Dovitinib | 度维替尼 | CHIR-258 | Multiple RTK Inhibitor

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多韦替尼 /Dovitinib {[allProObj[0].p_purity_real_show]}

货号：A325412 同义名： 度维替尼 / CHIR-258;TKI258

Dovitinib is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM.

Dovitinib 化学结构
CAS号：405169-16-6

Dovitinib 3D分子结构
CAS号：405169-16-6

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Dovitinib 纯度/质量文件产品仅供科研

货号：A325412 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

c-Kit 亚型比较
PDGFR 亚型比较
FGFR 亚型比较
FLT3 亚型比较
VEGFR 亚型比较

产品名称	c-Kit ↓ ↑	其他靶点	纯度
Tyrphostin AG1296	+ c-Kit (Swiss 3T3), IC50: 1.8 μM	PDGFR	99%+
Masitinib	+ Kit, IC50: 200 nM		99%+
Motesanib Diphosphate	+++ Kit, IC50: 8 nM		98%
Ki8751	++ c-Kit, IC50: 40 nM		98+%
Tivozanib	++ c-Kit, IC50: 78 nM		99%+
Pazopanib	+ c-Kit, IC50: 140 nM		99%
Sitravatinib	+++ Kit, IC50: 6 nM		99%+
Pexidartinib	+++ Kit, IC50: 10 nM		99%+
Lactate	++++ c-Kit, IC50: 2 nM	FLT3	85%
Amuvatinib	+++ c-Kit (D816H), IC50: 10 nM		99%+
Imatinib Mesylate	+ c-Kit, IC50: 100 nM	PDGFR	99%
AZD2932	+++ c-Kit, IC50: 9 nM		98%
Axitinib	++++ Kit, IC50: 1.7 nM		98%
Dovitinib	++++ c-Kit, IC50: 2 nM	FLT3	99%+
Sunitinib	✔	FLT3	98%
OSI-930	+ Kit, IC50: 80 nM		99%+
Telatinib	++++ c-Kit, IC50: 1 nM		99%+
Dasatinib monohydrate	++ c-Kit (D816V), IC50: 37 nM c-Kit (wt), IC50: 79 nM	Src	98%
Dasatinib	++ c-Kit (D816V), IC50: 37 nM c-Kit (wt), IC50: 79 nM	Src	98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	PDGFR ↓ ↑	PDGFRα ↓ ↑	PDGFRβ ↓ ↑	其他靶点	纯度
Tyrphostin A9	+ PDGFR, IC50: 0.5 μM			EGFR	98%
Tyrphostin AG1296					99%+
Motesanib Diphosphate	++ PDGFR, IC50: 84 nM				98%
Pazopanib	++ PDGFR, IC50: 84 nM				99%
Imatinib	+ PDGFR, IC50: 100 nM			c-Kit	98%
Imatinib Mesylate	+ PDGFR, IC50: 100 nM			c-Kit	99%
Sennoside B	✔				99%+
PP121	++++ PDGFR, IC50: 2 nM			mTOR,VEGFR	99%+
Crenolanib		++++ PDGFRα, Kd: 2.1 nM	++++ PDGFRβ, Kd: 3.2 nM		99%+
Masitinib		+ PDGFRα, IC50: 540 nM	+ PDGFRβ, IC50: 800 nM		99%+
Ki8751		++ PDGFRα, IC50: 67 nM		c-Kit	98+%
Tivozanib		++ PDGFRα, IC50: 40 nM	++ PDGFRβ, IC50: 49 nM		99%+
Ponatinib		++++ PDGFRα, IC50: 1.1 nM			98%
Amuvatinib		++ PDGFRα (V561D), IC50: 40 nM			99%+
Axitinib		+++ PDGFRα, IC50: 5.0 nM	++++ PDGFRβ, IC50: 1.6 nM		98%
CP-673451		+++ PDGFRα, IC50: 10 nM	++++ PDGFRβ, IC50: 1 nM		99%+
Telatinib		+++ PDGFRα, IC50: 15 nM		c-Kit	99%+
Nintedanib		++ PDGFRα, IC50: 59 nM	++ PDGFRβ, IC50: 65 nM		99+%
Avapritinib		++++ PDGFRα (D842V), IC50: 0.5 nM			99%+
