Tivantinib

别名: ARQ 197

目录号：S2753 Purity: 99.65%

Tivantinib是第一个非ATP竞争性的c-Met抑制剂，在无细胞试验中K_i为0.355 μM，对Ron几乎没有作用活性，对EGFR，InsR，PDGFRα和FGFR1/4没有抑制作用。Tivantinib (ARQ 197) 可诱导G2/M期细胞阻滞和凋亡。

Tivantinib Chemical Structure

CAS: 905854-02-6

规格	价格	库存
10mM (1mL in DMSO)	RMB 958.23	现货
10mg	RMB 904.93	现货
50mg	RMB 3844.69	现货
更大包装有超大折扣
400-668-6834 info@selleck.cn

客户使用Selleck的Tivantinib发表文献47篇

产品质控

批次：纯度： 99.65%

99.65

Tivantinib相关产品

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相关化合物库	激酶抑制剂库酪氨酸激酶抑制剂分子库 PI3K/Akt 抑制剂库细胞周期化合物库血管生成相关化合物库	点击展开

c-Met抑制剂选择性比较

细胞实验数据示例

细胞系	实验类型	给药浓度	活性描述	文献信息
MNK-45	Kinase assay	~10 μM	inhibits c-Met phosphorylation and downstream c-Met signaling pathways	20484018
HT29	Kinase assay	~10 μM	inhibits c-Met phosphorylation and downstream c-Met signaling pathways	20484018
MDA-MB-231	Kinase assay	~10 μM	inhibits c-Met phosphorylation and downstream c-Met signaling pathways	20484018
NCI-H441	Kinase assay	~10 μM	inhibits c-Met phosphorylation and downstream c-Met signaling pathways	20484018
SK-MEL-28	Growth inhibitory assay	33 μM	IC50>33 μM	20484018
NCI-H661	Growth inhibitory assay	33 μM	IC50>33 μM	20484018
NCI-H446	Growth inhibitory assay	33 μM	IC50=7 μM	20484018
MDA-MB-231	Growth inhibitory assay	33 μM	IC50=0.55 μM	20484018
DLD-1	Growth inhibitory assay	33 μM	IC50=0.53 μM	20484018
A549	Growth inhibitory assay	33 μM	IC50=0.59 μM	20484018
SK-OV-3	Growth inhibitory assay	33 μM	IC50=0.66 μM	20484018
NCI-H460	Growth inhibitory assay	33 μM	IC50=0.6 μM	20484018
A375	Growth inhibitory assay	33 μM	IC50=0.42 μM	20484018
NCI-H441	Growth inhibitory assay	33 μM	IC50=0.3 μM	20484018
HT29	Growth inhibitory assay	33 μM	IC50=0.49 μM	20484018
MKN-45	Growth inhibitory assay	33 μM	IC50=0.58 μM	20484018
HT29	Apoptosis assay	~10 μM	significantly induces apoptosis by 80-90%.	20484018
MKN-45	Apoptosis assay	~10 μM	significantly induces apoptosis by 80-90%.	20484018
MDA-MB-231	Apoptosis assay	~10 μM	modestly induces apoptosis by 35%.	20484018
MDA-MB-231/TGL	Growth inhibitory assay	~100 μM	GI50=1.2 μM	22027690
1833/TGL	Growth inhibitory assay	~100 μM	GI50=3.7 μM	22027690
EBC1	Cytotoxic assay	~10 μM	inhibits the cell growth.	23598276
SNU638	Cytotoxic assay	~10 μM	inhibits the cell growth.	23598276
A549	Cytotoxic assay	~10 μM	not affect	23598276
H460	Cytotoxic assay	~10 μM	not affect	23598276
HCC827	Cytotoxic assay	~10 μM	not affect	23598276
A549	Function assay	10 μM	disrupts microtubule	23598276
EBC1	Function assay	10 μM	disrupts microtubule	23598276
H460	Function assay	10 μM	inhibits tubulin polymerization	25313010
K562/VCR	Cytotoxic assay	~10 μM	shows cytotoxic activity	25313010
CEM/VBL	Cytotoxic assay	~10 μM	shows cytotoxic activity	25313010
U266	Cytotoxic assay	~3 μM	IC50=1.1 μM	25810013
OPM-2	Cytotoxic assay	~3 μM	IC50=1.8 μM	25810013
MM.1S	Cytotoxic assay	~3 μM	IC50=1.6 μM	25810013
MM.1R	Growth inhibitory assay	3 μM	inhibits cell growth by 49%	25810013
RPMI-8226	Cytotoxic assay	~3 μM	IC50=0.9 μM	25810013
