(-)-Irofulven
(-)-Irofulven用途
(-)-Irofulven(MGI 114),一种伊卢定S类似物,是一种DNA烷基化剂。(-)-Irofulven抑制DNA复制,诱导肿瘤细胞凋亡,并具有强大的抗肿瘤活性[1][2]。
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(-)-Irofulven名称
[ CAS 号 ]:
158440-71-2
[ 英文名 ]:
(-)-Irofulven
[英文别名 ]:
- HMAF
- [14C]-Irofulven
- 6-hydroxymethylacylfulvene
- (-)-irofulven
- Acylfulvene,6-(hydroxymethyl)
- MGI 114
(-)-Irofulven生物活性
[ 描述 ]:
(-)-Irofulven(MGI 114),一种伊卢定S类似物,是一种DNA烷基化剂。(-)-Irofulven抑制DNA复制,诱导肿瘤细胞凋亡,并具有强大的抗肿瘤活性[1][2]。
[ 相关类别 ]:
[体外研究]
(-)-Irofulven(2.8μM；1小时)诱导p53依赖性细胞周期阻滞[1]。(-)-Irofulven(0.8μM、0.9μM和2.8μM；1小时)诱导CHK2激活与细胞中的p53状态有关[1]。(-)-Irofulven抑制DNA复制并诱导染色体畸变(断裂和放射状)[1]。细胞周期分析[1]细胞系：A2780、CAOV3和HCT116细胞浓度：2.8μM孵育时间：1小时结果：p53野生型细胞主要阻滞于G1/S期,而p53突变或p53缺失细胞则阻滞于S期和G2/M期。Western Blot分析[1]细胞系：A2780、CAOV3和HCT116细胞浓度：0.8μM、0.9μM和2.8μM培养时间：1小时结果：诱导细胞内CHK2激酶的Thr 68磷酸化。
[体内研究]
(-)-Irofulven(第1-5天和第8-12天为7 mg/kg；i.p.)可显著提高荷瘤小鼠的中位生存率[2]。动物模型：雄性和雌性无胸腺BALB/c小鼠(nu/nu基因型,6周龄或以上)注射人类多形性胶质母细胞瘤[2]。剂量：7mg/kg给药：腹腔注射；在第1-5天和第8-12天,结果：对所有肿瘤细胞株都有效。
[参考文献]
(-)-Irofulven物理化学性质
[ 密度 ]:
1.28g/cm3
[ 沸点 ]:
501ºC at 760 mmHg
[ 分子式 ]:
C15H18O3
[ 分子量 ]:
246.30200
[ 闪点 ]:
270.9ºC
[ 精确质量 ]:
246.12600
[ PSA ]:
57.53000
[ LogP ]:
1.66560
[ 蒸汽压 ]:
3.9E-12mmHg at 25°C
[ 折射率 ]:
1.617
[ 储存条件 ]:
-20°C
(-)-Irofulven毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- WH0204487
- CHEMICAL NAME :
- Spiro(cyclopropane-1,5'(5H)-inden)-7'(6'H)-one, 6'-hydroxy-3'-(hydroxymethyl)-2',4',6'- trimethyl-, (R)-
- CAS REGISTRY NUMBER :
- 158440-71-2
- LAST UPDATED :
- 199712
- DATA ITEMS CITED :
- 4
- MOLECULAR FORMULA :
- C15-H18-O3
- MOLECULAR WEIGHT :
- 246.33
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- LD - Lethal dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- >6610 ug/kg
- TOXIC EFFECTS :
- Cardiac - other changes Blood - changes in bone marrow (not otherwise specified) Blood - changes in other cell count (unspecified)
- REFERENCE :
- FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 36(1, Pt 2),180,1997
- TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 2 mg/kg
- TOXIC EFFECTS :
- Blood - thrombocytopenia Blood - changes in bone marrow (not otherwise specified) Blood - changes in other cell count (unspecified)
- REFERENCE :
- FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 36(1, Pt 2),180,1997 ** OTHER MULTIPLE DOSE TOXICITY DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 20339 ug/kg/5D-I
- TOXIC EFFECTS :
- Cardiac - other changes Blood - changes in bone marrow (not otherwise specified) Blood - changes in other cell count (unspecified)
- REFERENCE :
- FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 36(1, Pt 2),180,1997
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 3 mg/kg/5D-I
- TOXIC EFFECTS :
- Blood - thrombocytopenia Blood - changes in bone marrow (not otherwise specified) Blood - changes in other cell count (unspecified)
- REFERENCE :
- FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 36(1, Pt 2),180,1997
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