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Tivantinib

別名: ARQ 197

Tivantinib是第一個非ATP競爭性的c-Met抑制劑，在無細(xì)胞試驗(yàn)中Ki為0.355 μM，對Ron幾乎沒有作用活性，對EGFR，InsR，PDGFRα和FGFR1/4沒有抑制作用。Tivantinib (ARQ 197) 可誘導(dǎo)G2/M期細(xì)胞阻滯和凋亡。

Tivantinib Chemical Structure

Tivantinib Chemical Structure

CAS: 905854-02-6

規(guī)格 價(jià)格 庫存 購買數(shù)量
10mM (1mL in DMSO) 958.23 現(xiàn)貨
10mg 904.93 現(xiàn)貨
50mg 3844.69 現(xiàn)貨
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Tivantinib相關(guān)產(chǎn)品

相關(guān)信號通路圖

c-Met Signaling Pathways

c-Met信號通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)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
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生物活性

產(chǎn)品描述 Tivantinib是第一個非ATP競爭性的c-Met抑制劑，在無細(xì)胞試驗(yàn)中Ki為0.355 μM，對Ron幾乎沒有作用活性，對EGFR，InsR，PDGFRα和FGFR1/4沒有抑制作用。Tivantinib (ARQ 197) 可誘導(dǎo)G2/M期細(xì)胞阻滯和凋亡。
特性 ARQ-197是第一個應(yīng)用到晚期人類臨床試驗(yàn)的c-Met選擇性抑制劑。
靶點(diǎn)
c-Met [1]
(Cell-free assay)
0.355 μM(Ki)
體外研究(In Vitro)
體外研究活性

ARQ-197抑制HGF/c-met誘導(dǎo)的細(xì)胞反應(yīng)。ARQ-197具有抗腫瘤活性，抑制A549, DBTRG和NCI-H441細(xì)胞增殖，IC50分別為0.38, 0.45, 0.29 μM。用ARQ-197處理，導(dǎo)致MAPK信號級聯(lián)放大磷酸化降低，且阻斷入侵和遷移。此外,沒有內(nèi)源性c-Met表達(dá)的NCI-H661細(xì)胞中c-Met異常表達(dá)，形成一種入侵表現(xiàn)型，也被ARQ-197抑制。加入濃度不斷增加的ARQ-197不會明顯影響ATP的Km值，但是用0.5 μM ARQ-197處理c-Met，則降低c-Met的Vmax值，降低3倍。ARQ-197降低Vmax而不影響ATP的Km值說明ARQ-197抑制c-Met是非ATP競爭抑制，也說明ARQ-197具有高度激酶選擇性。ARQ-197抑制人類重組c-Met，具有恒定的Ki值，為355 nM。雖然使用過的ATP最高濃度為200 μM, 但是當(dāng)ATP濃度為1 mM時(shí)，ARQ-197抑制c-Met效果不會降低。ARQ-197抑制c-Met磷酸化，且阻斷下游c-Met信號通路。ARQ-197阻斷組成型和配體調(diào)節(jié)的c-Met自磷酸化，通過增強(qiáng)c-Met活性, 反過來抑制下游c-Met效應(yīng)器。ARQ-197作用于表達(dá)c-Met的人類癌細(xì)胞包括HT29, MKN-45, 和MDA-MB-231細(xì)胞，誘導(dǎo)caspase依賴的凋亡。[1]
激酶實(shí)驗(yàn) 體外c-Met SDS-PAGE 激酶試驗(yàn)
100 ng重組c-Met蛋白和濃度不斷增高ARQ-197在室溫下預(yù)溫育30分鐘。隨后，100 μM 聚Glu-Tyr底物和含5 μCi[γ-32P]ATP的不同濃度ATP加到反應(yīng)混合物中。反應(yīng)在室溫下進(jìn)行5分鐘，然后加入5 μL SDS-聚丙烯酰胺膠,降低樣本緩沖液。上樣到7.5%丙烯酰胺膠上，進(jìn)行SDS-PAGE。通過放射自顯影觀察到磷酸化的聚Glu-Tyr底物。通過光密度法測定c-Met活性。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 T29, MKN-45和MDA-MB-231細(xì)胞
濃度 0.03-10 μM
孵育時(shí)間 24, 32,和48細(xì)胞
方法