MK-2461			+++ PDGFRβ, IC50: 22 nM		98%+
Lactate			+++ PDGFRβ, IC50: 27 nM	c-Kit,FLT3	85%
Linifanib			++ PDGFRβ, IC50: 66 nM		99%+
AZD2932			+++ PDGFRβ, IC50: 4 nM	c-Kit	98%
Dovitinib			+++ PDGFRβ, IC50: 27 nM	c-Kit,FLT3	99%+
Sorafenib			++ mPDGFRβ, IC50: 57 nM PDGFRβ, IC50: 57 nM		99%
Sunitinib			++++ PDGFRβ , IC50: 2 nM	FLT3	98%
Orantinib			+++ PDGFRβ, Ki: 8 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	FGFR ↓ ↑	FGFR1 ↓ ↑	FGFR2 ↓ ↑	FGFR3 ↓ ↑	FGFR4 ↓ ↑	其他靶点	纯度
Tyrphostin AG1296	+ FGFR (Swiss 3T3), IC50: 12.3 μM					PDGFR	99%+
Pazopanib	+ FGFR, IC50: 140 nM						99%
Erdafitinib	✔					RET	99%+
Gambogenic acid	✔						98+%
Sulfatinib		+++ FGFR1, IC50: 15 nM					99+%
Nintedanib esylate		+ FGFR1, IC50: 69 nM	++ FGFR2, IC50: 37 nM	+ FGFR3, IC50: 108 nM			98%
Zoligratinib		+++ FGFR1, IC50: 9.3 nM	+++ FGFR2, IC50: 7.6 nM	++ FGFR3, IC50: 22 nM	+ FGFR4, IC50: 290 nM		99%+
MK-2461		+ FGFR1, IC50: 65 nM	++ FGFR2, IC50: 39 nM	++ FGFR3, IC50: 50 nM			98%+
SU 5402		++ FGFR1, IC50: 30 nM					98%
Brivanib		+ FGFR1, IC50: 148 nM					99%+
Lucitanib		++ FGFR1, IC50: 17.5 nM	+ FGFR2, IC50: 82.5 nM				99%+
Ponatinib		++++ FGFR1, IC50: 2.2 nM					98%
PD-166866		+ FGFR1, IC50: 52.4 nM					98%
Narazaciclib		++ FGFR1, IC50: 26 nM				RET	99%+
Lactate		+++ FGFR1, IC50: 8 nM		+++ FGFR3, IC50: 9 nM		c-Kit,FLT3	85%
Lenvatinib mesylate		++ FGFR1, IC50: 46 nM				c-RET	99%
LY2874455		++++ FGFR1, IC50: 2.8 nM	++++ FGFR2, IC50: 2.6 nM	+++ FGFR3, IC50: 6.4 nM	+++ FGFR4, IC50: 6 nM		99%+
FIIN-2		+++ FGFR1, IC50: 3.09 nM	+++ FGFR2, IC50: 4.3 nM	++ FGFR3, IC50: 27 nM	++ FGFR4, IC50: 45.3 nM		98%
FIIN-3		+++ FGFR1, IC50: 13.1 nM	++ FGFR2, IC50: 21 nM	++ FGFR3, IC50: 31.4 nM	++ FGFR4, IC50: 35.3 nM		98%
Infigratinib		++++ FGFR1, IC50: 0.9 nM	++++ FGFR2, IC50: 1.4 nM	++++ FGFR3, IC50: 1.0 nM FGFR3 (K650E), IC50: 4.9 nM	+ FGFR4, IC50: 60 nM		99%+
Danusertib		++ FGFR1, IC50: 47 nM				RET	99%+
R1530		++ FGFR1, IC50: 28 nM					98%
ENMD-2076		+ FGFR1, IC50: 92.7 nM	+ FGFR2, IC50: 70.8 nM			RET,FLT3	98%
Dovitinib		+++ FGFR1, IC50: 8 nM		+++ FGFR3, IC50: 9 nM		c-Kit,FLT3	99%+
Sorafenib		+ FGFR1, IC50: 580 nM					99%
SSR128129E		+ FGFR1, IC50: 1.9 μM					99%+
AZD-4547		++++ FGFR1, IC50: 0.2 nM	++++ FGFR2, IC50: 2.5 nM	++++ FGFR3, IC50: 1.8 nM			98%
Lenvatinib		++ FGFR1, IC50: 46 nM				RET	98%
PD173074		++ FGFR1, IC50: ~25 nM					99%+
S49076		++ FGFR1, IC50: 18 nM	+++ FGFR2, IC50: 17 nM	+++ FGFR3, IC50: 15 nM			98%
