4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)-
cytosine arabinoside hydrochloride
CAS: 69-74-9
Molecular Formula: C9H14ClN3O5
4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)- - Names and Identifiers
4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)- - Physico-chemical Properties
| Molecular Formula | C9H14ClN3O5 |
| Molar Mass | 279.68 |
| Melting Point | 197-198°C(lit.) |
| Boling Point | 545.7°C at 760 mmHg |
| Flash Point | 283.8°C |
| Vapor Presure | 3.5E-14mmHg at 25°C |
| Appearance | White crystal |
| Color | White to off-white |
| Storage Condition | 2-8°C |
| Stability | Stable. Combustible. Incompatible with strong oxidizing agents. |
| Sensitive | Easily absorbing moisture |
| MDL | MFCD00012839 |
| Physical and Chemical Properties | This product is white fine needle-like crystal or crystalline powder. Odorless, easily soluble in water, slightly soluble in methanol and ethanol, slightly soluble in ether. mp189-195 C (decomposition). The specific rotation should be 127 °- 133 °(10 mg/ml). Acid and alkaline aqueous solution hydrolysis to produce uridine Arabinoside, the most stable pH value of 6.9. |
| Use | For acute leukemia, also for head and neck squamous cell carcinoma, external for viral keratitis and epidemic conjunctivitis |
4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)- - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R36 - Irritating to the eyes R43 - May cause sensitization by skin contact R63 - Possible risk of harm to the unborn child |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36/37 - Wear suitable protective clothing and gloves. |
| WGK Germany | 3 |
| RTECS | HA5500000 |
| HS Code | 29389090 |
| Hazard Class | IRRITANT |
| Toxicity | LD50 oral in rat: > 3200mg/kg |
4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)- - Reference
| Reference Show more | 1. [IF=3.785] Jun Wu et al."Estrogen regulates forkhead transcription factor 2 to promote apoptosis of human ovarian granulosa-like tumor cells."J Steroid Biochem. 2019 Nov;194:105418 |
4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)- - Nature
Open Data Verified Data
- This product is white fine needle-like crystal or crystalline powder. This product is very soluble in water, slightly soluble in ethanol, almost insoluble in ether. Melting point 189~195 °c (decomposition). The specific rotation should be 127. In 133. (10 mg/mL).
- This synthetic nucleoside differs from a normal nucleoside in that the sugar moiety is arabinose rather than ribose or deoxyribose. Sequential conversion by deoxycytidine kinase, dCMP kinase and nucleoside diphosphate kinase to the triphosphate derivative vidarofuran cytidine triphosphate (ara-CTP), the latter being an active metabolite. ara-CTP interferes with the synthesis of DNA by blocking the DNA polymerase and binds into the DNA, causing further defects in chain termination. This effect is manifested in the S phase. It has inhibitory effect on a variety of tumors.
Last Update：2024-01-02 23:10:35
4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)- - Preparation Method
Open Data Verified Data
- 5 '-cytidine monophosphate was used as a raw material.
- calcium gluconate was used as raw material.
Last Update：2022-01-01 11:12:42
4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)- - Standard
Authoritative Data Verified Data
This product is 1-b-d-arabinofuranosyl-4-amino-2 (1H )-pyrimidinone hydrochloride. The content of C9H13N305 • HCl should be between 98.0% and 102.0% based on the dry product.
Last Update：2024-01-02 23:10:35
4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)- - Trait
Authoritative Data Verified Data
- This product is white or off-white fine needle-like crystal or crystalline powder.
- This product is easily soluble in water, slightly soluble in ethanol, and almost insoluble in ether.
melting point
The melting point of this product (General rule 0612) is 189~195°C, melting and decomposition.
specific rotation
take this product, precision weighing, adding water to dissolve and quantitatively dilute to prepare a solution containing 10 mg per lml, and determine according to law (General rule 0621), calculate according to the dry product, the specific rotation was 127 ° to 133 °.
Last Update：2022-01-01 15:05:19
4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)- - Use
Open Data Verified Data
- Anti-tumor drug.
- specification (1)50mg; (2) lOOmg.
Last Update：2022-01-01 11:12:42
4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)- - Differential diagnosis
Authoritative Data Verified Data
- take an appropriate amount of this product, add hydrochloric acid solution (9-1000) to dissolve and dilute to prepare a solution containing about 10ug per lml, and measure it by UV-Vis spectrophotometry (General rule 0401), there is a maximum absorption at a wavelength of 280nm and a minimum absorption at a wavelength of 241NM.
- in the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 361).
- the aqueous solution of this product was chloride identification (1) of the reaction (General 0301).
