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LY3009120
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LY3009120图片
CAS NO:1454682-72-4
包装与价格:
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

产品名称
DP-4978
产品介绍
LY3009120 (DP-4978) 是泛RAF抑制剂,其抑制BRAFV600E,BRAFWT和CRAFWTIC50分别为 5.8,9.1和15 nM。
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]

BRafV600E

5.8 nM (IC50)

Braf

9.1 nM (IC50)

CRAF

15 nM (IC50)

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
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 38 mg/mL(89.51 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.3557 mL11.7783 mL23.5566 mL
5 mM0.4711 mL2.3557 mL4.7113 mL
10 mM0.2356 mL1.1778 mL2.3557 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 5% DMSO    95% (20%SBE-β-CDin saline)

    Solubility: 2.5 mg/mL (5.89 mM); Suspended solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。