Dovitinib (TKI-258)

別名: CHIR-258

目錄號(hào)：S1018 Purity: 99.98%

Dovitinib (TKI-258, CHIR-258)是一種多靶點(diǎn)的RTK抑制劑，在無(wú)細(xì)胞試驗(yàn)中對(duì)III型(FLT3/c-Kit)作用最強(qiáng)，IC50為1 nM/2 nM，同時(shí)也作用于IV類(FGFR1/3)和V類(VEGFR1-4) RTKs，IC50為8-13 nM，但對(duì)InsR，EGFR，c-Met，EphA2，Tie2，IGF-1R和HER2作用較弱。Phase 4。

Dovitinib (TKI-258) Chemical Structure

CAS: 405169-16-6

規(guī)格	價(jià)格	庫(kù)存
10mM (1mL in DMSO)	1559.76	現(xiàn)貨
10mg	1382.19	現(xiàn)貨
25mg	2198.71	現(xiàn)貨
50mg	3845.24	現(xiàn)貨
1g	15900	現(xiàn)貨
更大包裝有超大折扣
400-668-6834 info@selleck.cn

產(chǎn)品質(zhì)控

批次：純度： 99.98%

99.98

Dovitinib (TKI-258)相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	FLT3-WT FLT3-ITD FLT3-D835Y	點(diǎn)擊展開(kāi)
相關(guān)產(chǎn)品	Dovitinib (TKI258) Lactate monohydrate Tandutinib (MLN518) KW-2449 ENMD-2076 UNC2025 AST-487 (NVP-AST487) TCS 359 FF-10101 G-749 SKLB4771 (FLT3-IN-1) AMG 925	點(diǎn)擊展開(kāi)
相關(guān)化合物庫(kù)	酪氨酸激酶抑制劑分子庫(kù) PI3K/Akt 抑制劑庫(kù) 血管生成相關(guān)化合物庫(kù) HIF-1信號(hào)通路化合物庫(kù) FDA抗癌藥物庫(kù)	點(diǎn)擊展開(kāi)

