Clolar
clofarabine
CAS: 123318-82-1
Molecular Formula: C10H11ClFN5O3
Clolar - Names and Identifiers
| Name | clofarabine |
| Synonyms | CAFDA Clolar CLOFARABINE clofarabine 2-CHLORO-2'-ARABINOFLUORO-2'-DEOXYADENOSINE 2-chloro-9-(2-deoxy-2-fluoroarabinofuranosyl)adenine 2-chloro-9-(2-deoxy-2-fluoro-beta-d-arabinofuranosyl)adenine 2-Chloro-9-(2-Deoxy-2-Fluoro-β-D-Arabinofuranosyl)-9H-Purin-6-Amine 5-(6-amino-2-chloro-purin-9-yl)-4-fluoro-2-(hydroxymethyl)oxolan-3-ol 2-chloro-9-(2-deoxy-2-fluoro-beta-d-arabinofuranosyl)-9h-purin-6-amin 2-chloro-9-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)-9H-purin-6-amine (2R,4R,5R)-5-(6-amino-2-chloro-purin-9-yl)-4-fluoro-2-(hydroxymethyl)tetrahydrofuran-3-ol (2R,3R,4S,5S)-5-(4-amino-6-chloro-1H-benzo[d]imidazol-1-yl)-4-fluoro-2-(hydroxymethyl)-tetrahydrofuran-3-ol |
| CAS | 123318-82-1 |
| EINECS | 631-422-9 |
| InChI | InChI=1/C10H11ClFN5O3/c11-10-15-7(13)5-8(16-10)17(2-14-5)9-4(12)6(19)3(1-18)20-9/h2-4,6,9,18-19H,1H2,(H2,13,15,16)/t3-,4-,6?,9-/m1/s1 |
| InChIKey | INHHKRVRRUIAPA-KJHIFWANSA-N |
Clolar - Physico-chemical Properties
| Molecular Formula | C10H11ClFN5O3 |
| Molar Mass | 303.68 |
| Density | 1.4804 (estimate) |
| Melting Point | 228-2310C |
| Boling Point | 550.0±60.0 °C(Predicted) |
| Flash Point | 316.4°C |
| Solubility | DMSO: >10mg/mL |
| Vapor Presure | 3.19E-15mmHg at 25°C |
| Appearance | White powder |
| Color | white |
| Maximum wavelength(λmax) | ['263nm(EtOH)(lit.)'] |
| Merck | 14,2372 |
| pKa | 12.56±0.70(Predicted) |
| Storage Condition | 2-8°C |
| Refractive Index | 1.843 |
| MDL | MFCD00871077 |
| Physical and Chemical Properties | Properties: white crystalline powder; Dry loss |
| Use | For the treatment of acute lymphoblastic leukemia |
| In vitro study | Clofarabine is efficiently transported into the cell by two facilitating and equilibrating nucleoside transporters, hENT1 and hENT2, and a concentrating nucleoside transporter, hcnt253. Clofarabine is progressively phosphorylated by kinases in the cytosol to the nucleoside analog Clofarabine 5 ′-mono-, di-, and triphosphates and then enters the cell, Clofarabine triphosphate being the active form. Clofarabine 5 ′-mono-, di-, and triphosphates are not substrates for nucleoside transporters and must be enzymatically converted by 5 ′-nucleotidase to their dephosphorylated forms for transport out of the cell. Clofarabine triphosphate is a potent inhibitor of ribonucleotide reductase (IC50=65 nM), presumed to bind to allosteric sites via a regulatory subunit. Clofarabine acts directly on mitochondria to release cytochrome C, apoptosis-inducing factor (AIF), apoptotic protease-activating factor 1 (APAF1), and caspase 9 into the cytoplasm by altering the transmembrane potential. In a variety of leukemia and solid tumor cell lines, Clofarabine showed strong growth inhibition and cytotoxicity in vitro (IC50 value = 0.028-0.29 μm). Clofarabine was able to increase the activity of dCK in HL6 cells and also to increase the formation of ara-C mono-, di-and triphosphates in K562 cells. Clofarabine (10 μm) inhibited 4-peroxycyclophosphamide (4-HC)-induced repair with a peak of 5 μm intracellular concentration in chronic lymphocytic leukemia (CLL) lymphocytes. The combination of Clofarabine (10 μm) with 4-peroxycyclophosphamide (4-HC) produced more additional apoptotic cell death than either alone. The combination of Clofarabine (1 μm) and ara-C (10 μm) produced ara-CTP biochemical regulation and synergistically killed K562 cells. |
| In vivo study | In athymic nude mice or severe combined immunodeficient mice, Clofarabine administered intraperitoneally has significant activity against various subcutaneously transplanted human tumor grafts. |
Clolar - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | 25 - Toxic if swallowed |
| Safety Description | 45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| UN IDs | UN 2811 6.1 / PGIII |
| WGK Germany | 2 |
| RTECS | UD7473000 |
| HS Code | 29349990 |
| Hazard Class | 6.1 |
Clolar - Reference Information
| Introduction | Crorabine (Clofarabine) is a nucleotide analog that combines the advantages of fludarabine (Fludarabine) and cladribine (Cladribine). It inhibits both DNA polymerase and ribonucleic acid reductase. It is currently the only drug suitable for the treatment of childhood leukemia. Studies have proved that its treatment efficiency is very high, the total response rate of patients who did not respond to two conventional chemotherapy was 31%. Moreover, the patient has good tolerance and no unpredictable adverse reactions. It has potential broad-spectrum anti-tumor properties. |
| anticancer drug | clorabine, also known as clofarabine, is a new type of purine nucleoside anticancer drug, which is successfully developed by the top ten biopharmaceutical company in the United States (Genzyme Corporation,NASDAQ: GENZ), with the clofarabine product name, on December 28, 2004, the U.S. Food and Drug Administration (FDA) approved the clofarabine for the treatment of refractory or relapsed acute lymphoblastic leukemia in children through fast-track access. It is currently the only drug that can be specifically used for the treatment of childhood acute myelogenous leukemia (ALL); the treatment of leukemia is highly effective and well tolerated without unpredictable adverse reactions. It can be administered intravenously or orally. This product is the first new drug approved for the treatment of leukemia in children in more than a decade. |
