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CAS:1374640-70-6|CO-1686(AVL-301)
作者:德尔塔 日期:2022-03-15
产品名称 CO-1686(AVL-301) 英文名称 CO-1686 (AVL-301) 规格或纯度 ≥99% 生化机理 Description:IC50 Value: 21.5±1.7 nM (EGFRL858R/T790M); 303.3 ± 26.7 nM (EGFRWT) [1]CO-1686 is a novel, irreversible and orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M while exhibiting minimal activity towards the wild-type (WT) receptor.in vitro: CO-1686 is a potent inhibitor of EGFR L858R/T790M kinase (kinact/Ki = (2.41 ± 0.30) x 105 M-1s-1) and is approximately 22-fold selective over WT EGFR (kinactt/Ki = (1.12 ± 0.14) x 104 M-1s-1). CO-1686 potently inhibited proliferation in the mutant-EGFR NSCLC cellswith GI50 values ranging from 7 - 32 nM. In comparison, the GI50 value for A431 cells, an epidermoid cell line that is driven by amplified WT EGFR(19), was 547 nM. Two cell linesexpressing WT EGFR in the presence of an N- or KRAS mutation (NCI-H1299 and NCI-H358,respectively) were inhibited by CO-1686 at a concentration of 4275 and 1806 nM, respectively [1].CAS编号 1374640-70-6
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CAS:1206799-15-6|LY2801653
作者:德尔塔 日期:2022-03-15
产品名称 LY2801653 英文名称 LY2801653 规格或纯度 98% 英文别名 LY-2801653;LY 2801653;N-[3-fluoro-4-[1-methyl-6-(1H-pyrazol-4-yl)indazol-5-yl]oxyphenyl]-1-(4-fluorophenyl)-6-methyl-2-oxopyridine-3-carboxamide;Merestinib 运输条件 超低温冰袋运输 生化机理 Description: IC50 Value: 2 nM(Ki value) LY2801653 is a potent, orally bioavailable, small-molecule inhibitorLY2801653 targeting MET kinase. in vitro: LY2801653 is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase with a dissociation constant (K(i)) of 2 nM, a pharmacodynamic residence time (K(off)) of 0.00132 min(-1) and t(1/2) of 525 min [1]. LY2801653 was found to have potent activity against several other receptor tyrosine oncokinases including MST1R, FLT3, AX
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CAS:1254473-64-7|LY2874455
作者:德尔塔 日期:2022-03-15
产品名称 LY2874455 英文名称 LY2874455 规格或纯度 ≥99% 别名 LY 2874455; LY-2874455;4-[(1E)-2-[5-[(1R)-1-(3,5-Dichloro-4-pyridinyl)ethoxy]-1H-indazol-3-yl]ethenyl]-1H-pyrazole-1-ethanol 英文别名 LY 2874455; LY-2874455;4-[(1E)-2-[5-[(1R)-1-(3,5-Dichloro-4-pyridinyl)ethoxy]-1H-indazol-3-yl]ethenyl]-1H-pyrazole-1-ethanol 运输条件 超低温冰袋运输 生化机理 LY2874455 is a novel and potent FGF/FGFR Inhibitor. LY2874455 exhibits a potent activity against FGF/FGFR-mediated signaling in several cancer cell lines and shows an excellent broad spectrum of antitumor activity in several t
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CAS:388082-77-7|二对甲苯磺酸拉帕替尼(GW-572016)
作者:德尔塔 日期:2022-03-15