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
Hep3B	Growth Inhibition Assay	0.1-10 μM	24 h	induces G2?arrest?	24238094
HeLa	Growth Inhibition Assay	0.1-10 μM	24 h	induces G2/M arrest in a concentration-dependent manner	24238094
C666-1	Growth Inhibition Assay	0.1-10 μM	48?h	induces G2/M delay in a concentration-dependent manner	24238094
CNE2?	Growth Inhibition Assay	0.1-10 μM	48?h	induces G2/M delay in a concentration-dependent manner	24238094
HNE1	Growth Inhibition Assay	0.1-10 μM	48?h	induces G2/M delay in a concentration-dependent manner	24238094
HONE1	Growth Inhibition Assay	0.1-10 μM	48?h	induces G2/M delay in a concentration-dependent manner	24238094
RT4	Cell Viability Assay	1-10 μM	72 h	inhibits cell growth in a dose dependent manner	24325461
TCC-SUP	Cell Viability Assay	1-10 μM	72 h	inhibits cell growth in a dose dependent manner	24325461
BFTC905	Cell Viability Assay	1-10 μM	72 h	inhibits cell growth in a dose dependent manner	24325461
T24	Cell Viability Assay	1-10 μM	72 h	inhibits cell growth in a dose dependent manner	24325461
RT112	Cell Viability Assay	1-10 μM	72 h	inhibits cell growth in a dose dependent manner	24325461
HT1376	Cell Viability Assay	1-10 μM	72 h	inhibits cell growth in a dose dependent manner	24325461
MGHU4	Cell Viability Assay	1-10 μM	72 h	inhibits cell growth in a dose dependent manner	24325461
HU456	Cell Viability Assay	1-10 μM	72 h	inhibits cell growth in a dose dependent manner	24325461
5637	Cell Viability Assay	1-10 μM	72 h	inhibits cell growth in a dose dependent manner	24325461
UMC3	Cell Viability Assay	1-10 μM	72 h	inhibits cell growth in a dose dependent manner	24325461
MFE-296?	Function Assay	0.05/0.1/0.5 μM	72 h	causes a decrease in STAT3, ERK, and AKT phosphorylation	24495750
AN3CA	Function Assay	0.05/0.1/0.5 μM	72 h	causes a decrease in STAT3, ERK, and AKT phosphorylation	24495750
HEC-1A	Function Assay	0.05/0.1/0.5 μM	72 h	causes a decrease in STAT3, ERK, and AKT phosphorylation	24495750
SEM-K2	Apoptosis Assay	0.1/1 μM	24 h	induces early apoptosis of SEM-K2 cells at 0.1 μM after 24 h	25202072
Nalm-6	Apoptosis Assay	2 μM	24/48 h	induces apoptosis resulting in about 72% of cell death after 24 h treatment and 81% after 48 h	25202072
HUVEC	Cell Viability Assay	0-25 μM	72 h	inhibits cell growth in a dose dependent manner	23228017
HMVEC	Cell Viability Assay	0-25 μM	72 h	inhibits cell growth in a dose dependent manner	23228017
MHCC-97H	Cell Viability Assay	0-25 μM	72 h	inhibits cell growth in a dose dependent manner	23228017
SMMC7721	Cell Viability Assay	0-25 μM	72 h	inhibits cell growth in a dose dependent manner	23228017
Huh-7	Apoptosis Assay	0-12.5 μM	24 h	sensitizes HCC cells to TRAIL- and tigatuzumab-induced apoptosis in a dose-dependent manner	22230479
Sk-Hep1	Apoptosis Assay	0-12.5 μM	24 h	sensitizes HCC cells to TRAIL- and tigatuzumab-induced apoptosis in a dose-dependent manner	22230479
Hep3B	Apoptosis Assay	0-12.5 μM	24 h	sensitizes HCC cells to TRAIL- and tigatuzumab-induced apoptosis in a dose-dependent manner	22230479
PLC5	Apoptosis Assay	0-12.5 μM	24 h	sensitizes HCC cells to TRAIL- and tigatuzumab-induced apoptosis in a dose-dependent manner	22230479
PLC5	Cell Viability Assay	0-15 μM	72 h	reduces cell viability in a dose-dependent manner?	22180308
Hep3B	Cell Viability Assay	0-15 μM	72 h	reduces cell viability in a dose-dependent manner?	22180308
Sk-Hep1	Cell Viability Assay	0-15 μM	72 h	reduces cell viability in a dose-dependent manner?	22180308
Huh-7	Cell Viability Assay	0-15 μM	72 h	reduces cell viability in a dose-dependent manner?	22180308
PLC5	Apoptosis Assay	0-15 μM	24 h	increases apoptotic cell death in a dose-dependent manner?	22180308
Hep3B	Apoptosis Assay	0-15 μM	24 h	increases apoptotic cell death in a dose-dependent manner?	22180308
Sk-Hep1	Apoptosis Assay	0-15 μM	24 h	increases apoptotic cell death in a dose-dependent manner?	22180308
Huh-7	Apoptosis Assay	0-15 μM	24 h	increases apoptotic cell death in a dose-dependent manner?	22180308
PLC5	Function Assay	0-10 μM	24 h	causes dose-dependent DNA fragmentation	22180308
Hep3B	Function Assay	0-10 μM	24 h	causes dose-dependent DNA fragmentation	22180308
