CAS 147-94-4 MFCD00066487-Cytosine-beta-D-arabinofuranoside 阿糖胞苷 TAO{mole}

Cytosine-beta-D-arabinofuranoside 阿糖胞苷

CAS 147-94-4 MFCD00066487

化学结构图

SMILES: Nc1ccn([C@@H]2O[C@H](CO)[C@@H](O)[C@@H]2O)c(=O)n1

化学属性

Mol. Formula	C9H13N3O5
Mol. Weight	243.22
Density	1.89
Melting Point	214 °C
Solubility	H2O: 50 mg/mL, clear, colorless
Appearance	crystalline
Boiling Point	386.09 °C at 760 mmHg

别名和识别编码

Chemical Name	Cytosine-beta-D-arabinofuranoside
CAS Number	147-94-4
Alfabeta Name	CYTARABINE
MDL Number	MFCD00066487
Synonym	Cytarabine {LY} Cytarabine Cytarabine Hydrochloride Cytonal Cytosar Cytosar U Cytosar-U Cytosine Arabinoside beta Ara C beta-Ara C {} {LY} Cytarabine {} {} {LY} Cytarabine {} {} {} {LY} Cytarabine {} {} {} {} {LY} Cytarabine {} {} {} {} {} {LY} Cytarabine {} {} {} {} {} {} {LY} Cytarabine {} {} {} {} {} {} {} {LY} Cytarabine {} {} {} {} {} {} {} {} {LY} Cytarabine {} {} {} {} {} {} {} {} {} {LY} Cytarabine {} {} {} {} {} {} {} {} {} {} {LY} Cytarabine {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {LY} Cytarabine {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} { {} {} {} {} {} {} {} {} {} {} {} {} {LY} Cytarabine {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {LY} Cytarabine {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {LY} Cytarabine {} {} {} {} {} {} {} {} {}
EC Number	205-705-9
Beilstein Registry Number	89175
PubChem Substance ID	6253
Reaxys-RN	89175
Merck Number	2784
Chemical Name Translation	阿糖胞苷
Wiswesser Line Notation	T6NVNJ DZ A- BT5OTJ CQ DQ E1Q
LabNetwork Molecule ID	LN00238525
Canonical SMILES	O=C1N=C(C=CN1[C@H]2[C@@H](O)[C@H](O)[C@@H](CO)O2)N
InChI	InChI=1S/C9H13N3O5/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)/t4-,6-,7+,8-/m1/s1

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产品应用

Ara-C 插入DNA，靠和拓扑异构酶I（topoisomerase I）形成络合物抑制DNA复制，导致DNA裂解。不能抑制RNA合成。抗白血病物质，用于各类急性白血病。

安全信息

Warnings IRRITANT

Signal word

GHS Symbol

WGK Germany3

Safety Statements

S36/37 Wear suitable protective clothing and gloves 穿戴适当的防护服和手套；

Risk Statements

R36/37/38 Irritating to eyes, respiratory system and skin 对眼睛、呼吸系统和皮肤有刺激性
R63 Possible risk of harm to the unborn child 可能危害未出生婴儿
R43 May cause sensitisation by skin contact 皮肤接触会产生过敏反应

Precautionary statements

P203
P261 Avoid breathing dust/fume/gas/mist/vapours/spray. 避免吸入粉尘/烟/气体/烟雾/蒸汽/喷雾。
P264+P265
P272 Contaminated work clothing should not be allowed out of the workplace. 污染的工作服不得带出工作场所。
P280 Wear protective gloves/protective clothing/eye protection/face protection. 戴防护手套/防护服/眼睛的保护物/面部保护物。
P281 Use personal protective equipment as required. 使用所需的个人防护装备。
P302+P352
P305+P351+P338
P318
P321 Specific treatment (see … on this label). 具体治疗（见本标签上的）。
P333+P313
P333+P317
P337+P317
P362+P364
P405 Store locked up. 上锁保管。
P501 Dispose of contents/container to..… 处理内容物/容器.....

