| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| G408475-1ml |
1ml |
现货  |
|
| 英文别名 | GTPL7939 | Benzamide, 2-[[5-chloro-2-[[3-methyl-1-(1-methylethyl)-1H-pyrazol-5-yl]amino]-4-pyridinyl]amino]-N-methoxy- |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | GSK2256098 |
| 生化机理 | GSK2256098 是一种强效、选择性、可逆、ATP 竞争性 FAK 激酶抑制剂，表观 Ki 为 0.4 nM。GSK2256098 可抑制癌细胞生长并诱导细胞凋亡。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 病灶粘附激酶 1 抑制剂 |
| 产品介绍 |
Information GSK2256098 GSK2256098 is a potent, selective, reversible, and ATP competitive FAK kinase inhibitor with apparent Ki of 0.4 nM. GSK2256098 inhibits cancer cell growth and induces apoptosis . GSK2256098 has been developed to inhibit FAK activity through targeting the phosphorylation site of FAK, tyrosine (Y) 397. After a 30-min incubation, GSK2256098 inhibits FAK activity or Y397 phosphorylation in cancer cell lines, OVCAR8 (ovary), U87MG (brain), and A549 (lung), at IC50 values of 15, 8.5 and 12 nM, respectively. In addition, the data suggests that cellular inhibition of FAK by GSK2256098 can occur as early as 30 min in cultured cells and lasts up to 12 hours in mouse tumor xenografts. GSK2256098 inhibition of FAK kinase activity can decrease Akt and ERK activity. PI3K/Akt and ERK signaling contributes to cell survival, implying a pharmacological value of GSK2256098 in attenuation of abnormal survival pathways in specific types of PDAC cells. GSK2256098 can promote apoptosis in L3.6P1 cells through caspase-9/PARP-related pathways. It attenuates abnormal growth and aberrant motility of PDAC cells in a FAK specific manner. GSK2256098 also inhibits growth, migration, and invasion and induces apoptosis in a subset of GBM cell lines. In vivo Pharmacokinetic (PK) studies in mice and rats with an intact blood brain barrier indicate that the penetration of GSK2256098 into the CNS is poor. However, it achieves concentrations in tumor of patients with GBM(glioblastoma) exceeding those associated with preclinical activity. GSK2256098 has an acceptable safety profile, has evidence of target engagement at doses at or below the MTD (maximum tolerated dose), and has clinical activity in patients with mesothelioma, particularly those with merlin loss. In the Ishikawa orthoptopic murine model, treatment with GSK2256098 results in lower tumor weights and fewer metastases than mice inoculated with Hec1A cells. Tumors treated with GSK2256098 have lower microvessel density (CD31), less cellular proliferation (Ki67), and higher apoptosis (TUNEL) rates in the Ishikawa model when compared to the Hec1a model. GSK2256098 may be therapeutically beneficial to patients with PTEN-mutant uterine cancer, and PTEN represents a potential predictive biomarker. cell lines：U937 cells Concentrations：0.1–10\xa0μM Incubation Time：48 or 72 h Powder Purity:≥99% |
| ALogP | 3.82 |
|---|---|
| hba_count | 4 |
| HBD Count | 3 |
| Rotatable Bond | 7 |
| Canonical SMILES | CONC(=O)C1=CC=CC=C1NC2=C(Cl)C=NC(=C2)NC3=CC(=N[N]3C(C)C)C |
|---|---|
| 分子量 | 414.89 |
| Reaxy-Rn | 20178710 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=20178710&ln= |
| DMSO(mg / mL) Max Solubility | 82 |
|---|---|
| DMSO(mM) Max Solubility | 197.64 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 20178710 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=20178710&ln= |
| Concentration(Compounding value) | 9-11（mmol/L） |
|---|---|
| Record the entire process by video | Conform |
首页
400-620-6333