Sk-Hep1	Function Assay	0-10 μM	24 h	causes dose-dependent DNA fragmentation	22180308
Huh-7	Function Assay	0-10 μM	24 h	causes dose-dependent DNA fragmentation	22180308
RT112	Function Assay	500 nM	24 h	increases the proportion of cells in G1?accompanied by a decrease in S and G2/M phases	21119661
RT4	Function Assay	500 nM	24 h	increases the proportion of cells in G1?accompanied by a decrease in S and G2/M phases	21119661
MGH-U3	Function Assay	500 nM	24 h	increases the proportion of cells in G1?accompanied by a decrease in S and G2/M phases	21119661
SW780	Function Assay	500 nM	24 h	increases the proportion of cells in G1?accompanied by a decrease in S and G2/M phases	21119661
97-7	Function Assay	500 nM	24 h	increases the proportion of cells in G1?accompanied by a decrease in S and G2/M phases	21119661
?J807C	Cell Viability Assay	0-400 nM	48 h	inhibits cell growth in a dose dependent manner	15598814
Y373C	Cell Viability Assay	0-400 nM	48 h	inhibits cell growth in a dose dependent manner	15598814
K650E	Cell Viability Assay	0-400 nM	48 h	inhibits cell growth in a dose dependent manner	15598814
G384D	Cell Viability Assay	0-400 nM	48 h	inhibits cell growth in a dose dependent manner	15598814
F384L	Cell Viability Assay	0-400 nM	48 h	inhibits cell growth in a dose dependent manner	15598814
NCI-H1703	Function assay	10 uM	24 hrs	Inhibition of TNIK in human NCI-H1703 cells transfected with lentiviral vector 7TFP assessed as reduction of GSK3 inhibitor X activated TNIK-mediated Wnt/TCF/beta-catenin-dependent transcription at 10 uM after 24 hrs by luciferase reporter assay	ChEMBL
LoVo	Cytotoxicity assay	10 uM	72 hrs	Cytotoxicity against Wnt/beta-catenin signalling dependent human LoVo cells assessed as cell viability at 10 uM after 72 hrs by ATPlite assay	ChEMBL
HCT116	Cytotoxicity assay	10 uM	72 hrs	Cytotoxicity against Wnt/beta-catenin signalling dependent human HCT116 cells assessed as cell viability at 10 uM after 72 hrs by ATPlite assay	ChEMBL
Huh7	Growth Inhibition Assay		72 h	IC50=3.980 ± 0.803 μM	23546591
PLC/PRF5	Growth Inhibition Assay		72 h	IC50=3.110 ± 0.337 μM	23546591
Hep3B	Growth Inhibition Assay		72 h	IC50=0.892 ± 0.044 μM	23546591
HepG2	Growth Inhibition Assay		72 h	IC50=1.200 ± 0.226 μM	23546591
Huh7	Growth Inhibition Assay		48 h	IC50=15.007 ± 7.334 μM	23546591
PLC/PRF5	Growth Inhibition Assay		48 h	IC50=16.120 ± 4.001 μM	23546591
Hep3B	Growth Inhibition Assay		48 h	IC50=4.223 ± 0.839 μM	23546591
HepG2	Growth Inhibition Assay		48 h	IC50=2.727 ± 0.429 μM	23546591
SW780	Growth Inhibition Assay		5 d	IC50=50 nM	21119661
RT112	Growth Inhibition Assay		5 d	IC50=15 nM	21119661
RT4	Growth Inhibition Assay		5 d	IC50=5 nM	21119661
JMSU1	Growth Inhibition Assay		5 d	IC50=50 nM	21119661
J82	Growth Inhibition Assay		5 d	IC50=1400 nM	21119661
97-7	Growth Inhibition Assay		5 d	IC50=1000 nM	21119661
KMS11	Growth Inhibition Assay		72 h	IC50=90 nM	15598814
KMS18	Growth Inhibition Assay		72 h	IC50=550 nM	15598814
OPM2	Growth Inhibition Assay		72 h	IC50=90 nM	15598814
H929	Growth Inhibition Assay		72 h	IC50> 2500 nM	15598814
8226	Growth Inhibition Assay		72 h	IC50> 2500 nM	15598814
U266	Growth Inhibition Assay		72 h	IC50> 2500 nM	15598814
insect cells	Function assay		1 to 4 hrs	Inhibition of recombinant PDGFRbeta (unknown origin) expressed in baculovirus infected insect cells using biotinylated peptide substrate GGLFDDPSYVNVQNL in presence of ATP incubated for 1 to 4 hrs by time resolved fluorescence assay, IC50=0.001μM	27914362
Sf9	Function assay		1 to 4 hrs	Inhibition of recombinant human N-terminal GST/His6-tagged c-KIT (544 to 976 residues) expressed in baculovirus infected sf9 cells using biotinylated peptide substrate GGLFDDPSYVNVQNL in presence of ATP incubated for 1 to 4 hrs by time resolved fluorescen, IC50=0.001μM	27914362
Sf9	Function assay		1 to 4 hrs	Inhibition of recombinant human N-terminal GST/His6-tagged FLT3 (571 to 993 residues) expressed in baculovirus infected sf9 cells using biotinylated peptide substrate GGLFDDPSYVNVQNL in presence of ATP incubated for 1 to 4 hrs by time resolved fluorescenc, IC50=0.001μM	27914362