Hazard statements

H317 May cause an allergic skin reaction 可能导致皮肤过敏
H319 Causes serious eye irritation 严重刺激眼睛
H340 May cause genetic defects 可能导致遗传性缺陷
H341 Suspected of causing genetic defects 怀疑导致遗传性缺陷
H360 May damage fertility or the unborn child 可能对生育能力或未出生婴儿造成伤害
H361 Suspected of damaging fertility or the unborn child 怀疑对生育能力或未出生婴儿造成伤害

Personal Protective Equipment Eyeshields, Faceshields, full-face particle respirator type N100 (US), Gloves, respirator cartridge type N100 (US), type P1 (EN143) respirator filter, type P3 (EN 143) respirator cartridges

RTECSHA5425000

Hazard Codes Xn

Storage condition 2-8°C {LY} 2-8°C {} {LY} 2-8°C {} {} {LY} 2-8°C {} {} {} {LY} 2-8°C {} {} {} {} {LY} 2-8°C {} {} {} {} {} {LY} 2-8°C {} {} {} {} {} {} {LY} 2-8°C {} {} {} {} {} {} {} {LY} 2-8°C {} {} {} {} {} {} {} {} {LY} 2-8°C {} {} {} {} {} {} {} {} {} {LY} 2-8°C {} {} {} {} {} {} {} {} {} {} {LY} 2-8°C {} {} {} {} {} {} {} {} {} {} {} {LY} 2-8°C {} {} {} {} {} {} {} {} {} {} {} {} {LY} 2-8°C {} {} {} {} {} {} {} {} {} {} {} {} {} {LY} 2-8°C {} {} {} {} {} {} {} {} {} {} {} {} {} {} {LY} 2-8°C {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {LY} 2-8°C {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {LY} 2-8°C {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {LY} 2-8°C {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {LY} 2-8°C {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {LY} 2-8°C {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} { {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {} {

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Intraperitoneal
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 2500 mg/kg/7W-I
TOXIC EFFECTS :
   Tumorigenic - equivocal tumorigenic agent by RTECS criteria
   Blood - lymphoma, including Hodgkin's disease
   Skin and Appendages - tumors
REFERENCE :
   CANCAR Cancer (Philadelphia).  (Lippincott/Harper, Journal Fulfillment
   Dept., 2350 Virginia Ave., Hagerstown, MD 21740)  V.1-    1948-
   Volume(issue)/page/year: 40,1935,1977

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Intraperitoneal
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 4836 mg/kg/26W-I
TOXIC EFFECTS :
   Tumorigenic - equivocal tumorigenic agent by RTECS criteria
   Lungs, Thorax, or Respiration - tumors
   Blood - lymphoma, including Hodgkin's disease
REFERENCE :
   CANCAR Cancer (Philadelphia).  (Lippincott/Harper, Journal Fulfillment
   Dept., 2350 Virginia Ave., Hagerstown, MD 21740)  V.1-    1948-
   Volume(issue)/page/year: 40,1935,1977

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intraperitoneal
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : >5 gm/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   NIIRDN Drugs in Japan (Ethical Drugs).  (Yakugyo Jiho Co., Ltd., Tokyo,
   Japan)  Volume(issue)/page/year: 6,321,1982

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Human - woman
DOSE/DURATION           : 720 mg/kg/3D-I
TOXIC EFFECTS :
   Brain and Coverings - other degenerative changes
REFERENCE :
   NEURAI Neurology.  (Modern Medicine Pub., Inc., 1 E. First St., Duluth, MN
   55802)  V.1-    1951-  Volume(issue)/page/year: 35,1475,1985

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Human - man
DOSE/DURATION           : 649 mg/kg/4D-I
TOXIC EFFECTS :
   Peripheral Nerve and Sensation - fasciculations
REFERENCE :
   DICPBB Drug Intelligence and Clinical Pharmacy.  (POB 42435, Cincinnati, OH
   45242)  V.3-    1969-  Volume(issue)/page/year: 21,177,1987

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : >5 gm/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   NIIRDN Drugs in Japan (Ethical Drugs).  (Yakugyo Jiho Co., Ltd., Tokyo,
   Japan)  Volume(issue)/page/year: 6,321,1982

TYPE OF TEST            :

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Human - child
DOSE/DURATION           : 33200 ug/kg/240D-I
TOXIC EFFECTS :
   Behavioral - somnolence (gene

TYPE OF TEST

TYPE OF TEST            : DNA inhibition
TEST SYSTEM             : Rodent - mouse Lung
DOSE/DURATION           : 136 nmol/L
REFERENCE :
   CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut
   Sts., Philadelphia, PA 19106)  V.1-    1941-  Volume(issue)/page/year:
   36,95,1976

