GNF-7
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.
GNF-7 对Colo205、SW620和TrkC-Ba/F3细胞的IC50分别为0.005、0.001、和0.008 μM。
GNF-7是T315I- Bcr-Abl的二型抑制剂[1]。BCR-ABL是组成性激活的酪氨酸激酶,是与慢性髓细胞性白血病(CML)和人类急性淋巴细胞白血病相关的致癌基因。
体外实验:GNF-7对一些人癌细胞具有优良的生长抑制活性。GNF-7在Colo205、SW620和TrkC-Ba/F3细胞系的IC50分别为0.005、0.001和0.008 μM。 GNF-7对正常的细胞系HEK293T的影响不大[1]。7.5 mg/kg QD或15 mg/kg QD处理24小时后,与对照组小鼠相比,GNF-7显著降低了疾病负担,延长了总体生存率[2]。
活体实验:在急性骨髓性白血病和淋巴母细胞白血病模型中,GNF-7强效选择性抑制了NRAS依赖性的细胞[2]。在T315I-BCR-ABL-Ba/F3细胞系生物发光异种移植小鼠模型中,口服给药GNF-710 10或20 mg/kg对T315I-BCR-ABL有显著功效,并且没有明显的毒性[1]。
参考文献:
Choi H G, Ren P, Adrian F, et al. A type-II kinase inhibitor capable of inhibiting the T315I “gatekeeper” mutant of Bcr-Abl[J]. Journal of medicinal chemistry, 2010, 53(15): 5439-5448.
Nonami A, Sattler M, Weisberg E, et al. Identification of novel therapeutic targets in acute leukemias with NRAS mutations using a pharmacologic approach[J]. Blood, 2015, 125(20): 3133-3143.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 547.53 |
Cas No. | 839706-07-9 |
Formula | C28H24F3N7O2 |
Solubility | insoluble in EtOH; insoluble in H2O; ≥5.48 mg/mL in DMSO |
Chemical Name | (Z)-N-(4-methyl-3-(1-methyl-7-((6-methylpyridin-3-yl)amino)-2-oxo-1,2-dihydropyrimido[4,5-d]pyrimidin-3(4H)-yl)phenyl)-3-(trifluoromethyl)benzimidic acid |
SDF | Download SDF |
Canonical SMILES | CC1=C(N(C2=O)CC(C(N2C)=N3)=CN=C3NC4=CN=C(C=C4)C)C=C(/N=C(O)/C5=CC(C(F)(F)F)=CC=C5)C=C1 |
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。 |
质量控制和MSDS
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