ANBL-6	Cytotoxic assay	1 μM	induces cell death by more than 50%	25810013
ANLB-6/V10R	Cytotoxic assay	1 μM	induces cell death by more than 50%	25810013
KAS-6/1	Cytotoxic assay	1 μM	induces cell death by more than 50%	25810013
KAS-6/V10R	Cytotoxic assay	1 μM	induces cell death by more than 50%	25810013
KAS-6/R10R	Cytotoxic assay	1 μM	induces cell death by more than 50%	25810013
8226/S	Growth inhibitory assay	3 μM	inhibits cell growth by 54%	25810013
8226/LR-5	Growth inhibitory assay	3 μM	inhibits cell growth by 54%	25810013
Huh7	Cytotoxic assay	~4.8 μM	IC50=9.9 nM	26259250
Hep3B	Cytotoxic assay	~4.8 μM	IC50=448.7 nM	26259250
HepG2	Cytotoxic assay	~4.8 μM	IC50=139.77 nM	26259250
Chang	Cytotoxic assay	~4.8 μM	IC50=448.7 nM	26259250
Huh7	Function assay	1.6 μM	causes a G2/M cell cycle arrest	26259250
Hep3B	Function assay	1.6 μM	causes a G2/M cell cycle arrest	26259250
HepG2	Function assay	1.6 μM	causes a G2/M cell cycle arrest	26259250
Chang	Function assay	1.6 μM	causes a G2/M cell cycle arrest	26259250
MHCC97L	Growth inhibitory assay	~10 μM	IC50=315 nM	26458953
MHCC97H	Growth inhibitory assay	~10 μM	IC50=368 nM	26458953
Huh7	Growth inhibitory assay	~10 μM	IC50=265 nM	26458953
HepG2	Growth inhibitory assay	~10 μM	IC50=392 nM	26458953
MHCC97L	Function assay	1 μM	induces microtubules depolymerization	26458953
Huh7	Function assay	1 μM	induces microtubules depolymerization	26458953
MHCC97L	Apoptosis assay	1 μM	induces apoptosis	26458953
Huh7	Apoptosis assay	1 μM	induces apoptosis	26458953
C3H 10T1/2 mouse fibroblasts	Kinase assay	25 μM	reduces Histone H3 and H4 acetylation levels	20534345
H23	Growth inhibitory assay	25 μM	significantly inhibits cell growth.	20534345
WM35	Growth inhibitory assay	10 μM	significantly inhibits cell growth.	20534345
NIH 3T3	Growth inhibitory assay	10 μM	does not have a significant inhibitory effect	20534345
H838	Growth inhibitory assay	10 μM	does not have a significant inhibitory effect	20534345
H1395	Growth inhibitory assay	10 μM	does not have a significant inhibitory effect	20534345
Quiescent S2	Kinase assay	30 μM	completely abrogates TSA-induced hyperacetylation of H3K4me3 histones	21518915
PC3	Apoptosis assay	20 μM	induces apoptosis	21709130
Du145	Apoptosis assay	20 μM	induces apoptosis	21709130
LNCaP	Apoptosis assay	20 μM	induces apoptosis	21709130
LAPC-4	Apoptosis assay	20 μM	induces apoptosis	21709130
LNCaP	Function assay	20 μM	decreases PSA secretion and p65 expression levels	21709130
LAPC-4	Function assay	20 μM	decreases PSA secretion and p65 expression levels	21709130
Kasumi-1	Growth inhibitory assay	~50 μM	inhibits cell proliferation	23390536
SKNO-1	Growth inhibitory assay	~50 μM	inhibits cell proliferation	23390536
Kasumi-1	Kinase assay	~10 μM	reduces expression of acetylated histone H3, c-kit and bcl-2	23390536
SKNO-1	Kinase assay	~10 μM	reduces expression of acetylated histone H3, c-kit and bcl-2	23390536
A549	Function assay	10 μM	enhances mitotic catastrophe	24746574