| pharmacological effects | clorabine combines the advantages of fludarabine (Fludarabine) and cladribine (Cladribine), inhibiting DNA polymerase and ribonucleic acid reductase; It has shown strong anti-cancer activity on different cell lines and tumor models. Early studies have shown that the concentration of this product below micromoles can effectively inhibit the proliferation of human CNS tumors, lung cancer, kidney cancer, leukemia cells and melanoma cell lines. In vivo and in vitro experiments have shown that clolabine is effective Leukemia cells have apoptosis effects, which are achieved by down-regulating the BCL-X and MCL-1 of group BCL-2 proteins and the dephosphorization of AKT. Its inhibitory effect on human leukemia cell K-562 is stronger than cladribine and fludalebine, IC50 is 5nmol/L, while cladribine IC50 is 16nmol/L, fludalribine is 460nmol/L. Preclinical and concomitant drug trials have shown that clofarabine, other deoxynucleotide analogs and other types of anti-cancer drugs such as etoposide (etoposide) can increase the deoxycytidine in normal or abnormal human lymphocytes The activity of kinase can increase the anti-cancer efficacy. |
| usage and dosage | clolabine is an anti-tumor drug that affects tubulin. it is mainly used for clinical treatment: ① recurrent or refractory drug-resistant acute lymphoblastic leukemia. ②It is effective for elderly patients with acute myeloid leukemia and myelodysplastic syndrome (MDS) and can be combined with cytarabine. adult routine dose: ① relapsed and refractory acute lymphoblastic leukemia: patients (1~21 years old) who have received at least two previous treatment schemes (1~21 years old) 52 mg/m2 × 5 days daily, intravenous drip (more than 2 hours), after organ function recovery or return to baseline level, repeat once every 2~6 weeks. ② acute myeloid leukemia and MDS: 52 mg/m2 × 5 days per day, intravenous drip for 1 hour; Cytarabine was given 4 hours later, 1g/m2 × 5 days per day, intravenous drip for 2 hours, which has a positive effect on newly diagnosed elderly patients with acute myeloid leukemia and high-risk MDS. Children: Refractory recurrence of acute leaching, the dosage is the same as that of adults. Refractory and relapsed acute non-lymphocytic leukemia is treated with 52mg/m2 × 5 days daily, intravenous drip (greater than 2 hours), and repeated treatment every 2 to 6 weeks according to toxicity and patient response. |
| adverse reactions and precautions | common adverse reactions of clolabine are as follows: hematological system: leukopenia, neutropenia, thrombocytopenia and anemia can be seen. Digestive system: lack of appetite, nausea, vomiting, abdominal pain, abdominal secrecy; stomatitis, gingival hemorrhage, sore throat. Nervous system: fatigue, lethargy, headache, dizziness; anxiety, depression; irritability, excitement. Cardiovascular system: tachycardia, hypertension, hypotension, transient left ventricular systolic dysfunction, hypotension caused by any reason should be stopped; occasional pediatric patients have capillary leakage syndrome and systemic Inflammatory response syndrome (SIRS), which can be prevented by using hormones on the 1st to 3rd of treatment. In the medication, once the above syndrome occurs, the drug should be stopped immediately and the treatment should be supported in parallel. Once the condition is stable and organ function is restored, the drug can be restarted in a lower amount. liver toxicity: reversible liver injury, can be seen aspartate aminotransferase, alanine aminotransferase and bilirubin increased; hepatomegaly, yellow bile. respiratory system: visible respiratory distress, cough, pleural effusion, etc. genitourinary system: hematuria, secondary hyperuricemia, serum creatinine and creatine increased. Others: visible dermatitis, erythema; muscle pain, arthralgia; fever, infection, etc. [Precautions] Women of childbearing age should use contraception when using drugs, and breastfeeding should stop breastfeeding. Hypotension dehydration, liver and kidney insufficiency, bone marrow suppression secondary infection with caution. Crolabine may cause tumor lysis syndrome, which should be prevented. |
| biological activity | Clofarabine inhibit the enzyme activity of ribonucleotide reductase (RNR) (IC50=65 nM) and DNA polymerase. Clofarabine can induce autophagy and apoptosis. |
| Target | Value |
| Ribonucleotide reductase (Cell-free assay) | 65 nM |
| category | toxic substances |
| flammability hazard characteristics | flammability; fire scene decomposition of toxic nitrogen oxides; fluoride and chloride smoke |
| storage and transportation characteristics | warehouse low temperature ventilation and drying |
| fire extinguishing agent | water, carbon dioxide, dry powder, sand |
Last Update：2024-04-10 22:29:15
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