Cladribine
- CAS No.
- 4291-63-8
- Chemical Name:
- Cladribine
- Synonyms
- CDA;Leustat;(2R,3S,5R)-5-(6-aMino-2-chloro-9H-purin-9-yl)-2-(hydroxyMethyl)tetrahydrofuran-3-ol;2CDA;CldAdo;2-Cl-dA;Jk 6251;CS-1392;rwj26251;Leustati
- CBNumber:
- CB4222723
- Molecular Formula:
- C10H12ClN5O3
- Molecular Weight:
- 285.69
- MOL File:
- 4291-63-8.mol
- Modify Date:
- 2024/7/26 17:49:17
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. | -20°C |
solubility | Slightly soluble in water, soluble in dimethyl sulfoxide, slightly soluble in methanol, practically insoluble in acetonitrile. It shows polymorphism (5.9). |
pka | 13.75±0.60(Predicted) |
form | White solid |
color | White to Pale Yellow |
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
Risk and Safety Statements
Symbol(GHS) | GHS06,GHS08 |
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Signal word | Danger | |||||||||
Hazard statements | H301-H341-H361fd-H372 | |||||||||
Precautionary statements | P201-P202-P260-P264-P270-P301+P310 | |||||||||
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 | |||||||||
Toxicity | LD50 intraperitoneal in mouse: 150mg/kg | |||||||||
NFPA 704 |
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Cladribine price More Price(4)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich(India) | C4438 | 2-Chloro-2′-deoxyadenosine antileukemic | 4291-63-8 | 10MG | ₹25265.55 | 2022-06-14 | Buy |
Sigma-Aldrich(India) | C4438 | 2-Chloro-2′-deoxyadenosine antileukemic | 4291-63-8 | 25MG | ₹57036.93 | 2022-06-14 | Buy |
Sigma-Aldrich(India) | 220467 | 2-Chloro-2ʹ-deoxyadenosine - CAS 4291-63-8 - Calbiochem A deoxyadenosine analog that displays strong antileukemic and immunosuppressive activity. | 4291-63-8 | 10MG | ₹8210 | 2022-06-14 | Buy |
TCI Chemicals (India) | C2499 | Cladribine | 4291-63-8 | 50MG | ₹19800 | 2022-05-26 | Buy |
Cladribine Chemical Properties,Uses,Production
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
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.
General Description
The drug is available in a 10-mg or 10-mL single-use vialfor IV use. Cladribine is used for chronic lymphocyticleukemia, hairy cell leukemia, and non-Hodgkin’s lymphoma.The mechanism of action of this purine deoxyadenosineanalog involves incorporation into DNA resultingin inhibition of DNA chain extension and inhibitionof DNA synthesis and function. This incorporation intoDNA occurs via the triphosphate metabolite active species.The 2-chloro group on the adenine ring produces resistanceto breakdown by adenosine deaminase. Resistance to the anticancereffects can occur because of decreased expressionof the activating enzyme or overexpression of the catabolicenzymes. Oral bioavailability is variable and averages about50%. The drug crosses the blood-brain barrier; however,CSF concentrations reach only 25% of those in plasma. Thedrug is selectively activated inside the cell, and intracellularconcentrations of phosphorylated metabolites exceed thosein plasma. Toxicities include myelosuppression, neutropenia,immunosuppression, fever, nausea, and vomiting.
Cladribine Preparation Products And Raw materials
Raw materials
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Supplier | Tel | Country | ProdList | Advantage | Inquiry |
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Hetero Drugs Limited | +91-4023704923 +91-4023704923 | Telangana, India | 296 | 58 | Inquiry |
Ralington Pharma | +91-7948911722 +91-9687771722 | Gujarat, India | 1350 | 58 | Inquiry |
Biophore India Pharmaceuticals Pvt Ltd | +91-9100031592 +91-9030907714 | Telangana, India | 134 | 58 | Inquiry |
Mac Chem Products (India) Pvt Ltd (Naprod Group) | +91-9727753234 +91-7770016606 | Maharashtra, India | 37 | 58 | Inquiry |
Aspen Biopharma Labs Pvt Ltd | +91-9248058660 +91-9248058662 | Telangana, India | 234 | 58 | Inquiry |
Hetero Drugs Limited | 08048372500Ext 439 | Hyderabad, India | 174 | 58 | Inquiry |
BIOPHORE INDIA PHARMACEUTICALS PVT LTD | +91-4047474545 | New Delhi, India | 105 | 58 | Inquiry |
A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
SynZeal Research Pvt Ltd | +1 226-802-2078 | Gujarat, India | 6522 | 58 | Inquiry |
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