Futibatinib		++++ FGFR1, IC50: 1.8 nM	++++ FGFR2, IC50: 1.4 nM	++++ FGFR3, IC50: 1.6 nM	+++ FGFR4, IC50: 3.7 nM		99%+
Ferulic Acid		+ FGFR1, IC50: 3.78 μM	+ FGFR2, IC50: 12.5 μM				98%
Nintedanib		+ FGFR1, IC50: 69 nM	++ FGFR2, IC50: 37 nM	+ FGFR3, IC50: 108 nM	+ FGFR4, IC50: 610 nM		99+%
ASP5878		++++ FGFR1, IC50: 0.47 nM	++++ FGFR2, IC50: 0.6 nM	++++ FGFR3, IC50: 0.74 nM	+++ FGFR4, IC50: 3.5 nM		98%
PRN1371		++++ FGFR1, IC50: 0.6 nM	++++ FGFR2, IC50: 1.3 nM	+++ FGFR3, IC50: 4.1 nM	++ FGFR4, IC50: 19.3 nM		99%
Derazantinib		+++ FGFR1, IC50: 4.5 nM	++++ FGFR2, IC50: 1.8 nM	+++ FGFR3, IC50: 4.5 nM	++ FGFR4, IC50: 34 nM	RET	99%+
ODM-203		+++ FGFR1, IC50: 11 nM	+++ FGFR2, IC50: 16 nM	+++ FGFR3, IC50: 6 nM	++ FGFR4, IC50: 35 nM		99%+
Pemigatinib		++++ FGFR1, IC50: 0.4 nM	++++ FGFR2, IC50: 0.5 nM	++++ FGFR3, IC50: 1.2 nM	++ FGFR4, IC50: 30 nM		99%+
SKLB 610			✔			PDGFR	99%+
Alofanib			✔				99%+
Lirafugratinib			✔				98%
Masitinib mesylate				✔		FAK	99%+
BLU9931				+ FGFR3, IC50: 150 nM	+++ FGFR4, IC50: 3 nM		99%+
BO-264				✔			99%+
Fisogatinib					+++ FGFR4, IC50: 5 nM		99%+
H3B-6527					++++ FGFR4, IC50: <1.2 nM		99%+
Roblitinib					++++ FGFR4, IC50: 1.9 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	FLT3 ↓ ↑	其他靶点	纯度
R406	✔	Syk	98%
Go6976	✔		99%+
Quizartinib	+++ FLT3 (WT), IC50: 4.2 nM FLT3 (ITD), IC50: 1.1 nM		98%
Gilteritinib	++++ FLT3, IC50: 0.29 nM		99%+
Amuvatinib	+ FLT3 (D835Y), IC50: 81 nM		99%+
Pacritinib	++ FLT3 (D835Y), IC50: 6 nM FLT3, IC50: 22 nM		97%
Dovitinib	++++ FLT3, IC50: 1 nM	c-Kit	99%+
Denfivontinib	++++ FLT3 (D835Y), IC50: 0.4 nM FLT3, IC50: 0.4 nM	RET	99%+
TAK-659 HCl	++ FLT3, IC50: 4.6 nM	Syk	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	VEGFR1 ↓ ↑	VEGFR2 ↓ ↑	VEGFR3 ↓ ↑	其他靶点	纯度
Motesanib Diphosphate	++++ VEGFR1, IC50: 2 nM	++++ VEGFR2/Flk1, IC50: 3 nM VEGFR2, IC50: 3 nM	+++ VEGFR3, IC50: 6 nM	RET,PDGFR	98%
Tivozanib	++ VEGFR1, IC50: 30 nM	+++ VEGFR2, IC50: 6.5 nM	++ VEGFR3, IC50: 15 nM		99%+
Brivanib	+ VEGFR1, IC50: 380 nM	++ Flk1, IC50: 25 nM VEGFR2, IC50: 25 nM			99%+
Regorafenib	+++ VEGFR1, IC50: 13 nM	+++ VEGFR2, IC50: 4.2 nM	+ VEGFR3, IC50: 46 nM	RET	98%
Pazopanib	+++ VEGFR1, IC50: 10 nM	++ VEGFR2, IC50: 30 nM	+ VEGFR3, IC50: 47 nM	FGFR,c-Kit,PDGFR	99%
Sitravatinib	+++ VEGFR1 (FLT1), IC50: 6 nM	+++ VEGFR2 (KDR), IC50: 5 nM	++++ VEGFR3 (FLT4), IC50: 2 nM		99%+
Foretinib	+++ VEGFR1/FLT1, IC50: 6.8 nM	++++ KDR, IC50: 0.86 nM	++++ VEGFR3/FLT4, IC50: 2.8 nM	Tie-2	99%+