NRK-52E	Function assay	10 μM	inhibits Ang II-induced STAT3 nuclear translocation and the expression of TGF-β1, collagen IV and fibronectin	25088002
PC12	Growth inhibitory assay	~12.5 μM	prevents TSA-induced neurite formation	25128386
A549	Function assay	~50 μM	affects the viral life cycle and host response	26711748
RAW264.7	Function assay	~30 μM	reduces pro-inflammatory gene expression	26718586
MEMM	Kinase assay	15 µM	decreases acetylation of histone H3	26921506
MEMM	Growth inhibitory assay	~20 µM	inhibits cell proliferation	26921506
MEMM	Apoptosis assay	15 µM	induces the presence of the apoptosis protein, cleaved Caspase-3	26921506
T47D	Growth inhibitory assay	10 μM	IC50=72 nM	18381444
ZR-75-1	Growth inhibitory assay	10 μM	IC50=79 nM	18381444
BT474	Growth inhibitory assay	10 μM	IC50=86 nM	18381444
HCC1954	Growth inhibitory assay	10 μM	IC50=119 nM	18381444
MDA-MB-453	Growth inhibitory assay	10 μM	IC50=975 nM	18381444
MDA-MB-468	Growth inhibitory assay	10 μM	IC50=3208 nM	18381444
SkBr3	Growth inhibitory assay	10 μM	IC50>10,000 nM	18381444
MDA-MB-231	Growth inhibitory assay	10 μM	IC50>10,000 nM	18381444
HCT116	Growth inhibitory assay	10 μM	IC50=5836 nM	18381444
HT29	Growth inhibitory assay	10 μM	IC50>10,000 nM	18381444
HFF	Growth inhibitory assay	10 μM	IC50=7615 nM	18381444
HN5	Growth inhibitory assay	10 μM	IC50>10,000 nM	18381444
786-0	Growth inhibitory assay	10 μM	IC50=4009 nM	18381444
H157	Growth inhibitory assay	10 μM	IC50=2642 nM	18381444
NCI-H460	Growth inhibitory assay	10 μM	IC50>2,500 nM	18381444
SKOV-3	Growth inhibitory assay	10 μM	IC50=2126 nM	18381444
OVCAR-3	Growth inhibitory assay	10 μM	IC50=2918 nM	18381444
BXPC3	Growth inhibitory assay	10 μM	IC50=3141 nM	18381444
MiaPaCa	Growth inhibitory assay	10 μM	IC50=5433 nM	18381444
PANC-1	Growth inhibitory assay	10 μM	IC50=8681 nM	18381444
LNCaP	Growth inhibitory assay	10 μM	IC50=147 nM	18381444
DU145	Growth inhibitory assay	10 μM	IC50=3812 nM	18381444
PC3	Growth inhibitory assay	10 μM	IC50>10,000 nM	18381444
BT474	Kinase assay	10 μM	inhibits pGSK3β with IC50 of 160 nM	18381444
786-0	Kinase assay	10 μM	inhibits pGSK3β with IC50 of 150 nM	18381444
LNCaP	Kinase assay	10 μM	inhibits pGSK3β with IC50 of 43 nM	18381444
PC3	Kinase assay	10 μM	inhibits pGSK3β with IC50 of 49 nM	18381444
KARPAS-231	Growth inhibitory assay	10 μM	EC50=41 nM	19064730
CCRFSB	Growth inhibitory assay	10 μM	EC50=155 nM	19064730
SUP B15	Growth inhibitory assay	10 μM	EC50=197 nM	19064730
SD-1	Growth inhibitory assay	10 μM	EC50=320 nM	19064730
RS4;11	Growth inhibitory assay	10 μM	EC50=654 nM	19064730
MN-60	Growth inhibitory assay	10 μM	EC50=3602 nM	19064730
Tanoue	Growth inhibitory assay	10 μM	EC50=4517 nM	19064730
RCH-ACV	Growth inhibitory assay	10 μM	EC50=152 nM	19064730
SEM	Growth inhibitory assay	10 μM	EC50=202 nM	19064730
KASUMI-2	Growth inhibitory assay	10 μM	EC50=225 nM	19064730
REH	Growth inhibitory assay	10 μM	EC50=288 nM	19064730
697	Growth inhibitory assay	10 μM	EC50=338 nM	19064730
NALM-6	Growth inhibitory assay	10 μM	EC50=421 nM	19064730