insect cells	Function assay		1 to 4 hrs	Inhibition of recombinant FGFR1 (unknown origin) expressed in baculovirus infected insect cells using biotinylated peptide substrate GGGGQDGKDYIVLPI in presence of ATP incubated for 1 to 4 hrs by time resolved fluorescence assay, IC50=0.008μM	27914362
insect cells	Function assay		1 to 4 hrs	Inhibition of recombinant VEGFR3 (unknown origin) expressed in baculovirus infected insect cells using biotinylated peptide substrate GGGGQDGKDYIVLPI in presence of ATP incubated for 1 to 4 hrs by time resolved fluorescence assay, IC50=0.008μM	27914362
insect cells	Function assay		1 to 4 hrs	Inhibition of recombinant VEGFR1 (unknown origin) expressed in baculovirus infected insect cells using biotinylated peptide substrate GGGGQDGKDYIVLPI in presence of ATP incubated for 1 to 4 hrs by time resolved fluorescence assay, IC50=0.01μM	27914362
insect cells	Function assay		1 to 4 hrs	Inhibition of recombinant VEGFR2 (unknown origin) expressed in baculovirus infected insect cells using biotinylated peptide substrate GGGGQDGKDYIVLPI in presence of ATP incubated for 1 to 4 hrs by time resolved fluorescence assay, IC50=0.013μM	27914362
insect cells	Function assay		1 to 4 hrs	Inhibition of recombinant FGFR1 (unknown origin) expressed in baculovirus infected insect cells using GGGGQDGKDYIVLPI as substrate after 1 to 4 hrs by time-resolved fluorescence assay, IC50=0.008μM	30503938
MFE319	Growth Inhibition Assay			IC50=1.87 ± 0.45 μM	23443805
EN	Growth Inhibition Assay			IC50=1.66 ± 0.01 μM	23443805
USPC2	Growth Inhibition Assay			IC50=1.62 ± 0.01 μM	23443805
SNGM	Growth Inhibition Assay			IC50=1.42 ± 0.13 μM	23443805
KLE	Growth Inhibition Assay			IC50=1.37 ± 0.02 μM	23443805
HEC1A	Growth Inhibition Assay			IC50=1.34 ± 0.30 μM	23443805
ISHIKAWA	Growth Inhibition Assay			IC50=1.30 ± 0.11 μM	23443805
SNGII	Growth Inhibition Assay			IC50=1.24 ± 0.28 μM	23443805
EN1	Growth Inhibition Assay			IC50=1.02 ± 0.25 μM	23443805
RL952	Growth Inhibition Assay			IC50=0.93 ± 0.01 μM	23443805
SPAC1S	Growth Inhibition Assay			IC50=0.77 ± 0.08 μM	23443805
MFE296	Growth Inhibition Assay			IC50=0.66 ± 0.19 μM	23443805
HEC155	Growth Inhibition Assay			IC50=0.66 ± 0.09 μM	23443805
AN3CA	Growth Inhibition Assay			IC50=0.50 ± 0.10 μM	23443805
MFE280	Growth Inhibition Assay			IC50=0.42 ± 0.06 μM	23443805
LS174T	Growth Inhibition Assay			IC50=4.330.47 μM	24495750
CaCO2	Growth Inhibition Assay			IC50=3.230.64 μM	24495750
SW-480	Growth Inhibition Assay			IC50=4.330.47 μM	24495750
HT-29	Growth Inhibition Assay			IC50=5.21.93 μM	24495750
HCT-116	Growth Inhibition Assay			IC50=3.050.58 μM	24495750
RS4:11	Growth Inhibition Assay			IC50=2.81 μM	25202072
HB-1119	Growth Inhibition Assay			IC50=0.028 μM	25202072
SEM-K2	Growth Inhibition Assay			IC50=0.022 μM	25202072
Nalm-6	Growth Inhibition Assay			IC50=0.382 μM	25202072
CEM/C2	Growth Inhibition Assay			IC50=1.125 μM	25202072
CCRF-CEM	Growth Inhibition Assay			IC50=0.398 μM	25202072
BaF3-p210Bcr-Abl-T315I	Growth Inhibition Assay			IC50=2.626 μM	25202073
BaF3-p210Bcr-Abl	Growth Inhibition Assay			IC50=0.692 μM	25202073
BaF3-pSRα	Growth Inhibition Assay			IC50=0.668 μM	25202073
SupB15-R	Growth Inhibition Assay			IC50=0.558 μM	25202073
SupB15	Growth Inhibition Assay			IC50=0.449 μM	25202073
EFE184	Growth Inhibition Assay			IC50=2.04 ± 0.13 μM	23443805
ECC1	Growth Inhibition Assay			IC50=2.07 ± 0.01 μM	23443805
HEC1B	Growth Inhibition Assay			IC50=2.57 ± 0.23 μM	23443805
USPC1	Growth Inhibition Assay			IC50=2.60 ± 0.13 μM	23443805
SPAC1L	Growth Inhibition Assay			IC50=3.06 ± 1.14 μM	23443805
KM12L4A	Function assay			Inhibition of VEGFR2 phosphorylation expressed in human KM12L4A cells by Western blot analysis, EC50=0.046μM	19113866
KM12L4A	Function assay			Inhibition of PDGFRbeta phosphorylation expressed in human KM12L4A cells Western blot analysis, EC50=0.051μM	19113866
KM12L4A	Function assay			Inhibition of FGFR1 phosphorylation expressed in human KM12L4A cells by Western blot analysis, EC50=0.166μM	19113866
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
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生物活性

