“betaine hydrochloride”的搜索结果
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Src 抑制剂
Dasatinib hydrochloride是一种有效的Abl/Src双重抑制剂,IC50分别<1 nM/0.8 nM。还可以抑制c-Kit(WT/c-Kit(D816V),IC50为79 nM/37 nM。有效,选择性Raf激酶抑制剂能够抑制野生型B-Raf,B-RafV600E和c -Raf的IC50值分别为3.2、0.8和5.0 nM。
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EGFR, HER2 and HER4 inhibitor
Epertinib hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib shows potent antitumor activity.
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MET/Axl 抑制剂
Glesatinib hydrochloride是MET和Axl受体酪氨酸激酶途径的抑制剂,当改变时,它们会驱动肿瘤的生长。
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VEGFR 抑制剂
Vandetanib hydrochloride是一种有效的VEGFR2抑制剂,IC50为40 nM。
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EGFR 抑制剂
Gefitinib hydrochloride是一种EGFR抑制剂,可通过靶细胞中的表皮生长因子受体(EGFR)中断信号传导。因此,它仅在EGFR突变和过度活跃的癌症中有效。
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EGFR/T790M inhibitor
HS-10296 hydrochloride is an orally available and third-Generation inhibitor of epidermal growth factor receptor (EGFR)-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.
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VEGFR1/2/3/PDGFRβ/Kit/RET/Raf-1 inhibitor
Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
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c-Met/NPM-ALK 抑制剂
Crizotinib hydrochloride是c-Met激酶和NPM-ALK的抑制剂。
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- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
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VEGFr2 抑制剂
TG 100801 HCl是TG 100572(HY-10184)的前药,TG 100572是一种多靶点激酶抑制剂,可抑制选择性生长因子受体酪氨酸激酶和Src家族激酶,IC50值为2/7/2/1/0.5 nM或VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse分别。
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VEGFR2/Src kinase 抑制剂
TG 100572 HCl是一种多靶点激酶抑制剂,可抑制选择性生长因子受体酪氨酸激酶和Src家族激酶,分别对VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse的IC50值为2/7/2/1/0.5 nM。
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EGFR 抑制剂
Icotinib hydrochloride是一种有效的特异性表皮生长因子受体(EGFR)酪氨酸激酶抑制剂(TKI),IC(50)为5 nM,包括EGFR(L858R),EGFR(L861Q),EGFR(T790M)和EGFR的突变体(T790M,L858R)。
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VEGFR 抑制剂
ZM 323881 hydrochloride是一种有效且选择性的人血管内皮生长因子受体2(VEGFR2/KDR)激酶活性抑制剂。
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EGFR inhibitor
Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM.
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Src 抑制剂
Tirbanibulin dihydrochloride是首个靶向Src肽底物位点的临床Src抑制剂(拟肽类),在癌细胞系中GI50为9-60 nM。
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MET 抑制剂
LY2801653 dihydrochloride是一种有效的,口服可生物利用的c-MET激酶小分子抑制剂(Ki = 2 nM)。
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ALK 抑制剂
LDK378 (Ceritinib) dihydrochloride是有效的抗ALK抑制剂,IC50为0.2 nM,对IGF-1R和InsR的选择性分别为40倍和35倍。
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SFK 抑制剂
A-419259是Src家族激酶(SFK)的抑制剂(IC50 = 0.1-0.3 uM)。
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VEGFR 抑制剂
ZM 306416 hydrochloride是一种VEGF受体酪氨酸激酶抑制剂,可抑制KDR(IC50 = 100 nM)和Flt(IC50 = 2 uM)酪氨酸激酶。
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EGFR 抑制剂
Erlotinib hydrochloride是一种可逆的酪氨酸激酶抑制剂,作用于表皮生长因子受体(EGFR)。
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- Yuta Yamamoto, .et al. Quantitative determination of erlotinib in human serum using competitive enzyme-linked immunosorbent assay, J Pharm Anal, 2018, Apr; 8(2): 119-123 PMID: 29736298
- Aikawa S, .et al. Proliferation of mouse endometrial stromal cells in culture is highly sensitive to lysophosphatidic acid signaling, Biochem Biophys Res Commun, 2017, Feb 26;484(1):202-208 PMID: 28073697
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VEGFR/PDGFR/FGFR 抑制剂
Pazopanib HCl (GW786034)是VEGFR-1,VEGFR-2,VEGFR-3,PDGFR-a/β和c-kit的有效且选择性的多靶点酪氨酸激酶抑制剂,可阻止肿瘤生长并抑制血管生成。
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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Hideharu Yamada, .et al. lncRNA HAR1B has potential to be a predictive marker for pazopanib therapy in patients with sarcoma, Oncol Lett, 2021, Jun;21(6):455 PMID: 33907565
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298