产品名称 二对甲苯磺酸拉帕替尼(GW-572016) 英文名称 Lapatinib Ditosylate (GW-572016) 规格或纯度 ≥98% 别名 GW-572016 生化机理 Lapatinib ditosylate is a selective and effective inhibitor of ErbB-2 and EGFR dual tyrosine kinases. ErbB-2 and EGFR dual tyrosine kinases are growth promoting factors that are over expressed in some breast cancer cell lines. Research studies have reported that Lapatinib Ditosylate can inhibit breast cancer cell proliferation.CAS编号 388082-77-7 溶解性
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CAS:796967-16-3|Linifanib (ABT-869)
作者:德尔塔 日期:2022-03-15
产品名称 Linifanib (ABT-869) 英文名称 Linifanib (ABT-869) 应用 A VEGF (Flk/Flt) and PDGFR inhibitor. 规格或纯度 ≥99% 生化机理 ABT-869 is an ATP-competitive, multi-targeted RTK inhibitor that is completely effective against all members of the vascular endothelial growth factor (Flt/Flk) and PDGFR families (e.g., KDR, Flt1, Flt3, Flt4, CSF-1R, and KIT) demonstrating IC50 values ranging from 4-190 nM. ABT-869 shows little activity against unrelated RTKs, cytoplasmic tyrosine kinases, or Ser/Thr kinases (IC50 > 1 μM). ABT-869 inhibits proliferation in MV-4-11 and MOLM-13 cells (acute myeloid leukemia cell lines harboring RTK mutations; IC50 = 4 and 6 nM, respectively), inducing apoptosis as evidenced by an increased sub-G0/G1 phase cell population, caspase activation, and PARP cleavage. In murine xenograft models, as well as in a phase 1 clinical trial, ABT-869 demonstrated respectable efficacy
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CAS:417716-92-8|Lenvatinib (E7080)
作者:德尔塔 日期:2022-03-15
产品名称 Lenvatinib (E7080) 英文名称 Lenvatinib (E7080) 规格或纯度 ≥99% 别名 乐伐替尼;仑伐替尼 英文别名 E7080;Vargatef;E-7080;E 7080; 4-[3-Chloro-4-(cyclopropylaminocarbonyl)aminophenoxy]-7-methoxy-6-quinolinecarboxamide 运输条件 超低温冰袋运输CAS编号 417716-92-8 溶解性
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CAS:24502-79-2|(β,β-二甲基丙烯酰基)紫草素
作者:德尔塔 日期:2022-03-15
产品名称 (β,β-二甲基丙烯酰基)紫草素 英文名称 (β,β-Dimethylacryl)shikonin 规格或纯度 >90.0%(HPLC) 别名 BATA,BATA-二甲基丙烯酰紫草素 英文别名 5,8-Dihydroxy-2-[1-(β,β-dimethylacryloyloxy)-4-methyl-3-pentenyl]-1,4-naphthalenedioneCAS编号 24502-79-2 敏感性 熔点 103-105℃
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CAS:845272-21-1|Varlitinib
作者:德尔塔 日期:2022-03-15
产品名称 Varlitinib 英文名称 Varlitinib 规格或纯度 ≥96%CAS编号 845272-21-1 敏感性 比旋光度 折光率 凝固点 沸点 溶解性
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CAS:443913-73-3|Vandetanib(ZD6474)
作者:德尔塔 日期:2022-03-15
产品名称 Vandetanib(ZD6474) 英文名称 Vandetanib (ZD6474) 应用 An antagonist of VEGFR (Flk and Flk) and EGFR families. 规格或纯度 ≥99% 别名 凡德他尼 英文别名 ZD6474;N-(4-bromo-2-fluorophenyl)-6-methoxy-7-((1-methylpiperidin-4-yl)methoxy)quinazolin-4-amine 运输条件 超低温冰袋运输 生化机理 口服有效的VEGFR2酪氨酸激酶\ xa0抑制剂\ xa0(KDR IC 50 = 40 nM)。\ xa0还抑制fms样酪氨酸激酶4(VEGFR3,IC 50 = 110 nM)和表皮生
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CAS:1214265-56-1|WZ3146
作者:德尔塔 日期:2022-03-15
产品名称 WZ3146 英文名称 WZ3146 应用 A mutant EGFR phosphorylation inhibitor 规格或纯度 ≥98% 别名 WZ3146; WZ 3146 英文别名 WZ3146;WZ 3146;N-[3-[[5-Chloro-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-2-propenamide 运输条件 超低温冰袋运输 生化机理 WZ3146 significantly suppresses the growth of EGFR mutation containing cell lines with IC50 of 3 nM in EGFR Del
