Linifanib (ABT-869)

Name: Linifanib (ABT-869)
SKU: A10025

目录号: A10025

VEGFR/PDGFR 抑制剂

Product Citations (1)

Linifanib (ABT-869) Chemical Structure

CAS NO. 796967-16-3

Linifanib (ABT-869)是一种结构新颖的有效RTK，VEGF和PDGF抑制剂，对人内皮细胞，PDGFR-β，KDR和CSF-1R的IC50分别为0.2、2、4和7 nM。

库存：现货

规格	价格	数量
5 mg	￥ 400.00
10 mg	￥ 700.00
50 mg	￥ 2,000.00
100 mg	￥ 3,500.00
10mM * 1mL in DMSO	￥ 890.00

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生物活性

Linifanib (ABT-869)是一种结构新颖的有效RTK，VEGF和PDGF抑制剂，对人内皮细胞，PDGFR-β，KDR和CSF-1R的IC50分别为0.2、2、4和7 nM。

Targets

Target	Value
VEGFR1/FLT1	IC50: 3nM
CSF-1R	IC50: 3nM
VEGFR2/KDR	IC50: 4nM
FLT3	IC50: 4nM
Kit	IC50: 14nM
PDGFRβ	IC50: 66nM
Tie-2	IC50: 170nM
VEGFR3/FLT4	IC50: 190nM
SGK	IC50: 940nM
RET	IC50: 1.9μM
PKA	IC50: 5.9μM
Cdc2	IC50: 9.8μM
FGFR	IC50: >12.5μM
Lyn	IC50: >20μM
LCK	IC50: 38μM
Src	IC50: >50μM
IGFR	IC50: >50μM
INSR	IC50: >50μM
EGFR	IC50: >50μM
Hck	IC50: >50μM
c-Met	IC50: >50μM
Fyn	IC50: >50μM
FGR	IC50: >50μM
Akt	IC50: >50μM

溶解度 *

In vitro (25°C)	DMSO	73 mg/mL (194.45 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	5%DMSO+40%PEG 300+5%Tween80+50%ddH2O	9 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

制备储备液

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	26.64 mL	133.19 mL	266.38 mL
0.5 mM	5.33 mL	26.64 mL	53.28 mL
1 mM	2.66 mL	13.32 mL	26.64 mL
5 mM	0.53 mL	2.66 mL	5.33 mL

*The above data is based on the productmolecular weight 375.4 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

化学数据

目录号	A10025
作用机制	Inhibitor (抑制剂)
M. Wt	375.4
Formula	C21H18FN5O
Purity	>99%
Storage	Store lyophilized at -20ºC, keep desiccated. In lyophilized form, the chemical is stable for 36 months. In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
CAS No.	796967-16-3
Synonyms	ABT869, ABT-869
SMILES	CC1=CC(=C(C=C1)F)NC(=O)NC2=CC=C(C=C2)C3=C4C(=CC=C3)NN=C4N

参考文献

1. Zhou J, Khng J, Jasinghe VJ, Bi C, Neo CH, Pan M, Poon LF, Xie Z, Yu H, Yeoh AE, Lu Y, Glaser KB, Albert DH, Davidsen SK, Chen CS: In vivo activity of ABT-869, a multi-target kinase inhibitor, against acute myeloid leukemia with wild-type FLT3 receptor. Leuk Res. 2008 Jul;32(7):1091-100. Epub 2007 Dec 26. [PubMed:18160102 ]

2. Guo J, Marcotte PA, McCall JO, Dai Y, Pease LJ, Michaelides MR, Davidsen SK, Glaser KB: Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors. Mol Cancer Ther. 2006 Apr;5(4):1007-13. [PubMed:16648572 ]

3. Albert DH, Tapang P, Magoc TJ, Pease LJ, Reuter DR, Wei RQ, Li J, Guo J, Bousquet PF, Ghoreishi-Haack NS, Wang B, Bukofzer GT, Wang YC, Stavropoulos JA, Hartandi K, Niquette AL, Soni N, Johnson EF, McCall JO, Bouska JJ, Luo Y, Donawho CK, Dai Y, Marcotte PA, Glaser KB, Michaelides MR, Davidsen SK: Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. Mol Cancer Ther. 2006 Apr;5(4):995-1006. [PubMed:16648571 ]