MGCD-265 analog	++++ VEGFR1, IC50: 3 nM	++++ VEGFR2, IC50: 3 nM	++++ VEGFR3, IC50: 4 nM	Tie-2	99%+
Lactate	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	c-Kit,FLT3	85%
AEE788	+ FLT1, IC50: 59 nM	+ KDR, IC50: 77 nM		EGFR	98+%
Linifanib	++++ VEGFR1/FLT1, IC50: 3 nM	++++ VEGFR2/KDR, IC50: 4 nM	+ VEGFR3/FLT4, IC50: 190 nM	FLT3	99%+
Vatalanib 2HCl	+ VEGFR1/FLT1, IC50: 77 nM	++ VEGFR2/KDR, IC50: 37 nM VEGFR2/Flk1, IC50: 270 nM	+ VEGFR3/FLT4, IC50: 660 nM	c-Kit,c-Fms	99%+
Axitinib	++++ VEGFR1/FLT1, IC50: 0.1 nM	++++ VEGFR2/KDR, IC50: 0.2 nM VEGFR2/Flk1, IC50: 0.18 nM			98%
Dovitinib	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	c-Kit,FLT3	99%+
ZM 306416	+ VEGFR1, IC50: 0.33 μM			Src	99%+
KRN-633	+ VEGFR1, IC50: 170 nM	+ VEGFR2, IC50: 160 nM	+ VEGFR3, IC50: 125 nM	c-Kit,BTK	98%
OSI-930	+++ FLT1, IC50: 8 nM	+++ KDR, IC50: 9 nM			99%+
Lenvatinib	++ VEGFR1/FLT1, IC50: 22 nM	++++ VEGFR2/KDR, IC50: 4.0 nM	+++ VEGFR3/FLT4, IC50: 5.2 nM		98%
NVP-BAW2881	+ hVEGFR1, IC50: 820 nM	+++ mVEGF2, IC50: 165 nM hVEGFR2, IC50: 9 nM	+ hVEGFR3, IC50: 420 nM		98%
Cediranib	+++ VEGFR1/FLT1, IC50: 5 nM	++++ VEGFR2/KDR, IC50: 0.5 nM		c-Kit	99%+
Nintedanib	++ VEGFR1, IC50: 34 nM	+++ VEGFR2, IC50: 13 nM	+++ VEGFR3, IC50: 13 nM	FLT3	99+%
BMS-794833		++ VEGFR2, IC50: 15 nM			99%+
SKLB1002		++ VEGFR2, IC50: 32 nM			98%
Cabozantinib S-malate		++++ VEGFR2/KDR, IC50: 0.035 nM			99+%
Ki8751		++++ VEGFR2, IC50: 0.9 nM		c-Kit	98+%
SU 5402		++ VEGFR2, IC50: 20 nM			98%
Rivoceranib Mesylate		++++ VEGFR2, IC50: 1 nM		RET	98+%
Ponatinib		++++ VEGFR2, IC50: 1.5 nM			98%
LY2874455		+++ VEGFR2, IC50: 7 nM			99%+
ZM323881 HCl		++++ VEGFR2, IC50: <2 nM			98%
AZD2932		+++ VEGFR-2, IC50: 8 nM		c-Kit	98%
Cabozantinib		++++ VEGFR2/KDR, IC50: 0.035 nM			98%
Sorafenib		++ VEGFR2/Flk1, IC50: 90 nM VEGFR2, IC50: 90 nM			99%
CYC-116		++ VEGFR2, Ki: 44 nM		FLT3	99%+
Golvatinib		++ VEGFR2, IC50: 16 nM			99%+
Sunitinib		+ VEGFR2 , IC50: 80 nM		FLT3	98%
RAF265		++ VEGFR2, EC50: 30 nM			99%+
PD173074					99%+
BFH772		++++ VEGFR2, IC50: 3 nM			98%
Semaxinib		+ VEGFR2/Flk1, IC50: 1.23 μM			98%
Vandetanib		++ VEGFR2, IC50: 40 nM	+ VEGFR3, IC50: 110 nM	EGFR	98%
SAR131675			++ VEGFR3, IC50: 23 nM		99%+
ENMD-2076		+ VEGFR2/KDR, IC50: 58.2 nM	++ VEGFR3/FLT4, IC50: 15.9 nM	RET,FLT3	98%
Telatinib		+++ VEGFR2, IC50: 6 nM	++++ VEGFR3, IC50: 4 nM	c-Kit	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Dovitinib 生物活性