產(chǎn)品描述

特性

Dovitinib是MMRC的首要候選藥MMRC, 促進(jìn)多發(fā)性骨髓瘤藥物研究；MMRC是匯合領(lǐng)先學(xué)術(shù)機(jī)構(gòu)的非盈利機(jī)構(gòu)。

靶點(diǎn)

FLT3 ^[1] (Cell-free assay)	c-Kit ^[1] (Cell-free assay)	FGFR1 ^[1] (Cell-free assay)	VEGFR3/FLT4 ^[1] (Cell-free assay)	FGFR3 ^[1] (Cell-free assay)	點(diǎn)擊更多
1 nM	2 nM	8 nM	8 nM	9 nM	點(diǎn)擊更多

體外研究(In Vitro)
體外研究活性	Dovitinib有效抑制FGFR1/3和VEFFR1-2，IC50為8-13 nM。Dovitinib對(duì)InsR, EGFR, c-Met, EphrinA2, Tie2, IGFR1,和HER2抑制效果不大。Dovitinib作用于FGF刺激的野生型B9細(xì)胞和F384L突變型B9細(xì)胞的生長(zhǎng)顯示出強(qiáng)細(xì)胞毒性，IC50為25 nM。然而，Dovitinib作用于MINV突變型B9細(xì)胞顯示出低細(xì)胞毒性。Dovitinib抑制下游ERK1/2的磷酸化作用。^[1] Dovitinib作用于MV4;11 (FLT-3 ITD突變型)時(shí)比作用于RS4;11 (FLT-3野生型)顯示出更高的抗惡性細(xì)胞增生的能力。^[2] 另一方面，Dovitinib也選擇性地抑制FGFR1癌基因配體2-FGFR-陽(yáng)性的KG1和KG1A細(xì)胞系，這些細(xì)胞系有FGFR1癌基因配體2-FGFR１聚合基因。另外，Dovitinib抑制8p11骨髓增殖綜合征(EMS)病人的原代細(xì)胞生長(zhǎng)。^[3]
激酶實(shí)驗(yàn)	體外激酶實(shí)驗(yàn)
激酶實(shí)驗(yàn)	在體外研究時(shí)，Dovitinib溶解在DMSO中，濃度達(dá)到20mM,在實(shí)驗(yàn)使用前用培養(yǎng)基稀釋。FGFR3, FGFR1, PDGFR-β, 和VEGFR1-3的激酶域在含有如下物質(zhì)的混合物中測(cè)定?；旌衔锇?0 mM HEPES (pH 7.0), 2 mM MgCl₂, 10 mM MnCl₂，1 mM NaF, 1 mM DTT (二硫蘇糖醇), 1 mg/mL BSA (牛血清清蛋白), 0.25 μM 生物肽段基質(zhì)(GGGGQDGKDYIVLPI), 1到30 μM ATP (加量取決于酶的Km值)。測(cè)定c-KIT 和FLT3的反應(yīng)，調(diào)節(jié)PH到7.5，先加入0.25 到1 μM生物肽段基質(zhì)(GGLFDDPSYVNVQNL)，然后加入0.2到 8 μM ATP。反應(yīng)在室溫下溫育1到4小時(shí)，磷酸化的肽段移到含有封閉緩沖液(含25 mM EDTA和50 mM HEPES, pH 為7.5)，且包被鏈霉親和素的微量滴定板上。使用回歸曲線計(jì)算IC50值。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	B9細(xì)胞及多發(fā)性骨髓瘤細(xì)胞(Y373C, G384D, K650E，和J807C)
	濃度	400 nM 左右
	孵育時(shí)間	72小時(shí)
	方法	MTT實(shí)驗(yàn)測(cè)細(xì)胞活力，B9細(xì)胞及多發(fā)性骨髓瘤細(xì)胞按5x10³或20x10³密度接種在96孔板上。細(xì)胞加入30 ng/mL aFGF和100 µg/mL肝素或者1% IL-6 ,及Dovitinib 溫育72小時(shí)，然后測(cè)定細(xì)胞活力。
實(shí)驗(yàn)圖片	檢測(cè)方法	檢測(cè)指標(biāo)	實(shí)驗(yàn)圖片	PMID
	Western blot	CDK1 / p-CDK1 / p53 / p21 p-PDGFR-β / PDGFR-β / p-ERK / ERK p-VEGFR-2 / VEGFR-2 / p-FGFR-1 / FGFR-1 p-STAT3 / STAT3 / Mcl-1 / LC3 / Beclin 1 / p62		24238094
	Growth inhibition assay	Cell viability		28467797

