine) is an adenosine deaminase-resistant analogue of deoxyadenosine. The drug has a broad range of in vitro activity against both lymphoid and myeloid neoplasms [mean IC50values (drug concentration required to inhibit cell growth by 50% of control): 20 to 87 nmol/L]. But it possesses little activity against multiple myeloma specimens and many solid tumor cell lines. Monocytes are highly sensitive to cladribine in vitro. Cladribine demonstrates activity against both dividing and nondividing cells and this activity distinguishes it from many other agents. It has activity in murine models of leukaemia. Cladribine is used to treat chronic progressive multiple sclerosis, hairy cell leukemia, systemic mastocytosis, and histiocytosis (including Erdheim–Chester disease and Langerhans cell histiocytosis).
After a 2-hour intravenous infusion of cladribine 0.14 mg/kg/day, the mean maximum plasma drug concentration was 198 nmol/L. Intracellular concentrations of phosphorylated cladribine derivatives exceed plasma concentrations 128- to 375-fold. Cladribine penetrates into the CSF. The terminal elimination half-life (6.7 hours) is long, which suggests that the drug may be administered intermittently without loss of efficacy. The volume of distribution of cladribine is 9.2 L/kg.
References [1] J.C Sipe, J. S Romine, R. McMillan, E. Beutler, J. C. Sipe, J. S. Romine, J. Zyroff (1994) Cladribine in treatment of chronic progressive multiple sclerosis, 344, 9-13
[2] Alan Saven, Carol Burian (1999) Cladribine Activity in Adult Langerhans-Cell Histiocytosis, 93, 4125-4130
[3] #
[4] Harriet M. Bryson, Eugene M. Sorkin (1993) Cladribine: A Review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in haematological malignancies, 46, 872-894
Description Cladribine, an adenosine deaminase inhibitor, was introduced in the United States as a single intravenous treatment for hairy cell leukemia. The incorporation of a chlorine atom at the 2-position of deoxyadenosine renders cladribine more resistant to enzymatic attack by adenosine deaminase, resulting in a more prolonged cytotoxic effect. Cladribine efficiently crosses lymphocyte and monocyte cell membranes and is metabolized in cells to the biologically active triphosphate, which inhibits DNA synthesis. While most antineoplastic drugs are active primarily against dividing cells, cladribine destroys both resting and proliferating cells. Its potential uses in the treatment of autoimmune hemolytic anemia, multiple sclerosis, chronic lymphocytic leukemia and various lymphomas have also been evaluated.
Chemical Properties White Crystalline Solid
Originator Johnson & Johnson (U.S.A.)
Uses It is a substituted purine nucleoside with antileukemic activity
Indications Cladribine (Leustatin) is a synthetic purine nucleoside that is converted to an active cytotoxic metabolite by the enzyme deoxycytidine kinase. Like the other purine antimetabolites, it is relatively selective for both normal and malignant lymphoid cells and kills resting as well as dividing cells by mechanisms that are not completely understood.
The drug is highly active against hairy cell leukemia, producing complete remissions in more than 60% of patients treated with a single 7-day course. Activity has also been noted in other low-grade lymphoid malignancies. The major side effect is myelosuppression.
Definition ChEBI: 2'-Deoxyadenosine in which the hydrogen at position 2 on the purine ring has been substituted by chlorine. It inhibits the synthesis and repair of DNA, particularly in lymphocytes and monocytes, and is used as an antimetabolite antineoplastic drug for the treatment of lymphoid malignancies including hairy-cell leukaemia and chronic lymphocytic leukaemia.