靶点

VEGFR1

VEGFR1/FLT1, IC50:10 nM
VEGFR3

VEGFR3/FLT4, IC50:8 nM
VEGFR2

VEGFR2/Flk1, IC50:13 nM
PDGFRβ

PDGFRβ, IC50:27 nM

描述

Receptor tyrosine kinases (RTK) are mediators of cellular proliferation. These transmembrane RTKs contain an extracellular domain for ligand binding and intracellular kinase domains that mediate autophosphorylation, recruitment of downstream signaling molecules, and signal transduction. Type III RTKs, such as PDGFR (platelet-derived growth factor receptor), FGFR (fibroblast growth factor receptor), VEGFR (vascular endothelial growth factor receptor), FLT3 and c-KIT are often overexpressed in tumor and implicated in tumor growth and progression^[3]. Tandutinib is an inhibitor of FLT3, PDGFR and c-Kit. The kinase inhibitory IC₅₀s were 0.22, 0.20 and 0.17 μM, respectively. Tandutinib inhibited phosphorylation of WT FLT3 and FLT3-ITD (internal tandem duplication) in Ba/F3 cells with IC₅₀s of 30-100nM. Tandutinib inhibited cell proliferation of the FLT3-ITD-positive cells (Molm-13 and Molm-14 cells） with an IC₅₀ value of 10 nM, whereas the FLT3-ITD-negative cells (THP-1, KG-1, and RS4 cells) were resistant, requiring 1000-fold higher concentrations to inhibit cell growth. Treatment of Molm-14 cells with 1 μM tandutinib resulted in an increase of the percentage of apoptotic cells from a background level of 5% to 51% at 24h and 78% at 96h^[6]. Tandutinib preferentially inhibited the growth of blast colonies derived from FLT3 ITD-positive patients with IC₅₀s between 75 and 400 nM^[7]. In a nude mice model established by injection of FLT3-ITD-transformed Ba/F3 cells, oral administration of tandutinib at 60 mg/kg bid significantly increased the survival of mice and resulted in a significant reduction in mortality in a mouse bone marrow transplantation model^[6].

Dovitinib 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
5637	1-10 μM	Cell Viability Assay	72 h	inhibits cell growth in a dose dependent manner	24325461
8226		Growth Inhibition Assay	72 h	IC50> 2500 nM	15598814
97-7		Growth Inhibition Assay	5 d	IC50=1000 nM	21119661
97-7	500 nM	Function Assay	24 h	increases the proportion of cells in G1 accompanied by a decrease in S and G2/M phases	21119661

Dovitinib 参考文献

[1]Huynh H, Chow PK, et al. Dovitinib demonstrates antitumor and antimetastatic activities in xenograft models of hepatocellular carcinoma. J Hepatol. 2012 Mar;56(3):595-601.

[2]Huynh H, Chow PK, et al. Dovitinib demonstrates antitumor and antimetastatic activities in xenograft models of hepatocellular carcinoma. J Hepatol. 2012 Mar;56(3):595-601.

[3]Lee SH, Lopes de Menezes D, Vora J, Harris A, Ye H, Nordahl L, Garrett E, Samara E, Aukerman SL, Gelb AB, Heise C. In vivo target modulation and biological activity of CHIR-258, a multitargeted growth factor receptor kinase inhibitor, in colon cancer models. Clin Cancer Res. 2005 May 15;11(10):3633-41. doi: 10.1158/1078-0432.CCR-04-2129. PMID: 15897558.

[4]Trudel S, Li ZH, Wei E, Wiesmann M, Chang H, Chen C, Reece D, Heise C, Stewart AK. CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood. 2005 Apr 1;105(7):2941-8.

[5]Eucker J, Zang C, Zhou Y, Li X, Habbel P, Schulz CO, Scholz C, Liu H. TKI258, a multi-tyrosine kinase inhibitor is efficacious against human infant/childhood lymphoblastic leukemia in vitro. Anticancer Res. 2014 Sep;34(9):4899-907.

[6]Kelly LM, Yu JC, Boulton CL, Apatira M, Li J, Sullivan CM, Williams I, Amaral SM, Curley DP, Duclos N, Neuberg D, Scarborough RM, Pandey A, Hollenbach S, Abe K, Lokker NA, Gilliland DG, Giese NA. CT53518, a novel selective FLT3 antagonist for the treatment of acute myelogenous leukemia (AML). Cancer Cell. 2002 Jun;1(5):421-32. doi: 10.1016/s1535-6108(02)00070-3. PMID: 12124172.

