|(Z)-3-(((4-(N-甲基-2-(4-甲基哌嗪-1-基)乙酰氨基)苯基)氨基)(苯基)亚甲基)-2-氧代吲哚啉-6-羧酸甲酯乙磺酸盐|CsnPharm

CAS No.: 656247-18-6

乙磺酸尼达尼布 Catalog No. CSN16881

Synonyms: BIBF 1120 esylate;Nintedanib Esylate;BIBF 1120 (esylate)

BIBF 1120 esylate is a multiple receptor tyrosine kinases inhibitors for VEGFR1/2/3, PDGFRα/β and FGFR1/2/3 with IC50 of 34 nM/13 nM/13 nM, 59 nM/65 nM and 69 nM/37 nM/108 nM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 VEGFR3

IC50:13nM VEGFR2

IC50:13nM VEGFR1

IC50:34nM
描述VEGF/VEGFR (vascular endothelial growth factor/vascular endothelial growth factor receptor) pathway plays a key role in tumor angiogenesis by promotion of vascular and lymphatic endothelial, as well as survival, and invasion, thus resulting in neovascularization, tumor growth and metastasis. In addition, blockade of additional proangiogenic receptor tyrosine kinases, including PDGFR and FGFR, may improve long-term clinical outcomes. BIBF 1120 Esylate is the esylate form of BIBF 1120. BIBF 1120 is a multi-RTKs inhibitor with IC50 values of 13nM, 13nM , 16nM , 26nM , 34nM , 37nM , 59nM , 65nM , 69nM , 108nM for VEGFR2, VEGFR3, LCK, FLT3, VEGFR1, FGFR2, PDGFRα, PDGFRβ, FGFR1, FGFR3 (measured by enzymatic assays), less potent to Src, Lyn and FGFR4 with IC50 values of 156nM , 195nM and 610nM, respectively. Treatment with BIBF 1120 resulted in cell proliferation and apoptosis (EC50<10nM) in HUVECs, HSMECs, as well as the downstream p-MAPK and p-AKT (0.1-1μM). Daily oral treatment with BIBF 1120 at dose of 100mg/kg for 5 days reduced vessel density by 76% in FaDu xenografts, as well as markedly reduced both Meca 32–positive and PDGFRβ-positive cells predominantly in the intratumoral compartment. Once daily oral administration of BIBF 1120 at dose of 50mg/kg and 100mg/kg inhibited tumor growth both in a model of human head and neck small cell carcinoma (FaDu cells) and in a human renal cancer model (Caki-1 cells).

动物研究

剂量

Mice: 25 mg/kg - 100 mg/kg^[2] (p.o.)
Rat: 8.3 mg/kg– 41.5 mg/kg^[3] (p.o.)

给药途径

p.o.

动物药代数据

Animal	Mice^[4]	Rats^[4]	Monkeys^[4]
Dose	50 mg/kg	50 mg/kg (p.o.) 2 mg/kg (i.v.)	40 mg/kg (cynomolgus, p.o.) 5 mg/kg (cynomolgus, i.v.)
Administration	p.o.	p.o. or i.v.	p.o. or i.v.
MRT	5.19 h	3.25 h (i.v.)	3.82 h (i.v.)
F		11.9% (p.o.)	13.2% (p.o.)
T_1/2	5.15 h	3.95 h (i.v.)	5.95 h (i.v.)
AUC	2720 ng·h/ml	375 ng·h/ml (p.o.) 181 ng·h/ml (i.v.)	2390 ng·h/ml (p.o.) 2260 ng·h/ml (i.v.)
CL		202 ml/min/kg (i.v.)	37.5 ml/min/kg (i.v.)
C_max	547 ng/ml	105 ng/ml (p.o.) 124 ng/ml (i.v.)	175 ng/ml (p.o.) 1300 ng/ml (i.v.)
Protein bound (%)			92.9% (p.o.)
Protein binding (free drug %)	97.2	98.5% (p.o.)
Vss		41.2 L/kg (i.v.)	8.64 L/kg (i.v.)

参考文献

[1] Roth GJ, Heckel A, et al. Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). J Med Chem. 2009 Jul 23;52(14):4466-80.
[2] Hilberg F, Roth GJ, et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008 Jun 15;68(12):4774-82.
[3] Nintedanib
[4] Nintedanib

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.5390 mL
- 7.6952 mL
- 15.3904 mL
- 5 mM
- 0.3078 mL
- 1.5390 mL
- 3.0781 mL
- 10 mM
- 0.1539 mL
- 0.7695 mL
- 1.5390 mL

技术信息

CAS号

656247-18-6

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C33H39N5O7S

运输

蓝冰

分子量

649.76

别名

BIBF 1120 esylate;Nintedanib Esylate;BIBF 1120 (esylate);Nintedanib;BIBF1120;BIBF 1120 BIBF-1120;Intedanib;Brand name OFEV. Vargatef;乙磺酸尼达尼布

溶解度

DMSO	50.0 mg/mL (77.0 mM)
Water	10.0 mg/mL (15.4 mM) warming

动物实验配方

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靶点	Description	IC50
VEGFR3		IC50:13nM
VEGFR2		IC50:13nM
VEGFR1		IC50:34nM

乙磺酸尼达尼布 Catalog No. CSN16881

靶点选择性

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