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Sibiromycin

Sibiromycin用途

西布罗霉素是一种天然产生的糖基化吡咯苯二氮卓类(PBD)。西布罗霉素也是一种有效的抗肿瘤抗生素,与鸟嘌呤NH2小沟中的DNA共价结合[1][2]。
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Sibiromycin名称

[ CAS 号 ]:
12684-33-2

[ 英文名 ]:
Sibiromycin

[英文别名 ]:

Sibiromycin生物活性

[ 描述 ]:

西布罗霉素是一种天然产生的糖基化吡咯苯二氮卓类(PBD)。西布罗霉素也是一种有效的抗肿瘤抗生素,与鸟嘌呤NH2小沟中的DNA共价结合[1][2]。

[ 相关类别 ]:

研究领域 >> 癌症
信号通路 >> 细胞周期/DNA损伤 >> DNA烷基化剂/交联剂

[体外研究]

吡咯苯二氮杂卓(PBD)是具有显著抗肿瘤活性的序列选择性DNA烷基化剂[1]。炭疽霉素、西伯利亚霉素和托霉素对DNA的烷基化具有序列特异性,结合偏好为5′-Pu-G-Pu>5′-Py-G-Pu>5′-Pu-G-Py>5′-Py-G-Py[1]。西布罗霉素对L1210(白血病)、ADJ/PC6(浆细胞瘤)和CH1(卵巢)细胞具有细胞毒性,IC50范围为0.000017~0.0029μM[1]。

[参考文献]

[1]. Gerratana B. Biosynthesis, synthesis, and biological activities of pyrrolobenzodiazepines. Med Res Rev. 2012;32(2):254-293.

[2]. Li W, et al. Biosynthesis of sibiromycin, a potent antitumor antibiotic. Appl Environ Microbiol. 2009;75(9):2869-2878.

Sibiromycin物理化学性质

[ 密度 ]:
1.41g/cm3

[ 沸点 ]:
755.7ºC at 760 mmHg

[ 分子式 ]:
C24H31N3O7

[ 分子量 ]:
473.51900

[ 闪点 ]:
410.8ºC

[ 精确质量 ]:
473.21600

[ PSA ]:
145.44000

[ LogP ]:
1.99250

[ 蒸汽压 ]:
5.32E-24mmHg at 25°C

[ 折射率 ]:
1.662

Sibiromycin毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UY8495000
CHEMICAL NAME :
5H-Pyrrolo(2,1-c)(1,4)benzodiazepin-5-one, 7-((4,6-dideoxy-3-(methyl-4-(methylamino)-beta- D-altropyranosyl)oxy))-10,11-dihydro-9,11-dihydroxy-8 -methyl-2-(1-propenyl )-
CAS REGISTRY NUMBER :
12684-33-2
LAST UPDATED :
199609
DATA ITEMS CITED :
13
MOLECULAR FORMULA :
C24-H31-N3-O7
MOLECULAR WEIGHT :
473.58
WISWESSER LINE NOTATION :
T C576 BVN IM HHJ E1U2 HQ KQ L1 MO- BT6OTJ CQ DQ D1 EM1 F1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
6 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
29 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
459 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
32 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
84 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
58 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD10 - Lethal Dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
5 ug/kg
TOXIC EFFECTS :
Cardiac - pericarditis Cardiac - other changes
TYPE OF TEST :
LD10 - Lethal Dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
12 ug/kg
TOXIC EFFECTS :
Blood - other changes
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
98 ug/kg/4D-I
TOXIC EFFECTS :
Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
22500 ng/kg/30D-I
TOXIC EFFECTS :
Cardiac - cardiomyopathy including infarction Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
30 ug/kg/15D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - other changes Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Related to Chronic Data - death

MUTATION DATA

TYPE OF TEST :
Mutation test systems - not otherwise specified
TEST SYSTEM :
Rodent - mouse Ascites tumor
DOSE/DURATION :
1 ug/L
REFERENCE :
NEOLA4 Neoplasma. (Karger-Libri, P.O. Box, CH-4009 Basel, Switzerland) V.4- 1957- Volume(issue)/page/year: 22,105,1975
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推荐生产厂家/供应商：

公司名：上海化源世纪贸易有限公司

区域：上海市普陀区

价格：

联系人：徐经理

产品详情：Sibiromycin

公司名：上海源溪生物科技有限公司

区域：上海市浦东新区

价格：
￥需询单/1g

联系人：赖经理

产品详情：Sibiromycin

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相关化合物

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标题：【Sibiromycin】Sibiromycin CAS号:12684-33-2【结构式 性质 活性】-化源网 地址：https://m.chemsrc.com/mip/cas/12684-33-2_336370.html