TP-0903
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
TP-0903对AXL的IC50值为0.027 μM.
AXL和其它TAM家族成员在维持癌细胞的间充质表型中起着重要作用.间充质细胞增强侵袭与迁移特性,在应激环境下提高细胞存活率,以及增加对靶向治疗的耐受性.TP-0903是一种有效的抗癌药,靶向作用于AXL受体酪氨酸激酶.
体外:基于TP-0903在生化实验中显示出的效力,在基于细胞的实验中对TP-0903活性进行评价.胰腺癌细胞系PSN-1的细胞活力实验表明,TP-0903具有高度有效的活性.此外,在胰腺癌细胞中评估TP-0903阻断GAS6介导的AXL激活的能力.在各种浓度的TP-0903存在时,PSN-1细胞经血清饥饿后用GAS6刺激[1].
体内:在癌症的细胞模型与临床前动物模型中,TP-0903逆转间充质表型驱动的耐受性,从而恢复对Erlotinib的敏感性[2].
临床试验:截至目前,TP-0903仍处于临床前开发阶段.
参考文献:
[1] Mollard A, Warner SL, Call LT, Wade ML, Bearss JJ, Verma A, Sharma S, Vankayalapati H, Bearss DJ. Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors. ACS Med Chem Lett. 2011 Dec 8;2(12):907-912.
[2] ToleroPharmaceuticals, Inc–TP-0903. http://www.toleropharmaceuticals.com/TP-0903.html.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 516.06 |
Cas No. | 1341200-45-0 |
Formula | C24H30ClN7O2S |
Solubility | ≥25.8 mg/mL in DMSO with gentle warming; insoluble in EtOH; insoluble in H2O |
Chemical Name | 2-((5-chloro-2-((4-((4-methylpiperazin-1-yl)methyl)phenyl)amino)pyrimidin-4-yl)amino)-N,N-dimethylbenzenesulfonamide |
SDF | Download SDF |
Canonical SMILES | CN(S(C1=CC=CC=C1NC2=NC(NC3=CC=C(CN4CCN(CC4)C)C=C3)=NC=C2Cl)(=O)=O)C |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Cell experiment:[1] | |
Cell lines |
Pancreatic cancer cell line PSN-1 |
Reaction Conditions |
6 nM TP-0903 (IC50) |
Applications |
TP-0903 showed extremely potent activity in cell viability assays with an IC50 of 6 nM against PSN-1 cells. When PSN-1 cells was stimulated by GAS6, TP-0903 was able to dose-dependently decrease phospho-AKT and phospho-AXL levels with an EC50 of 305 and 222 nM, respectively. |
Animal experiment:[2] | |
Animal models |
An HCT116 mouse xenograft model and a KRAS-mutant colorectal cancer (CRC) patient-derived xenograft (PDX) mouse model |
Dosage form |
40 mg/kg Administered orally |
Applications |
TP-0903 exhibited 69 and 44% tumor growth inhibition in an HCT116 mouse xenograft model and a KRAS-mutant PDX mouse model, respectively, when administered at a dose of 40 mg/kg. |
Note |
The technical data provided above is for reference only. |
References: 1. Mollard A, Warner SL, Call LT, et al. Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors. ACS Medicinal Chemistry Letters, 2011, 2(12): 907-912. 2. Mangelson R, Peterson P, Foulks JM, et al. Abstract 2197: The AXL kinase inhibitor, TP-0903, demonstrates efficacy in preclinical models of colorectal cancer independent of KRAS mutation status. Cancer Research, 2019, 79(13 Suppl): Abstract nr 2197. |
质量控制和MSDS
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