MGCD-265
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.
MGCD-265是多靶点和ATP竞争性抑制剂,对c-Met和 VEGFR1、2、3的IC50值分别为1 nM、3 nM、3 nM和4 nM[1]
在非小细胞肺癌异种移植瘤模型(包含一个含有TKI耐药性EGFR突变T790M的模型)中,MGCD265与紫杉醇(paclitaxel)、多西他赛(docetaxel)或厄洛替尼(erlotinib)联合使用,与单独使用MGCD265相比,组合使用诱导产生更大的肿瘤应答,与多西他赛共同使用产生抗血管生成的作用[2]。
在多种晚期实体瘤,包括非小细胞肺癌中,对MGCD265的效果进行研究,包括作为单一疗法或与多西他赛或厄洛替尼的组合使用。在I期临床研究阶段,针对晚期实体恶性肿瘤患者,每日口服MGCD265从每日24 mg/m2到235 mg/m2,每天两次不间断的治疗,直至病情有所改善[3]。在I期临床阶段,采用标准3 + 3剂量递增给药,96 mg/m2的MGCD265每天一次直到162 mg/m2,与100或150 mg埃罗替尼共同使用以确定其安全性,共有45例患者参与。在一个单独的I期剂量递增研究中,MGCD265与多西他赛结合使用,对34例晚期实体瘤先用50 mg/m2再用75 mg/m2静脉注射,每3周一次,其中包括9 个NSCLC患者。MGCD265微粉化制剂的MTD是72 mg/m2 bid,多西他赛的是每3周75 mg/m2,但还没有形成新的制剂[4,5]。
参考文献:
[1] Bonfils C. et al. AACR 2012 Annual Meeting, 2012. Abstract 1790.
[2]. Besterman JM, Fournel M, Dupont I, et al. Potent preclinical antitumor activity of MGCD265, an oral Met/VEGFR kinase inhibitor in phase II clinical development, in combination with taxanes or erlotinib. J Clin Oncol 2010;28:abstr e13595.
[3]. Kollmannsberger CK, Hurwitz H, Vlahovic G, et al. Phase I study of daily administration of MGCD265 to patients with advanced malignancies (Study 265-101). J Clin Oncol 2009;27:abstr e14525.
[4]. Kollmannsberger CK, Hurwitz H, Cleary JM, et al. MGCD265, a multitargeted oral tyrosine kinase receptor inhibitor of Met and VEGFR: Dose-escalation phase I study (abstr 3039). 2012 ASCO Annual Meeting Chicago, IL. J Clin Oncol 2012;30:abstr 3039.
[5]. Drouin MA, Kollmannsberger CK, Uronis HE, et al. Daily administration of MGCD265 to patients with solid tumors in a dose-escalation phase I study (study 265-101). J Clin Oncol 2010;28:abstr 3106.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 517.6 |
Cas No. | 875337-44-3 |
Formula | C26H20FN5O2S2 |
Solubility | ≥25.9 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | N-[[3-fluoro-4-[2-(1-methylimidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxyphenyl]carbamothioyl]-2-phenylacetamide |
SDF | Download SDF |
Canonical SMILES | CN1C=C(N=C1)C2=CC3=NC=CC(=C3S2)OC4=C(C=C(C=C4)NC(=S)NC(=O)CC5=CC=CC=C5)F |
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。 |
Description | MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1, 2, 3 with IC50 values of 1 nM, 3 nM, 3 nM and 4 nM, respectively. | |||||
Targets | c-Met | VEGFR1 | VEGFR2 | VEGFR3 | ||
IC50 | 1 nM | 3 nM | 3 nM | 4 nM |