[7]Griswold IJ, Shen LJ, La Rosée P, Demehri S, Heinrich MC, Braziel RM, McGreevey L, Haley AD, Giese N, Druker BJ, Deininger MW. Effects of MLN518, a dual FLT3 and KIT inhibitor, on normal and malignant hematopoiesis. Blood. 2004 Nov 1;104(9):2912-8. doi: 10.1182/blood-2003-05-1669. Epub 2004 Jul 8. PMID: 15242881.

Dovitinib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.55mL

0.51mL

0.25mL

12.74mL

2.55mL

1.27mL

25.48mL

5.10mL

2.55mL

Dovitinib 技术信息

CAS号	405169-16-6
分子式	C₂₁H₂₁FN₆O
分子量	392.43

别名	度维替尼 ;CHIR-258;TKI258
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 25 mg/mL(63.71 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 1 mg/mL clear

PO 0.5% CMC-Na 40 mg/mL suspension

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

5637	1-10 μM	Cell Viability Assay	72 h	inhibits cell growth in a dose dependent manner	24325461
8226		Growth Inhibition Assay	72 h	IC50> 2500 nM	15598814
97-7		Growth Inhibition Assay	5 d	IC50=1000 nM	21119661
97-7	500 nM	Function Assay	24 h	increases the proportion of cells in G1 accompanied by a decrease in S and G2/M phases	21119661
AN3CA	0.05/0.1/0.5 μM	Function Assay	72 h	causes a decrease in STAT3, ERK, and AKT phosphorylation	24495750
AN3CA		Growth Inhibition Assay		IC50=0.50 ± 0.10 μM	23443805
BaF3-p210Bcr-Abl		Growth Inhibition Assay		IC50=0.692 μM	25202073
BaF3-p210Bcr-Abl-T315I		Growth Inhibition Assay		IC50=2.626 μM	25202073
BaF3-pSRα		Growth Inhibition Assay		IC50=0.668 μM	25202073
BFTC905	1-10 μM	Cell Viability Assay	72 h	inhibits cell growth in a dose dependent manner	24325461
C666-1	0.1-10 μM	Growth Inhibition Assay	48 h	induces G2/M delay in a concentration-dependent manner	24238094
CaCO2		Growth Inhibition Assay		IC50=3.230.64 μM	24495750
CCRF-CEM		Growth Inhibition Assay		IC50=0.398 μM	25202072
CEM/C2		Growth Inhibition Assay		IC50=1.125 μM	25202072
CNE2	0.1-10 μM	Growth Inhibition Assay	48 h	induces G2/M delay in a concentration-dependent manner	24238094
ECC1		Growth Inhibition Assay		IC50=2.07 ± 0.01 μM	23443805
EFE184		Growth Inhibition Assay		IC50=2.04 ± 0.13 μM	23443805
EN		Growth Inhibition Assay		IC50=1.66 ± 0.01 μM	23443805
EN1		Growth Inhibition Assay		IC50=1.02 ± 0.25 μM	23443805
F384L	0-400 nM	Cell Viability Assay	48 h	inhibits cell growth in a dose dependent manner	15598814
G384D	0-400 nM	Cell Viability Assay	48 h	inhibits cell growth in a dose dependent manner	15598814
H929		Growth Inhibition Assay	72 h	IC50> 2500 nM	15598814
HB-1119		Growth Inhibition Assay		IC50=0.028 μM	25202072
HCT-116		Growth Inhibition Assay		IC50=3.050.58 μM	24495750
HEC155		Growth Inhibition Assay		IC50=0.66 ± 0.09 μM	23443805
HEC1A		Growth Inhibition Assay		IC50=1.34 ± 0.30 μM	23443805
HEC-1A	0.05/0.1/0.5 μM	Function Assay	72 h	causes a decrease in STAT3, ERK, and AKT phosphorylation	24495750
HEC1B		Growth Inhibition Assay		IC50=2.57 ± 0.23 μM	23443805
HeLa	0.1-10 μM	Growth Inhibition Assay	24 h	induces G2/M arrest in a concentration-dependent manner	24238094
Hep3B	0.1-10 μM	Growth Inhibition Assay	24 h	induces G2 arrest	24238094
Hep3B		Growth Inhibition Assay	48 h	IC50=4.223 ± 0.839 μM	23546591
Hep3B		Growth Inhibition Assay	72 h	IC50=0.892 ± 0.044 μM	23546591
Hep3B	0-12.5 μM	Apoptosis Assay	24 h	sensitizes HCC cells to TRAIL- and tigatuzumab-induced apoptosis in a dose-dependent manner	22230479