MHH-CALL–3	Growth inhibitory assay	10 μM	EC50=812 nM	19064730
MHH-CALL–2	Growth inhibitory assay	10 μM	EC50=2114 nM	19064730
J.GAMMA-1	Growth inhibitory assay	10 μM	EC50=65 nM	19064730
JR45.01	Growth inhibitory assay	10 μM	EC50=68 nM	19064730
A3	Growth inhibitory assay	10 μM	EC50=69 nM	19064730
I 2.1	Growth inhibitory assay	10 μM	EC50=73 nM	19064730
MOLT-3	Growth inhibitory assay	10 μM	EC50=74 nM	19064730
P116	Growth inhibitory assay	10 μM	EC50=78 nM	19064730
J.Cam1.6	Growth inhibitory assay	10 μM	EC50=79 nM	19064730
I 9.2	Growth inhibitory assay	10 μM	EC50=80 nM	19064730
LOUCY	Growth inhibitory assay	10 μM	EC50=117 nM	19064730
J.RT3-T3.5	Growth inhibitory assay	10 μM	EC50=123 nM	19064730
800000	Growth inhibitory assay	10 μM	EC50=163 nM	19064730
Jurkat	Growth inhibitory assay	10 μM	EC50=225 nM	19064730
MOLT-4	Growth inhibitory assay	10 μM	EC50=232 nM	19064730
Molt-16	Growth inhibitory assay	10 μM	EC50=241 nM	19064730
CEM/C3	Growth inhibitory assay	10 μM	EC50=257 nM	19064730
CEM/C2	Growth inhibitory assay	10 μM	EC50=271 nM	19064730
CCRFCEM	Growth inhibitory assay	10 μM	EC50=327 nM	19064730
CEM/C1	Growth inhibitory assay	10 μM	EC50=382 nM	19064730
SUPTI[VB]	Growth inhibitory assay	10 μM	EC50=619 nM	19064730
CCRF–HSB-2	Growth inhibitory assay	10 μM	EC50=2117 nM	19064730
I 2.1	Apoptosis assay	10 μM	induces apoptosis	19064730
I 9.2	Apoptosis assay	10 μM	induces apoptosis	19064730
A3	Apoptosis assay	10 μM	induces apoptosis	19064730
RD	Growth inhibitory assay	10 μM	IC50>10 μM	20740623
Rh41	Growth inhibitory assay	10 μM	IC50=33.8 nM	20740623
Rh18	Growth inhibitory assay	10 μM	IC50=303 nM	20740623
Rh30	Growth inhibitory assay	10 μM	IC50=4.81 μM	20740623
BT-12	Growth inhibitory assay	10 μM	IC50>10 μM	20740623
CHLA-266	Growth inhibitory assay	10 μM	IC50=1.22 μM	20740623
TC-71	Growth inhibitory assay	10 μM	IC50=2.52 μM	20740623
CHLA-9	Growth inhibitory assay	10 μM	IC50=591 nM	20740623
CHLA-10	Growth inhibitory assay	10 μM	IC50=102 nM	20740623
CHLA-258	Growth inhibitory assay	10 μM	IC50=1.05 μM	20740623
GBM2	Growth inhibitory assay	10 μM	IC50=9.15 μM	20740623
NB-1643	Growth inhibitory assay	10 μM	IC50=5.4 μM	20740623
NB-Ebc1	Growth inhibitory assay	10 μM	IC50>10 μM	20740623
CHLA-90	Growth inhibitory assay	10 μM	IC50>10 μM	20740623
CHLA-136	Growth inhibitory assay	10 μM	IC50>10 μM	20740623
NALM-6	Growth inhibitory assay	10 μM	IC50=265 nM	20740623
COG-LL-317	Growth inhibitory assay	10 μM	IC50=6.49 nM	20740623
RS4;11	Growth inhibitory assay	10 μM	IC50=147 nM	20740623
MOLT-4	Growth inhibitory assay	10 μM	IC50=40 nM	20740623
CCRF-CEM	Growth inhibitory assay	10 μM	IC50=268 nM	20740623
Kasumi-1	Growth inhibitory assay	10 μM	IC50=107 nM	20740623
Karpas-299	Growth inhibitory assay	10 μM	IC50=2.93 μM	20740623
Ramos-RA1	Growth inhibitory assay	10 μM	IC50=7.35 μM	20740623
H1299	Kinase assay	10 μM	inhibits IKBKE-induced Akt Activation	21908616
HPMCs	Function assay		reverses epithelial to mesenchymal transition of human peritoneal mesothelial cells	26045780
点击查看更多细胞系数据