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	在KMS-11移植鼠模型中，按鼠體重，每千克處理60 mg Dovitinib，導(dǎo)致FGFR3的衰退，結(jié)果腫瘤生長(zhǎng)抑制率達(dá)到94%。^[1] 在SCID-NOD 鼠中，Dovitinib作用于MV4;11腫瘤時(shí)顯示出強(qiáng)的抗癌活性。^[2] Dovitinib也有效抑制能激活FGFR3的KMS-11腫瘤。^[4]
動(dòng)物實(shí)驗(yàn)	Animal Models	右側(cè)腹皮下注射KMS-11細(xì)胞的雌性BNX 鼠
	Dosages	10, 30,或60 mg/kg
	Administration	飼喂處理

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05571969	Recruiting	Advanced Solid Tumors	Allarity Therapeutics\|Amarex Clinical Research	February 20 2023	Phase 1
NCT02268435	Withdrawn	Gastrointestinal Stromal Tumors	Asan Medical Center	March 2015	Phase 1
NCT01700270	Completed	Advanced Solid Tumors Excluding Breast Cancer	Novartis Pharmaceuticals\|Novartis	May 2013	Phase 1
NCT01680796	Withdrawn	Multiple Myeloma	University of Florida\|Novartis Pharmaceuticals	February 2013	Phase 1
NCT01266070	Terminated	Von Hippel-Lindau Syndrome	M.D. Anderson Cancer Center\|Novartis	November 2012	Phase 2

參考文獻(xiàn)
[1] Trudel S, et al. Blood. 2005, 105(7), 2941-2948. [2] Huynh H, et al. J Hepatol. 2012, 56(3), 595-601. [3] Lee SH, et al. Clin Cancer Res. 2005, 11(10), 3633-3641. [4] Azab AK, et al. Clin Cancer Res, 2011, 17(13), 4389-4399. [5] Trudel S, et al. Blood, 2005, 105(7), 2941-2948. + 展開(kāi)

參考文獻(xiàn)

[1] Trudel S, et al. Blood. 2005, 105(7), 2941-2948.
[2] Huynh H, et al. J Hepatol. 2012, 56(3), 595-601.
[3] Lee SH, et al. Clin Cancer Res. 2005, 11(10), 3633-3641.

[4] Azab AK, et al. Clin Cancer Res, 2011, 17(13), 4389-4399.
[5] Trudel S, et al. Blood, 2005, 105(7), 2941-2948.

+ 展開(kāi)

化學(xué)信息&溶解度

分子量	392.43	分子式	C₂₁H₂₁FN₆O
CAS號(hào)	405169-16-6	SDF	Download Dovitinib (TKI-258) SDF
Smiles	CN1CCN(CC1)C2=CC3=C(C=C2)N=C(N3)C4=C(C5=C(C=CC=C5F)NC4=O)N
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 30 mg/mL ( (76.44 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 40 mg/mL ( (101.92 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 34 mg/mL ( (86.63 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 37 mg/mL ( (94.28 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 26 mg/mL ( (66.25 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

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

動(dòng)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
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)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(qǐng)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(guò)該批次藥物DMSO溶解度，請(qǐng)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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* 必填項(xiàng)

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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Dovitinib (TKI-258)

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