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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]。

Sibiromycin名称

[ CAS 号 ]:
12684-33-2

[ 英文名 ]:
Sibiromycin

[英文别名 ]:

Sibiromycin
C24H31N3O7
Sybiromycin

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