Last Update：2022-01-01 15:05:20
4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)- - Safety
Open Data Verified Data
- (1) should be used with caution for patients with abnormal liver function;(2) during the treatment, the blood picture and white blood cell count should be checked frequently;(3) the liquid medicine should be freshly prepared and stored in the refrigerator for 1 week, give up if it becomes turbid.
- attention should be strictly checked during medication.
- light-shielded, sealed, and stored in a cold place.
Last Update：2022-01-01 11:12:43
4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)- - Exam
Authoritative Data Verified Data
clarity and color of solution
take 1.2g of this product and add 10ml of water to dissolve, the solution should be clear and colorless; If it is turbid, it should not be more concentrated compared with No. 1 turbidity standard solution (General rule 0902 first method); If it is colored, comparison with yellow No. 2 Standard Colorimetric solution (General rule 0901 first method), not deeper.
chlorine content
take this product about 0.30g, precision weighing, add water 50ml and dilute nitric acid 2ml dissolved, according to the potential titration method (General rule 0701 ), with silver nitrate titration solution (0.lmol/L) titration. Each 1 ml of silver nitrate titration solution (0.1 mol /L) corresponds to 3.545mg of chlorine (C1). The chlorine content shall be 12.4%-12.9% based on the dry product.
Related substances
- take an appropriate amount of this product, precisely weigh, add water to dissolve and quantitatively dilute to make a solution containing 5mg per lml, as a test solution; Take an appropriate amount of cytarabine hydrochloride reference, precisely weigh, water was added to dissolve and quantitatively diluted to prepare a solution containing 5% per 1 ml as a control solution. Silica gel bonded with eighteen alkyl silanes as fillers (0512 X 4.6mm mm, 5um) as determined by high performance liquid chromatography (General 7.0); (Take 0.02mol/L sodium dihydrogen phosphate solution and 0.02mol/L disodium hydrogen phosphate solution equal volume mixing, with 0.1 mol/L sodium hydroxide solution or 0.1 mol/L phosphoric acid solution to adjust the pH value to 7.0)-methanol (98:2) as mobile phase A, phosphate buffer (pH 7.0)-methanol (70:30) as mobile Phase B, the gradient elution was carried out as follows; The detection wavelength was 254mn. In addition, appropriate amounts of cytarabine hydrochloride and uridine were dissolved in water and diluted to prepare solutions containing 5mg and 20ul of each 1 ml as the system applicable solution. 20UL was injected into the liquid chromatograph, and the chromatographic system was adjusted. The resolution of cytarabine peak and uridine peak should meet the requirements. 2 Ou1 of the test solution and the reference solution were respectively injected into the liquid chromatograph, and the chromatograms were recorded. The relative retention times of uracil peak, uridine peak and uridine peak to cytarabine peak are about 0.55,1- 14 and 1.62, respectively, the correction factors of uridine peak and uridine arabinoside peak for cytarabine peak were 2.9, 1.72 and 1.54, respectively. The correction factors for chromatographic peaks with relative retention times of about 0.38 and 0.43 for cytarabine peak were both 1.72, the correction factors of other impurity peaks were calculated as 1.1.
- if there are impurity peaks in the chromatogram of the test solution, the following formula shall be calculated: uracil and uridine shall not exceed 0.1%; Uridine arabinoside shall not exceed 0.3%; Other individual impurities shall not exceed 0.1%; the sum of all impurities shall not exceed 0.3%.
residual solvent
take about 0.2g of this product, weigh it accurately, place it in the top empty bottle, add 5ml of water accurately to dissolve, Seal, shake, and use it as a test solution; take the appropriate amount of methanol and ethanol, precisely weigh, dilute with water to make a solution containing about 120ug of methanol and 200ug of ethanol in each lml respectively. Take 5ml of the precise amount, place it in the top empty bottle, and seal it, as a reference solution; Take the appropriate amount of methyl ethyl ketone and isopropyl alcohol separately, put in the same measuring flask, dilute with water to make the solution containing about lOug in each lml, take 5ml, put in the top empty bottle, Seal, as a system suitability solution. According to the determination method of residual solvent (General 0861 second method), using polyethylene glycol (or polar similar) as the stationary liquid capillary column; The initial temperature is 60 degrees C, maintain 6 minutes, increase the temperature to 100°C at a rate of 8°C per minute for 20 minutes; The inlet temperature was 200°C; The detector temperature was 230°C; The headspace bottle equilibrium temperature was 80°C and the equilibrium time was 30 minutes. The system applicable solution was sampled by Headspace injection, and the chromatographic system was adjusted. The resolution of methyl ethyl ketone peak and isopropanol peak should meet the requirements. The test solution and the reference solution were injected by Headspace, and the chromatograms were recorded. According to the external standard method, the residual amount of methanol and ethanol should be calculated by Peak area, and the requirements should be met.
loss on drying
take this product, put it in a phosphorus pentoxide dryer, and dry it under reduced pressure to constant weight. The weight loss shall not exceed 0.5% (General rule 0831).
ignition residue
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.5%.
