CAS NO: | 1454682-72-4 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | LY3009120 (DP-4978) is a panRAFinhibitor which inhibitsBRAFV600E,BRAFWTand CRAFWTwithIC50s of 5.8, 9.1 and 15 nM, respectively. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | In the whole-cell based KiNativ assay, LY3009120 shows affinity to each RAF isoform with the IC50of 44, 31-47 and 42 nM for ARAF, BRAF and CRAF respectively. LY3009120 exhibits anti-proliferative effects on cell lines harboring BRAFV600E, KRASG13and KRASG12mutations. LY3009120 (1 μM) inhibits the phosphorylation of both MEK1/2 and ERK1/2 in cell lines with high basal levels of pMEK1/2 and pERK1/2 (RKO and HCT 116)[1]. LY3009120 shows inhibitory effect on tumor cells such as BxPC-3, NCI-H2405 and OV-90 cell lines. LY3009120 (0.01 μM) demonstrates potent and dose-dependent inhibition of phospho-MEK and ERK in all three cell lines. LY3009120 demonstrates a concentration-dependent cell growth inhibition with IC50values of 0.04, 0.087, and 0.007 μM against H2405, BxPC-3, and OV-90 cells, respectively[2]. LY3009120 inhibits BRAFWT, CRAFWT, BRAFV600E, and BRAFV600E+G468Awith the IC50values of 9.1, 15, 5.8, and 17 nM, respectively. LY3009120 induces BRAF-CRAF dimerization but inhibits the phosphorylation of downstream MEK and ERK. LY3009120 also inhibits various forms of RAF dimers including BRAF or CRAF homodimers[3]. LY3009120 gives only very minor activation at very low doses, with near complete inhibition of phospho-ERK at concentrations above 100 nM[4]. | ||||||||||||||||
体内研究 (In Vivo) | LY3009120 (20 mg/kg bid) displays significant activity in in vivo BRAFmutand KRASmutCRC xenograft models. In Colo 205 xenografts (BRAFmut), LY3009120 results in statistically significant tumor regression, while treatment of HCT 116 xenografts (KRASmut) results in statistically significant inhibition of tumor growth. LY3009120 treatment reduces pMEK1/2 in all HT-29 xenografts and reduces pERK1/2 in the majority of HT-29 xenografts[1]. LY3009120 (15 or 30 mg/kg) achieves almost complete tumor growth regression, and inhibits downstream phospho-MEK and ERK by approximately 70% and 60%, respectively, in the H2405 model[2]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 424.51 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C23H29FN6O | ||||||||||||||||
CAS 号 | 1454682-72-4 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : ≥ 38 mg/mL(89.51 mM) *"≥" means soluble, but saturation unknown. 配制储备液
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