| Size | Price | Stock | Qty |
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| 10g |
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| 25g |
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| 50g |
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| 100g |
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Cytarabine hydrochloride (MK-8242; SCH-900242; AC-1075; CHX-3311; Arabitin), the hydrochloride salt of cytarabine, is a pyrimidine nucleoside analog and antimetabolic anticancer agent with a modified sugar moiety. It inhibits the synthesis of DNA.
| Targets |
DNA synthesis ( IC50 = 16 nM )
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|---|---|
| ln Vitro |
Cytarabine undergoes phosphorylation into a triphosphate form (Ara-CTP) through the action of deoxycytidine kinase (dCK), which inhibits the function of DNA and RNA polymerases and competes with dCTP for incorporation into DNA. With an IC50 of 16 nM, cytarabine exhibits greater growth inhibitory activity against wild-type CCRF-CEM cells than it does against other acute myelogenous leukemia (AML) cells[1]. It appears that cytarabine causes apoptosis in rat sympathetic neurons at 10 μM; the highest toxicity is at 100 μM, which kills over 80% of the neurons in 84 hours through the activation of caspase-3 and the release of mitochondrial cytochrome-c. The toxicity can be delayed by bax deletion and attenuated by p53 knockdown[2].
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| ln Vivo |
Cytarabine (250 mg/kg) also results in placental growth retardation and increases the apoptosis of placental trophoblastic cells in the placental labyrinth zone of pregnant Slc:Wistar rats. This process begins three hours after the treatment, peaks at six hours, and returns to control levels at forty-eight hours. Notably, p53 protein and p53 transcriptional target genes, including p21, cyclin G1, fas, and caspase-3 activity, are significantly increased[3]. The use of higher dosages of Cytarabine does not appear to contribute to its antileukaemic effectiveness in humans. Cytarabine is highly effective against acute leukaemias, which cause the chCytarabineteristic G1/S blockage and synchronization, and increases the survival time for leukaemic Brown Norway rats in a weak dose-related fashion[4].
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| Animal Protocol |
Intraperitoneal (i.p.) injection of 250 mg/kg Cytarabine is administered to pregnant rats on Day 13 of gestation (GD13). Congenital defects and growth retardation are frequently found in perinatal fetuses under the circumstances of this experiment, but the incidence of fetal death is not noticeably elevated. Following treatment, six dams are killed by heart puncture under ether anesthesia at 1, 3, 6, 9, 12, 24, and 48 hours. The placentas are then collected. In GD13, six pregnant rats serve as controls. They receive an intraperitoneal injection of the same volume of PBS and are killed concurrently with the groups treated with cytarabine. Three of the six dams collected at each time point are utilized for histopathological examinations, and the remaining three are used for RT-PCR (reverse transcription-polymerase chain reaction) analysis.
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| References |
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| Molecular Formula |
C9H14CLN3O5
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|---|---|
| Molecular Weight |
279.6776
|
| Exact Mass |
279.06
|
| Elemental Analysis |
C, 38.65; H, 5.05; Cl, 12.68; N, 15.02; O, 28.60
|
| CAS # |
69-74-9
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| Related CAS # |
147-94-4 (free); 69-74-9 (HCl)
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| Appearance |
White solid powder
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| SMILES |
C1=CN(C(=O)N=C1N)[C@H]2[C@H]([C@@H]([C@H](O2)CO)O)O.Cl
|
| InChi Key |
KCURWTAZOZXKSJ-JBMRGDGGSA-N
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| InChi Code |
InChI=1S/C9H13N3O5.ClH/c10-5-1-2-12(9(16)11-5)8-7(15)6(14)4(3-13)17-8;/h1-2,4,6-8,13-15H,3H2,(H2,10,11,16);1H/t4-,6-,7+,8-;/m1./s1
|
| Chemical Name |
4-amino-1-[(2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one;hydrochloride
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| Synonyms |
MK 8242; MK8242; MK-8242; SCH-900242; SCH 900242; SCH900242; aracytidine; cytarabine hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 50~55 mg/mL (178.8~196.7 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.94 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.94 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5755 mL | 17.8776 mL | 35.7551 mL | |
| 5 mM | 0.7151 mL | 3.5755 mL | 7.1510 mL | |
| 10 mM | 0.3576 mL | 1.7878 mL | 3.5755 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01661881 | Active Recruiting |
Drug: Rituximab Drug: Cytarabine |
Mantle Cell Lymphoma | Dana-Farber Cancer Institute | August 16, 2012 | Phase 2 |
| NCT04330820 | Active Recruiting |
Drug: Venetoclax Oral Tablet | Relapsed Adult AML Refractory AML |
Technische Universität Dresden | April 6, 2020 | Phase 1 Phase 2 |
| NCT03069352 | Active Recruiting |
Drug: Cytarabine Drug: Venetoclax |
Acute Myeloid Leukemia (AML) |
AbbVie | May 23, 2017 | Phase 3 |
| NCT02658487 | Active Recruiting |
Drug: Cytarabine Drug: Vosaroxin |
Myeloid Sarcoma Acute Myeloid Leukemia |
Vanderbilt-Ingram Cancer Center |
March 2016 | Phase 2 |
| NCT04115631 | Active Recruiting |
Drug: Cytarabine Drug: Acalabrutinib |
Mantle Cell Lymphoma Liver Lymphoma |
ECOG-ACRIN Cancer Research Group |
December 13, 2019 | Phase 2 |
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