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| Linifanib (ABT-869)VEGFR/PDGFR inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | Linifanib is a multitargeted inhibitor of receptor tyrosine kinase with IC50 value of 3 nM, 3 nM, 4 nM, 4 nM and 14 nM for VEGFR1/FLT1, CSF-1R, VEGFR2/KDR, FLT3 and KIT, respectively. | |||||
| Targets | VEGFR1/FLT1 | CSF-1R | VEGFR2/KDR | FLT3 | KIT | |
| IC50 | 3 nM | 3 nM | 4 nM | 4 nM | 14 nM | |
| Cell experiment [1]: | |
Cell lines | Ba/F3 FLT3 ITD mutant and WT cells |
Preparation method | The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
Reacting condition | 0.1 nM ~ 10 μM; 24 hrs |
Applications | Linifanib was more effective at inhibiting cell growth in ITD mutant cells with the IC50 value of 0.55 nM. In addition, treatment with 10 nM of Linifanib induced apoptosis in ITD mutant cells, but showed no observable effect on WT cells. |
| Animal experiment [1]: | |
Animal models | NOD/SCID mice with ITD mutant cells |
Dosage form | 0.2 mL/20 g; p.o.; q.d. |
Applications | In NOD/SCID mice with ITD mutant cells, Linifanib decreased leukemia progression. On day 7, untreated mice exhibited rapid progression of ITD mutant cells, whilst mice treated with Linifanib showed no detectable disease. In addition, Linifanib significantly prolonged survival duration of Ba/F3 FLT3 ITD-injected mice. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Jenny E. Hernandez-Davies, Joan P. Zape, Elliot M. Landaw, et al. The Multitargeted Receptor Tyrosine Kinase Inhibitor Linifanib (ABT-869) Induces Apoptosis through an Akt and Glycogen Synthase Kinase 3β–Dependent Pathway. Mol. Cancer Ther., 2011, 10(6):949-59. | |
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| Cas No. | 796967-16-3 | SDF | Download SDF |
| Chemical Name | 1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methylphenyl)urea | ||
| Canonical SMILES | CC1=CC(=C(C=C1)F)NC(=O)NC2=CC=C(C=C2)C3=C4C(=CC=C3)NN=C4N | ||
| Formula | C21H18FN5O | M.Wt | 375.41 |
| Solubility | ≥18.75mg/mL in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Linifanib (ABT-869) is an effective ATP-competitive tyrosine kinase inhibitor against the platelet-derived growth factor (PDGF) receptor and the vascular endothelial growth factor receptor (VEGFR) families, including constitutively active FMS-like receptor tyrosine kinase 3 (FLT3) [1][2]. It is of IC50 values of 0.55 nmol/L and 6 μmol/L to the cell growth in Ba/F3 FLT3 ITD mutant cells and in Ba/F3 FLT3 WT cells, respectively [1].
FLT3 is important in controlling the proliferation and differentiation of hematopoietic cells. Patients with acute myeloid leukemia (AML) showed activating mutations in FLT3. These mutations caused abnormal cell proliferation [1].
Linifanib at a concentration of 10 nmol/L induced apoptosis in internal tandem duplication (ITD) mutant cells, but showed no effect in WT cells. Treatment with linifanib did not differentiate WT cells from FLT3 mutant cells with mutation at D835V, in inhibiting proliferation or reducing cell viability. In Ba/F3 FLT3 ITD cell lines, linifanib at a concentration of 10 nmol/L, effectively inhibited the phosphorylation of FLT3. 10 nmol/L linifanib reduced the phosphorylation of Akt at Ser473 [1].
Daily orally treatment with linifanib by gavage in NOD/SCID mice with ITD mutant cell decreased the leukemia progression rate compared with the control. On day 7, ITD mutant cells showed rapid progression in control mice, whereas linifanib-treated mice showed no detectable disease. In addition, daily linifanib-treated mice with ITD mutant cells showed significantly longer (P < 0.01)="" survival="" duration="" than="" control="" mice="" with="" itd="" mutant="" cells="" only="" [1].="">
References: [1]. Jenny E. Hernandez-Davies, Joan P. Zape, Elliot M. Landaw, et al. The Multitargeted Receptor Tyrosine Kinase Inhibitor Linifanib (ABT-869) Induces Apoptosis through an Akt and Glycogen Synthase Kinase 3β–Dependent Pathway. Mol. Cancer Ther., 2011, 10(6):949-59.[2]. Joyce E. Ohm, Michael R. Shurin, Clemens Esche, et al. Effect of Vascular Endothelial Growth Factor and FLT3 Ligand on Dendritic Cell Generation In Vivo. Journal of Immunology, 1999, 163:3260-3268.
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（第1张图和第2张图是经旋转后方向恰好相反的两张图，上矢状窦等静脉也显示了）
女患，70岁，大专毕业，我院退休药师。7-8年前患脑梗（具体不详）。记忆力差5-6年，近记忆为著，几次做饭后忘记关火，将炉具的台板（玻璃的）烧裂。近5-6年来，病人每年住院彻底检查治疗1次（主要是使用活血化瘀及营养脑细胞药）。平素，病人双耳听力略差，睡眠欠佳、便秘、尿频，偶从卧位坐起时视蒙。既往有时血压略高，未降压治疗。本次为“通血管”再来住院。查体：血压：140/80mmHg,双耳听力略差，近记忆力差，但智力（MMSE：26分)正常，颅神经未见异常，四肢肌力、感觉未见异常，植物神经未查，双掌颌反射（+），双下肢病理反射均阴性。血常规：淋巴细胞比率略高，余均正常；尿常规、心电图、癌胚抗原均正常；凝血四项：除凝血酶时间略长外均正常；生化全项：除总胆固醇略高外均正常；超声心动图：老年瓣退行性改变，左室舒张功能减退，房膜瘤可能。彩超：双侧颈动脉粥样硬化形成。头MRA:右大脑中动脉及其分支未显示。
问题：1MRI怎么会这样逍遥？病人无肢体瘫，生活自理如常人。
2为明确头MRA:右大脑中动脉及其分支未显示的病因和程度，除做DSA外，还需做什么？
3如不做DSA，给他订类药、阿斯匹林及活血化瘀的中药可不可以？
教。
版主laocao留言:
患者的年龄，病史，症状，辅助检查传上来，便于进一步讨论，谢谢！