Heavy metals
The residue left under the item of taking the ignition residue shall not contain more than 10 parts per million of heavy metal when examined by law (General Principles 0821, Law II).
Last Update：2022-01-01 15:05:21
4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)- - Content determination
Authoritative Data Verified Data
measured by high performance liquid chromatography (General 0512).
chromatographic conditions and system suitability test
silica gel (4.6mm X 250mm,5um) bonded with eighteen alkyl silane as filler; the mobile phase was phosphate buffer (0.0106mol/L sodium dihydrogen phosphate solution and 0.0104mol/L disodium hydrogen phosphate solution were mixed in equal volume)-methanol (95:5); The detection wavelength was 254nm. Take appropriate amounts of cytarabine hydrochloride and uridine arabinoside in the same measuring flask, add water to dissolve and dilute to make each 1 ml containing 0.lmg solution, take 10ul injection of human liquid chromatography, adjust the chromatographic system, the separation of cytarabine peak and uracil arabinoside peak should be greater than 2.5.
assay
take about 50mg of this product, precision weighing, water dissolution and quantitative dilution made from each lml containing about 0. The lmg solution was used as the test solution, and the l0ul was injected into the human liquid chromatograph for precise measurement, and the chromatogram was recorded. The reference sample of cytarabine hydrochloride was taken and determined by the same method. According to the external standard method to calculate the peak area, that is.
Last Update：2022-01-01 15:05:22
4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)- - Category
Authoritative Data Verified Data
antineoplastic agents.
Last Update：2022-01-01 15:05:22
4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)- - Storage
Authoritative Data Verified Data
shading, sealing, storage in cold place.
Last Update：2022-01-01 15:05:22
4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)- - Cytarabine hydrochloride for injection
Authoritative Data Verified Data
This product is a sterile lyophilized product of cytarabine hydrochloride. Cytarabine hydrochloride (C3H13N305 • HCl) should be included in 93.0% to 107.0% of the labeled amount, based on the average loading.
trait
This product is white loose lumps or powder.
identification
The same results were obtained according to the tests (1), (2) and (4) for the identification of cytarabine hydrochloride.
examination
- the acidity of this product is dissolved in water and diluted to prepare a solution containing cytarabine hydrochloride 10 mg per lml, which is measured according to law (General rule 0631). The pH value should be 4.0~6.0.
- clarity of solution take this product, add water to be dissolved and diluted to make a solution containing 20mg per 1 ml, and the solution should be clear; If it is turbid, compared with No. 1 turbidity standard solution (General Principles 0902 first method), shall not be more concentrated.
- Related substances the contents of this product are dissolved in water and diluted quantitatively to prepare a solution containing 5mg cytarabine hydrochloride per 1 ml, which is used as a test solution for determination according to the method under the item of related substances of cytarabine hydrochloride, the requirements shall be met.
- the moisture content of this product shall not exceed 0832 as determined by the method for determination of moisture (General rule 3.0%, first method 1).
- abnormal toxicity: take this product, add sodium chloride injection to dissolve and dilute it to prepare a solution containing 30mg cytarabine hydrochloride per 1 ml, check according to law (General rule 1141), and give it by intravenous injection, the requirements shall be met.
- bacterial endotoxin this product, according to the law inspection (General 1143), each 1 mg of cytarabine hydrochloride containing endotoxin amount should be less than 0.050EU.
- others should comply with the relevant provisions under injection (General 0102).
Content determination
take 5 bottles of this product, weigh the contents accurately respectively, add appropriate amount of water to dissolve the contents in each container, transfer the contents to the same appropriate measuring bottle, dilute with water to the scale, shake well, take an appropriate amount of precision, quantitative dilution with water to make each lml containing cytarabine hydrochloride 0. The 1 mg solution was obtained as a test solution by measurement according to the method described under cytarabine hydrochloride.
category
Same as cytarabine hydrochloride.
specification
(l)50mg (2)100mg (3)0.3g (4)0.5g
storage
light shielding, closed, stored in cold place.
Last Update：2022-01-01 15:05:23
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Product Name: Cytarabine Hydrochloride Request for quotation
CAS: 69-74-9
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
CAS: 69-74-9
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: 1-Beta-D-Arabinofuranosylcytosine Hydrochloride Visit Supplier Webpage Request for quotationCAS: 69-74-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
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