Hep3B	0-15 μM	Cell Viability Assay	72 h	reduces cell viability in a dose-dependent manner	22180308
Hep3B	0-15 μM	Apoptosis Assay	24 h	increases apoptotic cell death in a dose-dependent manner	22180308
Hep3B	0-10 μM	Function Assay	24 h	causes dose-dependent DNA fragmentation	22180308
HepG2		Growth Inhibition Assay	48 h	IC50=2.727 ± 0.429 μM	23546591
HepG2		Growth Inhibition Assay	72 h	IC50=1.200 ± 0.226 μM	23546591
HMVEC	0-25 μM	Cell Viability Assay	72 h	inhibits cell growth in a dose dependent manner	23228017
HNE1	0.1-10 μM	Growth Inhibition Assay	48 h	induces G2/M delay in a concentration-dependent manner	24238094
HONE1	0.1-10 μM	Growth Inhibition Assay	48 h	induces G2/M delay in a concentration-dependent manner	24238094
HT1376	1-10 μM	Cell Viability Assay	72 h	inhibits cell growth in a dose dependent manner	24325461
HT-29		Growth Inhibition Assay		IC50=5.21.93 μM	24495750
HU456	1-10 μM	Cell Viability Assay	72 h	inhibits cell growth in a dose dependent manner	24325461
Huh7		Growth Inhibition Assay	48 h	IC50=15.007 ± 7.334 μM	23546591
Huh7		Growth Inhibition Assay	72 h	IC50=3.980 ± 0.803 μM	23546591
Huh-7	0-12.5 μM	Apoptosis Assay	24 h	sensitizes HCC cells to TRAIL- and tigatuzumab-induced apoptosis in a dose-dependent manner	22230479
Huh-7	0-15 μM	Cell Viability Assay	72 h	reduces cell viability in a dose-dependent manner	22180308
Huh-7	0-15 μM	Apoptosis Assay	24 h	increases apoptotic cell death in a dose-dependent manner	22180308
Huh-7	0-10 μM	Function Assay	24 h	causes dose-dependent DNA fragmentation	22180308
HUVEC	0-25 μM	Cell Viability Assay	72 h	inhibits cell growth in a dose dependent manner	23228017
ISHIKAWA		Growth Inhibition Assay		IC50=1.30 ± 0.11 μM	23443805
J807C	0-400 nM	Cell Viability Assay	48 h	inhibits cell growth in a dose dependent manner	15598814
J82		Growth Inhibition Assay	5 d	IC50=1400 nM	21119661
JMSU1		Growth Inhibition Assay	5 d	IC50=50 nM	21119661
K650E	0-400 nM	Cell Viability Assay	48 h	inhibits cell growth in a dose dependent manner	15598814
KLE		Growth Inhibition Assay		IC50=1.37 ± 0.02 μM	23443805
KMS11		Growth Inhibition Assay	72 h	IC50=90 nM	15598814
KMS18		Growth Inhibition Assay	72 h	IC50=550 nM	15598814
LS174T		Growth Inhibition Assay		IC50=4.330.47 μM	24495750
MFE280		Growth Inhibition Assay		IC50=0.42 ± 0.06 μM	23443805
MFE296		Growth Inhibition Assay		IC50=0.66 ± 0.19 μM	23443805
MFE-296	0.05/0.1/0.5 μM	Function Assay	72 h	causes a decrease in STAT3, ERK, and AKT phosphorylation	24495750
MFE319		Growth Inhibition Assay		IC50=1.87 ± 0.45 μM	23443805
MGH-U3	500 nM	Function Assay	24 h	increases the proportion of cells in G1 accompanied by a decrease in S and G2/M phases	21119661
MGHU4	1-10 μM	Cell Viability Assay	72 h	inhibits cell growth in a dose dependent manner	24325461
MHCC-97H	0-25 μM	Cell Viability Assay	72 h	inhibits cell growth in a dose dependent manner	23228017
Nalm-6		Growth Inhibition Assay		IC50=0.382 μM	25202072
Nalm-6	2 μM	Apoptosis Assay	24/48 h	induces apoptosis resulting in about 72% of cell death after 24 h treatment and 81% after 48 h	25202072
OPM2		Growth Inhibition Assay	72 h	IC50=90 nM	15598814
PLC/PRF5		Growth Inhibition Assay	48 h	IC50=16.120 ± 4.001 μM	23546591
PLC/PRF5		Growth Inhibition Assay	72 h	IC50=3.110 ± 0.337 μM	23546591
