Dovitinib (Synonyms: 多韦替尼; CHIR-258; TKI258)

目录号: HY-50905 纯度: 99.88%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Dovitinib (CHIR-258) 是口服有效的、多靶点的酪氨酸激酶 (RTK) 抑制剂，抑制 FLT3，c-Kit，CSF-1R，FGFR1/FGFR3，VEGFR1/VEGFR2/VEGFR3 和 PDGFRα/PDGFRβ 的 IC₅₀ 值分别为 1，2，36，8/9，10/13/8，27/210 nM。Dovitinib 具有抗肿瘤活性。

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Dovitinib Chemical Structure

CAS No. : 405169-16-6

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥550	In-stock
1 mg	￥200	In-stock
5 mg	￥500	In-stock
10 mg	￥800	In-stock
25 mg	￥1600	In-stock
50 mg	￥2600	In-stock
100 mg	￥4200	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Dovitinib:

MCE 顾客使用本产品发表的 8 篇科研文献

: Dovitinib purchased from MCE. Usage Cited in: Front Cell Dev Biol. 2020 May 7;8:287. [Abstract]; Determination in L3.6 cells of FGF2-induced FGFR phosphorylation by Western blot in the presence of Dovitinib. FGFR1 and alpha-Tubulin are used as loading controls.

: Dovitinib purchased from MCE. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278. [Abstract]; BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM) with the indicated antagonist of RTKs (Dovitinib at 1 µM, Gefinitib at 2.5 µM, Sunitinib at 2.5 µM and LDC1267 at 1 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 12 h.

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生物活性
纯度 & 产品资料
参考文献

生物活性

Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC₅₀s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity^[1]^[2].

IC₅₀ & Target^[1]

FLT3

1 nM (IC₅₀)

c-Kit

2 nM (IC₅₀)

FGFR1

8 nM (IC₅₀)

FGFR3

9 nM (IC₅₀)

VEGFR3

8 nM (IC₅₀)

VEGFR1

10 nM (IC₅₀)

VEGFR2

13 nM (IC₅₀)

PDGFRβ

27 nM (IC₅₀)

PDGFRα

210 nM (IC₅₀)

CSF-1R

36 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HL-60	IC₅₀	0.911 μM Compound: Dovitinib	Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
K562	IC₅₀	2.018 μM Compound: Dovitinib	Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
KCL-22	IC₅₀	2.552 μM Compound: Dovitinib	Antiproliferative activity against human KCL-22 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human KCL-22 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
KG-1	IC₅₀	0.035 μM Compound: Dovitinib	Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
KG-1a	IC₅₀	0.033 μM Compound: Dovitinib	Antiproliferative activity against human KG-1a cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human KG-1a cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
MOLM-13	IC₅₀	0.005 μM Compound: Dovitinib	Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
MOLM-13	IC₅₀	794.7 nM Compound: DOV	Antiproliferative activity against human MOLM-13 cells incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human MOLM-13 cells incubated for 48 hrs by CCK-8 assay	[PMID: 34694800]
MOLT-4	IC₅₀	0.266 μM Compound: Dovitinib	Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
MV4-11	IC₅₀	0.004 μM Compound: Dovitinib	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
MV4-11	IC₅₀	184.5 nM Compound: DOV	Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by CCK-8 assay	[PMID: 34694800]
NOMO-1	IC₅₀	1.493 μM Compound: Dovitinib	Antiproliferative activity against human NOMO-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human NOMO-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
OCI-AML2	IC₅₀	0.568 μM Compound: Dovitinib	Antiproliferative activity against human OCI-AML2 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human OCI-AML2 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
THP-1	IC₅₀	1.936 μM Compound: Dovitinib	Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]

体外研究
(In Vitro)

Dovitinib (CHIR-258) shows more than 10-fold inhibition InsR (IC50=2 μM), EGFR1 (IC50=2 μM), c-Met (IC50>3 μM), EphrinA2 (EphA2; IC50=4 μM), Tie2 (IC50=4 μM), IGFR1 (IC50>10 μM), and HER2 (IC50>10 μM)^[1].
Dovitinib (12.5-400 nM; 48 hours) potently inhibits the FGF-stimulated growth of WT and F384L-FGFR3-expressing B9 cells with IC50 values of 25 nM^[1].
Dovitinib (100, 500 nM; 96 hours) inhibits FGF-mediated ERK1/2 phosphorylation and induces apoptosis of FGFR3-expressing human myeloma cell lines^[1].
Dovitinib (72 hours) inhibits cell proliferation of KMS11 (FGFR3-Y373C), OPM2 (FGFR3-K650E), and KMS18 (FGFR3-G384D) cells with IC50 of values of 90 nM (KMS11 and OPM2) and 550 nM, respectively^[1].
Dovitinib (100 nM) augments Dexamethasone (0.5 μM) cytotoxicity in KMS11 cells^[1].
Dovitinib significantly reduces the basal phosphorylation levels of FGFR-1, FGFR substrate 2α (FRS2-α) and ERK1/2 but not Akt in both SK-HEP1 and 21-0208 cells^[2].
Dovitinib enhances the BMP-2-induced alkaline phosphatase (ALP) induction, which is a representative marker of osteoblast differentiation. Dovitinib also stimulates the translocation of phosphorylated Smad1/5/8 into the nucleus and phosphorylation of mitogen-activated protein kinases, including ERK1/2 and p38^[3].
Dovitinib strongly inhibits both the interaction of TNIK with ATP (K_i, 13 nM) and the activation of Wnt signaling effectors such as β-catenin and TCF4. Dovitinib also induces caspase-dependent apoptosis in IM-9 cells without significant cytotoxicity in PBMCs^[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:	WT and F384L-FGFR3-expressing B9 cells
Concentration:	12.5, 25, 50, 100, 200, 300, 400 nM
Incubation Time:	48 hours
Result:	Potently inhibited the FGF-stimulated growth of the cells.