生物活性

产品描述

特性

ARQ-197是第一个应用到晚期人类临床试验的c-Met选择性抑制剂。

靶点

c-Met ^[1]
(Cell-free assay)

0.355 μM(Ki)

体外研究(In Vitro)
体外研究活性	ARQ-197抑制HGF/c-met诱导的细胞反应。ARQ-197具有抗肿瘤活性，抑制A549, DBTRG和NCI-H441细胞增殖，IC50分别为0.38, 0.45, 0.29 μM。用ARQ-197处理，导致MAPK信号级联放大磷酸化降低，且阻断入侵和迁移。此外,没有内源性c-Met表达的NCI-H661细胞中c-Met异常表达，形成一种入侵表现型，也被ARQ-197抑制。加入浓度不断增加的ARQ-197不会明显影响ATP的K_m值，但是用0.5 μM ARQ-197处理c-Met，则降低c-Met的V_max值，降低3倍。ARQ-197降低V_max而不影响ATP的K_m值说明ARQ-197抑制c-Met是非ATP竞争抑制，也说明ARQ-197具有高度激酶选择性。ARQ-197抑制人类重组c-Met，具有恒定的K_i值，为355 nM。虽然使用过的ATP最高浓度为200 μM, 但是当ATP浓度为1 mM时，ARQ-197抑制c-Met效果不会降低。ARQ-197抑制c-Met磷酸化，且阻断下游c-Met信号通路。ARQ-197阻断组成型和配体调节的c-Met自磷酸化，通过增强c-Met活性, 反过来抑制下游c-Met效应器。ARQ-197作用于表达c-Met的人类癌细胞包括HT29, MKN-45, 和MDA-MB-231细胞，诱导caspase依赖的凋亡。^[1]
激酶实验	体外c-Met SDS-PAGE 激酶试验
激酶实验	100 ng重组c-Met蛋白和浓度不断增高ARQ-197在室温下预温育30分钟。随后，100 μM 聚Glu-Tyr底物和含5 μCi[γ-³²P]ATP的不同浓度ATP加到反应混合物中。反应在室温下进行5分钟，然后加入5 μL SDS-聚丙烯酰胺胶,降低样本缓冲液。上样到7.5%丙烯酰胺胶上，进行SDS-PAGE。通过放射自显影观察到磷酸化的聚Glu-Tyr底物。通过光密度法测定c-Met活性。
细胞实验	细胞系	T29, MKN-45和MDA-MB-231细胞
	浓度	0.03-10 μM
	孵育时间	24, 32,和48细胞
	方法	HT29,MKN-45,和MDA-MB-231细胞按每孔5×10³个接种在96孔板上，孔中有含10% FBS的培养基，在黑暗中过夜处理。第二天,用浓度不断增长的ARQ-197 (0.03-10 μM)在37^oC下处理细胞24,32,和48 小时。ARQ-197处理后，移除培养基，细胞在含2 μg/mL Hoescht 33342的标签溶液(10 mM HEPES, 140 mM NaCl,和6 mM CaCl₂)中温育至少10分钟, 用Annexin V-FITC(稀释500倍)和1 μg/mL碘化丙锭染色。进行高含量的图像采集和分析，每孔获取四个图像。 4,6-二脒基-2-苯基吲哚, FITC, 和罗丹明通道分别在16.7 ms/10%, 500 ms/35% ,和300 ms/30% 进行处理。处理图像，测定每组通道和每种情况下的阳性细胞数。此外,在有或者没有25,50,和100 μM ZvAD-FMK存在条件下，HT29细胞用浓度不断增加的ARQ-197处理32小时。所有实验重复进行三次。测定抑制c-Met是否导致细胞凋亡，当使用siRNA分解磷酸甘油醛脱氢酶(GAPDH)和c-Met时ARQ-197的作用效果。HT29, MKN-45,和MDA-MB-231细胞转染无靶点对照 siRNA, GAPDH靶点对照siRNA, 或met靶点siRNA。3天后，使用特点抗体测定c-Met, GAPDH, 和 β-actin表达水平。为了测定caspase依赖是否影响，HT29, MKN-45, 和MDA-MB-231细胞转染 met靶点 siRNA，进行2天。然后在有或没有浓度不断增高的ZvAD-FMK存在下再温育1天。无靶点siRNA和GAPDH siRNA也转染，作为对照。然后用Annexin V-FITC和碘化丙锭进行细胞染色,测定凋亡细胞百分数。
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	cMET / p-cMET / p-AKT / p-ERK / p-rpS6		23022995
	Growth inhibition assay	Cell viability		23598276

