FALNIDAMOL
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- CAS号:
- 196612-93-8
- 英文名:
- BIBX 1382 DIHYDROCHLORIDE
- 英文别名:
- Falnid;CS-928;Falnidamol;Unii-0mu316797d;Falnidamol [inn];BIBX 1382 DIHYDROCHLORIDE;FALNIDAMOL; BIBX-1382; BIBX 1382;8-(3-Chloro-4-fluoroanilino)-2-((1-methyl-4-piperidyl)amino)pyrimido(5,4-D)pyrimidine;N4-(3-chloro-4-fluoro-phenyl)-N6-(1-methyl-4-piperidyl)pyrimido[5,4-d]pyrimidine-4,6-diamine;N8-(3-Chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidinyl)pyrimido[5,4-d]pyrimidine-2,8-diamine
- 中文名:
- FALNIDAMOL
- 中文别名:
- BIBX1382游离态;化合物BIBX 1382;化合物FALNIDAMOL;N4-(3-氯-4-氟-苯基)-N6-(1-甲基-4-哌啶)嘧啶并5,4-D嘧啶-4,6-二胺;N8-(3-氯-4-氟苯基)-N2-(1-甲基哌啶-4-基)嘧啶并[5,4-D]嘧啶-2,8-二胺;N8-(3-氯-4-氟苯基)-N2-(1-甲基-4-哌啶基)嘧啶并[5,4-D]嘧啶-2,8-二胺
- CBNumber:
- CB6842590
- 分子式:
- C18H19ClFN7
- 分子量:
- 387.84
- MOL File:
- 196612-93-8.mol
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FALNIDAMOL化学性质
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熔点:
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>217°C (dec.)
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沸点:
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552.0±60.0 °C(Predicted)
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密度:
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1.427
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储存条件:
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Keep in dark place,Inert atmosphere,2-8°C
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溶解度:
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DMSO (Slightly), Methanol (Slightly)
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酸度系数(pKa):
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8?+-.0.10(Predicted)
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形态:
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Solid
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颜色:
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Pale Yellow to Yellow
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FALNIDAMOL性质、用途与生产工艺
Falnidamol (BIBX 1382) 是一种具有口服活性的，选择性的 EGFR 酪氨酸激酶抑制剂，IC50 为3 nM。Falnidamol 对 ErbB2 (IC50=3.4 μM) 和其他一系列相关酪氨酸激酶 (IC50>10 μM) 的选择性 >1000倍。Falnidamol 是嘧啶-嘧啶化合物，具有抗癌活性。
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EGFR
3 nM (IC
50
)
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ErbB2
3.4 μM (IC
50
)
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Falnidamol (BIBX 1382) demonstrates antiproliferative activity in mitogenic assays performed with KB cells.
Falnidamol (BIBX 1382; p.o.; 10 mg/kg/day; 16 days) completely suppressed tumor growth of human A431 xenografts with respective a T/C value of 15% after 2 weeks of treatment.
Falnidamol (50 mg/kg/day for 2 weeks) results in dephosphorylation of the EGF receptor in A431 xenograft-bearing mice.
With Falnidamol (p.o.; 10 mg/kg/day; 16 days), the C
4h
is 2222 nM and the C
24h
is 244 nM.
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Animal Model:
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Five- to six-week-old athymic NMRI-nu/nu female mice (21-31 g) with A431, FaDu, or HN5 cells
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Dosage:
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10 mg/kg
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Administration:
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p.o.; daily; 16 days
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Result:
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Completely suppressed tumor growth of human A431 xenografts with respective T/C values of 15 and 6% after 2 weeks of treatment.
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Animal Model:
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Five- to six-week-old athymic NMRI-nu/nu female mice (21–31 g) with A431 cells
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Dosage:
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10 mg/kg (Pharmacokinetic Analysis)
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Administration:
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p.o.; daily; 16 days
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Result:
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The C
4h
is 2222 nM and the C
24h
is 244 nM.
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FALNIDAMOL
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-10322 | Falnidamol | | 1 mg | 350元 |
| 2024/04/30 | HY-10322 | FALNIDAMOL
Falnidamol | 196612-93-8 | 5mg | 820元 |
196612-93-8, FALNIDAMOL 相关搜索:
- 合成有机化合物配体
- 实验化学品
- C18H19ClFN72HCl
- C18H21Cl3FN7
- C18H19ClFN7
- N8-(3-氯-4-氟苯基)-N2-(1-甲基哌啶-4-基)嘧啶并[5,4-D]嘧啶-2,8-二胺
- 化合物FALNIDAMOL
- N4-(3-氯-4-氟-苯基)-N6-(1-甲基-4-哌啶)嘧啶并5,4-D嘧啶-4,6-二胺
- BIBX1382游离态
- 化合物BIBX 1382
- N8-(3-氯-4-氟苯基)-N2-(1-甲基-4-哌啶基)嘧啶并[5,4-D]嘧啶-2,8-二胺
- 196612-93-8
- CS-928
- BIBX 1382 dihydrochloride,N8-(3-Chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidinyl)-pyrimido[5,4-d]pyrimidine-2,8-diaminedihydrochloride
- FALNIDAMOL; BIBX-1382; BIBX 1382
- N8-(3-CHLORO-4-FLUOROPHENYL)-N2-(1-METHYL-4-PIPERIDINYL)-PYRIMIDO[5,4-D]PYRIMIDINE-2,8-DIAMINE DIHYDROCHLORIDE
- N4-(3-chloro-4-fluoro-phenyl)-N6-(1-methyl-4-piperidyl)pyrimido[5,4-d]pyrimidine-4,6-diamine
- N8-(3-Chloro-4-fluorophenyl)-N2-(1-methylpiperidin-4-yl)pyrimido[5,4-d]pyrimidine-2,8-diamine
- N8-(3-Chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidinyl)pyrimido[5,4-d]pyrimidine-2,8-diamine BIBX 1382
- N8-(3-Chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidinyl)pyrimido[5,4-d]pyrimidine-2,8-diamine
- Falnid
- N8-(3-Chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidinyl)-pyrimido[5,4-d]pyrimidine-2,8-diaminedihydrochloride
- Unii-0mu316797d
- Pyrimido(5,4-D)pyrimidine-2,8-diamine, N8-(3-chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidinyl)-
- Falnidamol [inn]
- Falnidamol
- 8-(3-Chloro-4-fluoroanilino)-2-((1-methyl-4-piperidyl)amino)pyrimido(5,4-D)pyrimidine
- BIBX 1382 DIHYDROCHLORIDE