TYPE OF TEST            : Cytogenetic analysis
ROUTE OF EXPOSURE       : Subcutaneous
TEST SYSTEM             : Rodent - mouse
DOSE/DURATION           : 315 mg/kg
REFERENCE :
   MUREAV Mutation Research.  (Elsevier Science Pub. B.V., POB 211, 1000 AE
   Amsterdam, Netherlands) V.1-    1964-  Volume(issue)/page/year: 58,67,1978

TYPE OF TEST            : Morphological transformation
TEST SYSTEM             : Rodent - mouse Embryo
DOSE/DURATION           : 1 umol/L/24H
REFERENCE :
   CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut
   Sts., Philadelphia, PA 19106)  V.1-    1941-

{hazard_c

TYPE OF TEST            : Mutation in microorganisms
TEST SYSTEM             : Microorganism - not otherwise specified
DOSE/DURATION           : 50 mg/L
REFERENCE :
   MUREAV Mutation Research.  (Elsevier Science Pub. B.V., POB 211, 1000 AE
   Amsterdam,

TYPE OF TEST            : Specific locus test

TYPE OF TEST            : Cytogenetic analysis
TEST SYSTEM             : Rodent - hamster Ovary
DOSE/DURATION           : 1 mg/L
REFERENCE :
   ENMUDM Environmental Mutagenesis.  (New York, NY)  V.1-9, 1979-87.  For
   publisher information, see EMMUEG.  Volume(issue)/page/year: 2,455,1980

TYPE OF TEST            : DNA inhibition
TEST SYSTEM             : Human Lymphocyte
DOSE/DURATION           : 50 mg/L
REFERENCE :
   BBRCA9 Biochemical and Biophysical Research Communications.  (Academic
   Press, Inc., 1 E. First St., Duluth, MN 55802)  V.1-    1959-
   Volume(issue)/page/year: 60,96,1974

TYPE OF TEST            : Sperm M

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Intraperitoneal
SPECIES OBSERVED

TYPE OF TEST            : TDLo - Lowest publ

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Unreported
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 50 mg/kg
SEX/DURATION            : female 12 day(s) after conception
TOXIC EFFECTS :
   Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured
   before birth)
REFERENCE :
   TJADAB Teratology, The International Journal of Abnormal Development. (Alan
   R. Liss, Inc., 41 E. 11th St., New York, NY 10003)  V.1-    1968-
   Volume(issue)/page/year: 19,43A,1979

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EX

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Intraperitoneal
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 50 mg/kg
SEX/DURATION            : female 12 day(s) after conception
TOXIC EFFECTS :
   Reproductive - Specific Developmental Abnormalities - craniofacial
   (including nose and tongue)
   Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
   TJADAB Teratology, The International Journal of Abnormal Development. (Alan
   R. Liss, Inc., 41 E. 11th St., New York, NY 10003)  V.1-    1968-
   Volume(issue)/page/year: 4,7,1971

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Parenteral
SPECIES OBSERVED        : Rodent - mouse
DOSE                    : 60 mg/kg
SEX/DURATION            : female 13-14 day(s) after conception
TOXIC EFFECTS :
   Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight
   gain)
REFERENCE :
   TJADAB Teratology, The International Journal of Abnormal Development. (Alan
   R. Liss, Inc., 41 E. 11th St., N