PLC5	0-12.5 μM	Apoptosis Assay	24 h	sensitizes HCC cells to TRAIL- and tigatuzumab-induced apoptosis in a dose-dependent manner	22230479
PLC5	0-15 μM	Cell Viability Assay	72 h	reduces cell viability in a dose-dependent manner	22180308
PLC5	0-15 μM	Apoptosis Assay	24 h	increases apoptotic cell death in a dose-dependent manner	22180308
PLC5	0-10 μM	Function Assay	24 h	causes dose-dependent DNA fragmentation	22180308
RL952		Growth Inhibition Assay		IC50=0.93 ± 0.01 μM	23443805
RS4:11		Growth Inhibition Assay		IC50=2.81 μM	25202072
RT112	1-10 μM	Cell Viability Assay	72 h	inhibits cell growth in a dose dependent manner	24325461
RT112		Growth Inhibition Assay	5 d	IC50=15 nM	21119661
RT112	500 nM	Function Assay	24 h	increases the proportion of cells in G1 accompanied by a decrease in S and G2/M phases	21119661
RT4	1-10 μM	Cell Viability Assay	72 h	inhibits cell growth in a dose dependent manner	24325461
RT4		Growth Inhibition Assay	5 d	IC50=5 nM	21119661
RT4	500 nM	Function Assay	24 h	increases the proportion of cells in G1 accompanied by a decrease in S and G2/M phases	21119661
SEM-K2		Growth Inhibition Assay		IC50=0.022 μM	25202072
SEM-K2	0.1/1 μM	Apoptosis Assay	24 h	induces early apoptosis of SEM-K2 cells at 0.1 μM after 24 h	25202072
Sk-Hep1	0-12.5 μM	Apoptosis Assay	24 h	sensitizes HCC cells to TRAIL- and tigatuzumab-induced apoptosis in a dose-dependent manner	22230479
Sk-Hep1	0-15 μM	Cell Viability Assay	72 h	reduces cell viability in a dose-dependent manner	22180308
Sk-Hep1	0-15 μM	Apoptosis Assay	24 h	increases apoptotic cell death in a dose-dependent manner	22180308
Sk-Hep1	0-10 μM	Function Assay	24 h	causes dose-dependent DNA fragmentation	22180308
SMMC7721	0-25 μM	Cell Viability Assay	72 h	inhibits cell growth in a dose dependent manner	23228017
SNGII		Growth Inhibition Assay		IC50=1.24 ± 0.28 μM	23443805
SNGM		Growth Inhibition Assay		IC50=1.42 ± 0.13 μM	23443805
SPAC1L		Growth Inhibition Assay		IC50=3.06 ± 1.14 μM	23443805
SPAC1S		Growth Inhibition Assay		IC50=0.77 ± 0.08 μM	23443805
SupB15		Growth Inhibition Assay		IC50=0.449 μM	25202073
SupB15-R		Growth Inhibition Assay		IC50=0.558 μM	25202073
SW-480		Growth Inhibition Assay		IC50=4.330.47 μM	24495750
SW780		Growth Inhibition Assay	5 d	IC50=50 nM	21119661
SW780	500 nM	Function Assay	24 h	increases the proportion of cells in G1 accompanied by a decrease in S and G2/M phases	21119661
T24	1-10 μM	Cell Viability Assay	72 h	inhibits cell growth in a dose dependent manner	24325461
TCC-SUP	1-10 μM	Cell Viability Assay	72 h	inhibits cell growth in a dose dependent manner	24325461
U266		Growth Inhibition Assay	72 h	IC50> 2500 nM	15598814
UMC3	1-10 μM	Cell Viability Assay	72 h	inhibits cell growth in a dose dependent manner	24325461
USPC1		Growth Inhibition Assay		IC50=2.60 ± 0.13 μM	23443805
USPC2		Growth Inhibition Assay		IC50=1.62 ± 0.01 μM	23443805
Y373C	0-400 nM	Cell Viability Assay	48 h	inhibits cell growth in a dose dependent manner	15598814

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VEGFR1	VEGFR1/FLT1, IC50:10 nM
VEGFR3	VEGFR3/FLT4, IC50:8 nM
VEGFR2	VEGFR2/Flk1, IC50:13 nM
PDGFRβ	PDGFRβ, IC50:27 nM
FGFR3	FGFR3, IC50:9 nM
FGFR1	FGFR1, IC50:8 nM
c-Kit	c-Kit, IC50:2 nM
FLT3	FLT3, IC50:1 nM

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