体内研究(In Vivo)
体内研究活性	ARQ-197处理 HT29,MKN-45,和MDA-MB-231三种移植瘤模型，肿瘤生长率分别降低66%,45%,和79%。ARQ-197按200 mg/kg剂量口服给药这三种移植瘤模型，显示体重都没有明显改变。药效学方面，ARQ-197作用于人类结肠移植瘤HT29，强抑制c-Met的磷酸化, ARQ-197按200 mg/kg剂量单独口服给药24小时后，c-Met自磷酸化强烈下降。总之，ARQ-197抑制人类c-Met依赖的移植瘤生长。^[1]
动物实验	Animal Models	携带HT29,MKN-45,或MDA-MB-231移植瘤的无胸腺裸鼠
	Dosages	200 mg/kg
	Administration	口服处理

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT02150733	Completed	Hepatic Impairment\|Solid Tumor\|Cancer	Daiichi Sankyo Inc.\|Medpace Inc.	April 2014	Phase 1
NCT01892527	Completed	Colorectal Cancer Metastatic\|C-met Overexpression	Armando Santoro MD\|Istituto Clinico Humanitas	March 2013	Phase 2
NCT02049060	Completed	Malignant Pleural Mesothelioma\|Nonsquamous Nonsmall Cell Neoplasm of Lung	Armando Santoro MD\|Istituto Clinico Humanitas	January 2013	Phase 1\|Phase 2
NCT01755767	Completed	Hepatocellular Carcinoma	Daiichi Sankyo Inc.\|ArQule Inc. a subsidiary of Merck Sharp & Dohme LLC a subsidiary of Merck & Co. Inc. (Rahway NJ USA)	December 27 2012	Phase 3

参考文献
[1] Munshi N, et al. Mol Cancer Ther. 2010, 9(6), 1544-1553. [2] Comoglio PM, et al. Nat Rev Drug Discov, 2008, 7(6), 504-516.

参考文献

化学信息&溶解度

分子量	369.42	分子式	C₂₃H₁₉N₃O₂
CAS号	905854-02-6	SDF	Download Tivantinib SDF
Smiles	C1CC2=C3C(=CC=C2)C(=CN3C1)C4C(C(=O)NC4=O)C5=CNC6=CC=CC=C65
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 73 mg/mL ( (197.6 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 35 mg/mL

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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常见问题及建议解决方法

问题 1:
Are there any other solutions (apart from DMSO) I can dissolve S2753 for in vivo experiment?

回答：
S2753 Tivantinib (ARQ 197) can be dissolved in 1% methylcellulose at15 mg/ml as a suspension.

C1=C0/X	C1:	LOG(C1):
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