其他信息

{Chemicalbo
图谱信息:阿糖胞苷(147-94-4)质谱(MS) 阿糖胞苷(147-94-4)红外图谱(IR1) 阿糖胞苷(147-94-4)核磁图( 1 HNMR) 阿糖胞苷(147-94-4)红外图谱(IR2) 阿糖胞苷(147-94-4)核磁图( 13 CNMR)
下游产品:盐酸阿糖胞苷
溶于水，部分溶于甲醇，几乎不溶于乙醚，本品以D-阿拉伯糖或5′-胞嘧啶核苷酸为原料制得。常用其盐酸盐。
用法用量:成人用法： 1，急性白血病诱导治疗：常与其他化疗药联用，每次1～3mg/kg，静滴，q 12h，连用5～7日。间隔1～2周重复。 2，中、大减量疗法：常用于难治性或复发性急性白血病或急性白血病缓解后的强化治疗。中剂量指每次500～1000mg/m2，静滴1～3小时，q12h，2～6 日为一个疗程。大剂量指每次1000～3000mg/m2，用法同中剂量方案。由于阿糖胞苷的不良反应随剂量增大而加重，大剂量反而影响其疗效，故现多偏向用中剂量方案。 3，皮下注射：每次10mg/m2，q12h，14～21日为一个疗程。如不缓解而病人情况允许，可于2～3周后重复一个疗程。此方案可用于原始细胞增多的骨髓增生异常综合征、低增生性白血病、老年急性非淋巴细胞白血病等。 4，鞘内注射：脑膜白血病，每次25～75mg，加地塞米松5mg，以NS溶解后鞘内注射，每周1～2次，用至脑脊液检查正常。预防性用药则每4～8周1次。儿童用法：急性白血病诱导治疗，100mg/(m2·d)，连用5～7日。
刺激数据:皮肤-人 45 毫克/3周中度; 眼睛-人 105 毫克/7天
药动学:本药口服吸收量少，又极易在胃肠道黏膜及肝脏的胞嘧啶脱氨酶作用下脱氨而失去活性，故不宜口服。可经静脉、皮下、肌内或鞘内注射而吸收。静脉注射后能广泛分布于体液、组织及细胞内。静脉滴注后约有中等量的药物透入血—脑脊液屏障，脑脊液中药物浓度约为血药浓度的40%。本药在肝、肾等组织内代谢，被胞嘧啶脱氨酶迅速脱氨而形成无活性的尿嘧啶阿拉伯糖苷，在脑脊液内，由于该脱氨酶含量较低，故其脱氨作用较缓慢。静脉给药时，半衰期α相为10～15分钟，β相为2～2.5小时；鞘内给药时，半衰期可延至11小时。在24小时内，所给药物中，约 10%以药物原形、90%以尿嘧啶阿糖胞苷形式经肾脏排泄。
给药说明:1.使用阿糖胞苷给药时，应适当增加患者的液体摄入量，使尿液保持碱性，必要时可合用别嘌醇，以防止血尿酸增高及尿酸性肾病。 2.快速静脉注射引起的恶心、呕吐反应虽较严重，但对骨髓的抑制较轻，患者一般能耐受。 3.静脉滴注液应稀释至0.5mg/ml。 4.配制好的注射液可在4℃(冰箱中)保存7日，室温下仅能保存24小时。 5.鞘内注射用药，稀释液中应不含防腐剂。 6.采用中剂量或大剂量的阿糖胞苷治疗时，部分患者可能发生严重的胃肠道及神经系统不良反应，如胃肠道溃疡、胃肠囊样积气、坏死性结肠炎、周围神经病变、大脑或小脑功能障碍如性格改变、肌张力减退、癫、嗜睡、昏迷、定向力障碍、眼球震颤、构音障碍、步态不稳;尚可发生出血性结膜炎、皮疹、脱发、脱皮、严重心肌病等。 7.如出现各种严重不良反应时，应立即停药，并立即采取各种有效措施治疗。部分患者给予肾上腺皮质激素，可能减轻中剂量或大剂量阿糖胞苷引起的不良反应。
灭火剂:干粉,泡沫,沙土
毒性分级:中毒
不良反应:消化系统：常见食欲减退、恶心、呕吐、腹泻、胃炎、口腔炎和胃肠道溃疡等。部分病人出现肝功能异常、高胆红素及氨基转移酶升高。大剂量时可出现明显肝功能异常及黄疸，可引起肝脏中央静脉及肝小叶静脉闭塞，导致黄疸、肝大、腹水及肝性脑病。血液系统：骨髓抑制随剂量增大而加重，表现为白细胞、血小板减少。局部反应：静滴处疼痛和血栓性静脉炎大多在停药后消退，也有出现瘙痒和皮疹等反应;局部眼科用药时，常引起暂时性烧灼、痒等轻度刺激感，也可出现流泪、异物感、结膜充血、表浅点状角膜炎、疼痛、怕光等反应。中枢神经系统：偶尔发生不适、乏力、震颤、头晕、幻觉、精神症状和意识模糊，其发生与剂量有关，通常停药后消退，也有出现头痛和脑病的报道，后者常难以与原发病相识别，多发生于肝、肾功能不全者。逾量表现：每日摄入的阿糖胞苷剂量超过20mg/kg，可引起骨髓抑制;一旦
急性毒性:口服-大鼠 LD5