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CAS:1213269-23-8|WZ4002
作者:德尔塔 日期:2022-03-15
产品名称 WZ4002 英文名称 WZ4002 应用 An EGFR phosphorylation inhibitor 规格或纯度 ≥98% 别名 WZ 4002; WZ-4002 生化机理 WZ 4002 is an inhibitor of EGFR phosphorylation in a variety of cancer cell lines including NIH-3T3 and H1975 cells. WZ 4002 is a potent inhibitor of EGFR, exhibiting an IC50 = 2 nM. This induces apoptosis in the cell due to the blocking of signal transduction from EGFR.CAS编号 1213269-23-8
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CAS:1214265-57-2|WZ8040
作者:德尔塔 日期:2022-03-15
产品名称 WZ8040 英文名称 WZ8040 应用 A potent inhibitor of EGFR T790M 规格或纯度 ≥98% 别名 WZ-8040; WZ 8040 生化机理 WZ8040 is 30- to 100-fold more potent against EGFR T790M, and up to 100-fold less potent against wild-type EGFR, than quinazoline-based EGFR inhibitors such as CL-387785 and HKI-272. WZ8040 treatment potently inhibits the growth of HCC827 (EGFR Del E746_A750), PC9 (EGFR Del E746_A750), H3255 (EGFR L858R), H1975 (EGFR L858R/T790M), and PC9 GR (EGFR Del E746_A750/T790M) with IC50 of 1 nM, 6 nM, 66 nM, 9 nM, and 8 nM, respectively. WZ8040 weakly inhibits the growth of HCC827 GR (EGFR E746_A750/MET amp), H1819 (ERBB2 amp), Calu-3 (ERBB2 amp), H1781 (ERBB2 I
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CAS:649735-63-7|Brivanib Alaninate (BMS-582664)
作者:德尔塔 日期:2022-03-15
产品名称 Brivanib Alaninate (BMS-582664) 英文名称 Brivanib Alaninate (BMS-582664) 规格或纯度 ≥95% 别名 Brivanib 丙氨酸酯;BMS582664 英文别名 BMS-582664; BMS 582664; BMS582664; (1R)-2-((4-((4-Fluoro-2-methyl-1H-indol-5-yl)oxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)oxy)-1-methylethyl L-alanine ester 运输条件 干冰运输CAS编号 649735-63-7
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CAS:649735-46-6|Brivanib (BMS-540215)
作者:德尔塔 日期:2022-03-15
产品名称 Brivanib (BMS-540215) 英文名称 Brivanib (BMS-540215) 应用 An ATP-competitive inhibitor against VEGFR-2, Flk-1, VEGFR-1 and FGFR-1 规格或纯度 ≥98% 别名 酪氨酸激酶抑制剂 生化机理 Brivanib is an ATP-competitive inhibitor against human VEGFR-2 and mouse Flk-1 with IC50 of 25 nM and 89 nM, respectively. Brivanib also inhibits VEGFR-1 and FGFR-1 with IC50 of 0.38 and 0.148 μM. Brivanib displays antitumor activities in H3396 xenograft. This compound completely inhibits the tumor growth, with TGI of 85% and 97%, respectively.CAS编号 649735-46-6
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CAS:319460-85-0|阿西替尼
作者:德尔塔 日期:2022-03-15
产品名称 阿西替尼 英文名称 Axitinib 应用 An inhibitor of Flt and Flk (VEGFR) with antitumor properties 规格或纯度 ≥99% 别名 阿西替尼;N-甲基-2-((3-((1E)-2-(吡啶-2-基)乙烯)-1H-吲唑-6-基)硫)苯甲酰胺 英文别名 AG-013736; N-Methyl-2-((3-((1E)-2-(pyridin-2-yl)ethenyl)-1H-indazol-6-yl)sulfanyl)benzamide;Axitinib 运输条件 超低温冰袋运输 生化机理 VEGFR-2,-3和-1的有效抑制剂(IC50值分别为0