Apoptosis Analysis^[1]

Cell Line:	KMS11, OPM2, and KMS18 cells
Concentration:	100 nM or 500 nM
Incubation Time:	96 hours
Result:	Induced apoptosis of FGFR3-expressing human myeloma cell lines.

体内研究
(In Vivo)

Dovitinib (CHIR-258; 10-60 mg/kg/day; gavage; for 21 days) has a significant antitumor effect^[1].
Dovitinib (50 and 75 mg/kg) results in 97% and 98% tumor growth inhibition, respectively, and the maximal efficacy is at 50 mg/kg^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	6- to 8-week-old female BNX mice with KMS11 cells^[1]
Dosage:	10, 30, 60 mg/kg
Administration:	Gavage; daily for 21 days
Result:	Had a significant antitumor effect in all 3 dose groups with 48%, 78.5%, and 94% growth inhibition in the 10 mg/kg, 30 mg/kg, and 60 mg/kg treatment.

Clinical Trial

分子量

392.43

Formula

C₂₁H₂₁FN₆O

CAS 号

405169-16-6

性状

固体

颜色

Light yellow to green yellow

中文名称

多韦替尼；度维替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : 23.33 mg/mL (59.45 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5482 mL	12.7411 mL	25.4823 mL
5 mM	0.5096 mL	2.5482 mL	5.0965 mL
10 mM	0.2548 mL	1.2741 mL	2.5482 mL

查看完整储备液配制表

* 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°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.37 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.37 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.37 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.88%

选择批次：

Data Sheet (633 KB) SDS (393 KB)

COA (285 KB) LCMS (106 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Trudel S, et al. CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood. 2005, 105(7), 2941-2948. [Content Brief]

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

[3]. Lee Y, et al. A Receptor Tyrosine Kinase Inhibitor, Dovitinib (TKI-258), Enhances BMP-2-Induced Osteoblast Differentiation In Vitro. Mol Cells. 2016 May 31;39(5):389-94 [Content Brief]

[4]. Chon HJ, et al. Traf2- and Nck-interacting kinase (TNIK) is involved in the anti-cancer mechanism of dovitinib in human multiple myeloma IM-9 cells. Amino Acids. 2016 Jul;48(7):1591-9. [Content Brief]

Dovitinib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5482 mL	12.7411 mL	25.4823 mL	63.7056 mL
	5 mM	0.5096 mL	2.5482 mL	5.0965 mL	12.7411 mL
	10 mM	0.2548 mL	1.2741 mL	2.5482 mL	6.3706 mL
	15 mM	0.1699 mL	0.8494 mL	1.6988 mL	4.2470 mL
	20 mM	0.1274 mL	0.6371 mL	1.2741 mL	3.1853 mL
	25 mM	0.1019 mL	0.5096 mL	1.0193 mL	2.5482 mL
	30 mM	0.0849 mL	0.4247 mL	0.8494 mL	2.1235 mL
	40 mM	0.0637 mL	0.3185 mL	0.6371 mL	1.5926 mL
	50 mM	0.0510 mL	0.2548 mL	0.5096 mL	1.2741 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Dovitinib (Synonyms: 多韦替尼; CHIR-258; TKI258)

Customer Review

Other Forms of Dovitinib:

MCE 顾客使用本产品发表的 8 篇科研文献

Dovitinib 相关产品

•相关化合物库:

•同靶点产品:

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查看 FGFR 亚型特异性产品:

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生物活性

纯度 & 产品资料

参考文献

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Dovitinib (Synonyms: 多韦替尼; CHIR-258; TKI258)

Customer Review

Other Forms of Dovitinib:

Dovitinib 相关抗体

MCE 顾客使用本产品发表的 8 篇科研文献

Dovitinib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 FGFR 亚型特异性产品:

查看 VEGFR 亚型特异性产品:

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生物活性

纯度 & 产品资料

参考文献

Dovitinib 相关抗体:

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Dovitinib 相关分类

完整储备液配制表

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