HT29,MKN-45,和MDA-MB-231細(xì)胞按每孔5×103個接種在96孔板上，孔中有含10% FBS的培養(yǎng)基，在黑暗中過夜處理。第二天,用濃度不斷增長的ARQ-197 (0.03-10 μM)在37oC下處理細(xì)胞24,32,和48 小時(shí)。ARQ-197處理后，移除培養(yǎng)基，細(xì)胞在含2 μg/mL Hoescht 33342的標(biāo)簽溶液(10 mM HEPES, 140 mM NaCl,和6 mM CaCl2)中溫育至少10分鐘, 用Annexin V-FITC(稀釋500倍)和1 μg/mL碘化丙錠染色。進(jìn)行高含量的圖像采集和分析，每孔獲取四個圖像。 4,6-二脒基-2-苯基吲哚, FITC, 和羅丹明通道分別在16.7 ms/10%, 500 ms/35% ,和300 ms/30% 進(jìn)行處理。處理圖像，測定每組通道和每種情況下的陽性細(xì)胞數(shù)。此外,在有或者沒有25,50,和100 μM ZvAD-FMK存在條件下，HT29細(xì)胞用濃度不斷增加的ARQ-197處理32小時(shí)。所有實(shí)驗(yàn)重復(fù)進(jìn)行三次。測定抑制c-Met是否導(dǎo)致細(xì)胞凋亡，當(dāng)使用siRNA分解磷酸甘油醛脫氫酶(GAPDH)和c-Met時(shí)ARQ-197的作用效果。HT29, MKN-45,和MDA-MB-231細(xì)胞轉(zhuǎn)染無靶點(diǎn)對照 siRNA, GAPDH靶點(diǎn)對照siRNA, 或met靶點(diǎn)siRNA。3天后，使用特點(diǎn)抗體測定c-Met, GAPDH, 和 β-actin表達(dá)水平。為了測定caspase依賴是否影響，HT29, MKN-45, 和MDA-MB-231細(xì)胞轉(zhuǎn)染 met靶點(diǎn) siRNA，進(jìn)行2天。然后在有或沒有濃度不斷增高的ZvAD-FMK存在下再溫育1天。無靶點(diǎn)siRNA和GAPDH siRNA也轉(zhuǎn)染，作為對照。然后用Annexin V-FITC和碘化丙錠進(jìn)行細(xì)胞染色,測定凋亡細(xì)胞百分?jǐn)?shù)。
實(shí)驗(yàn)圖片 檢測方法 檢測指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot cMET / p-cMET / p-AKT / p-ERK / p-rpS6 23022995
Growth inhibition assay Cell viability 23598276
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

ARQ-197處理 HT29,MKN-45,和MDA-MB-231三種移植瘤模型，腫瘤生長率分別降低66%,45%,和79%。ARQ-197按200 mg/kg劑量口服給藥這三種移植瘤模型，顯示體重都沒有明顯改變。藥效學(xué)方面，ARQ-197作用于人類結(jié)腸移植瘤HT29，強(qiáng)抑制c-Met的磷酸化, ARQ-197按200 mg/kg劑量單獨(dú)口服給藥24小時(shí)后，c-Met自磷酸化強(qiáng)烈下降?？傊珹RQ-197抑制人類c-Met依賴的移植瘤生長。[1]
動物實(shí)驗(yàn) Animal Models 攜帶HT29,MKN-45,或MDA-MB-231移植瘤的無胸腺裸鼠
Dosages 200 mg/kg
Administration 口服處理
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02150733 Completed
Hepatic Impairment|Solid Tumor|Cancer
Daiichi Sankyo|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|ArQule Inc. a subsidiary of Merck Sharp & Dohme LLC a subsidiary of Merck & Co. Inc. (Rahway NJ USA)
 December 27 2012 Phase 3

化學(xué)信息&溶解度

分子量 369.42 分子式

C23H19N3O2
CAS號 905854-02-6 SDF Download Tivantinib SDF
Smiles C1CC2=C3C(=CC=C2)C(=CN3C1)C4C(C(=O)NC4=O)C5=CNC6=CC=CC=C65
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 73 mg/mL ( (197.6 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 35 mg/mL (94.74 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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常見問題及建議解決方法

問題 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.

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