Dovitinib lactate (Synonyms: CHIR-258 lactate; TKI-258 lactate)

Name: Dovitinib lactate
Brand: MedChemExpress
SKU: HY-10207
Rating: 5.0 (11 reviews)

Cat. No.: HY-10207 Purity: 99.75%: Data Sheet
COA

SDS
Handling Instructions
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Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC₅₀s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No. : 692737-80-7

사이즈	재고	수량

무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	해외재고보유	Estimated Time of Arrival: December 31
250 mg	해외재고보유	Estimated Time of Arrival: December 31
500 mg	해외재고보유	Estimated Time of Arrival: December 31
1 g	견적 받기
5 g	견적 받기

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 11 publication(s) in Google Scholar

Other Forms of Dovitinib lactate:

Dovitinib In-stock
Dovitinib dilactic acid 견적 받기
Dovitinib lactate hydrate 견적 받기
Dovitinib lactate (Standard) 견적 받기

11 Publications Citing Use of MCE Dovitinib lactate

: Dovitinib lactate purchased from MedChemExpress. 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 lactate purchased from MedChemExpress. 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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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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PDGFR PDGFRβ PDGFRα

Biological Activity
Protocol
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target^[1]

FLT3

1 nM (IC₅₀)

c-Kit

2 nM (IC₅₀)

FGFR1

8 nM (IC₅₀)

FGFR3

9 nM (IC₅₀)

VEGFR1

1 nM (IC₅₀)

VEGFR3

8 nM (IC₅₀)

VEGFR2

13 nM (IC₅₀)

PDGFRα

27 nM (IC₅₀)

PDGFRβ

210 nM (IC₅₀)

In Vitro

Dovitinib potently inhibits the FGF-stimulated growth of WT and F384L-FGFR3-expressing B9 cells with IC₅₀ values of 25 nM. B9-MINV cells are resistant to the inhibitory activity of Dovitinib at concentrations up to 1 μM. Dovitinib 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]. Treatment of SK-HEP1 cells with dovitinib results in G2/M cell cycle arrest, inhibition of colony formation in soft agar and blockade of bFGF-induced cell migration. Dovitinib inhibits basal expression and FGF-induced phosphorylation of FGFR-1, FRS2-α and ERK1/2^[2].

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

In Vivo

Dovitinib (10 mg/kg, 30 mg/kg, 60 mg/kg, p.o.) shows significant antitumor effect in the KMS11-bearing mice model, and the growth inhibition is 48%, 78.5%, and 94% in the 10 mg/kg, 30 mg/kg, and 60 mg/kg treatment arms, respectively, compared with the placebo-treated mice^[1]. Dovitinib demonstrates significant antitumor and antimetastatic activities in HCC xenograft models. Dovitinib potently inhibits tumor growth of six HCC lines. Inhibition of angiogenesis correlates with inactivation of FGFR/PDGFR-β/VEGFR-2 signaling pathways. Dovitinib also causes dephosphorylation of retinoblastoma, upregulation of p-histone H2A-X and p27, and downregulation of p-cdk-2 and cyclin B1, which results in a reduction in cellular proliferation and the induction of tumor cell apoptosis^[2].

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

분자량

482.51

화학식

C₂₄H₂₇FN₆O₄

CAS No.

692737-80-7

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N1)C(C(NC2=C3)=NC2=CC=C3N4CCN(C)CC4)=C(N)C5=C1C=CC=C5F.O=C(O)C(C)O

선적

Room temperature in continental US; may vary elsewhere.

보관

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

용액&용해도

In Vitro:

DMSO : 25 mg/mL (51.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0725 mL	10.3625 mL	20.7250 mL
5 mM	0.4145 mL	2.0725 mL	4.1450 mL
10 mM	0.2072 mL	1.0362 mL	2.0725 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

몰농도 계산기
농도 희석 계산기

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

Concentration _(start)

Volume _(start)

Concentration _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

순도&문서

Purity: 99.75%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (251 KB) HNMR (162 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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]

Cell Assay ^[2]	To determine IC₅₀ for SK-HEP1 cells, cells are plated at a density of 2×10⁴ cells per dish. After 48 h, cells are treated with 0, 0.01, 0.1, 1, 5, 10, 50, 100 μM dovitinib in DMEM containing 1% FBS for 24 h. Cell viability is determined with Cell Proliferation Assay. IC₅₀ is calculated by nonlinear regression analysis using GraphPad Prism software^[2]. MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
Animal Administration ^[2]	Mice: Six HCC lines (06-0606, 26-0808A, 26-1004, 25-0705A, 5-1318, 21-0208) are used to establish tumors in male SCID mice. or dose-esponse experiments, mice bearing the 06-0606 xenografts re orally given vehicle (5% dextrose) or two doses of dovitinib (50 and 75 mg/kg) daily for 14 days. For time-dependent inhibition of dovitinib targets, mice bearing 06-0606 tumors are given orally 200 μL of either vehicle (n=6) or 50 mg/kg/day of dovitinib (n=10)^[2]. MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
References	[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0725 mL	10.3625 mL	20.7250 mL	51.8124 mL
	5 mM	0.4145 mL	2.0725 mL	4.1450 mL	10.3625 mL
	10 mM	0.2072 mL	1.0362 mL	2.0725 mL	5.1812 mL
	15 mM	0.1382 mL	0.6908 mL	1.3817 mL	3.4542 mL
	20 mM	0.1036 mL	0.5181 mL	1.0362 mL	2.5906 mL
	25 mM	0.0829 mL	0.4145 mL	0.8290 mL	2.0725 mL
	30 mM	0.0691 mL	0.3454 mL	0.6908 mL	1.7271 mL
	40 mM	0.0518 mL	0.2591 mL	0.5181 mL	1.2953 mL
	50 mM	0.0414 mL	0.2072 mL	0.4145 mL	1.0362 mL

Dovitinib lactate Related Classifications

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 lactate (Synonyms: CHIR-258 lactate; TKI-258 lactate)

고객리뷰

Other Forms of Dovitinib lactate:

Dovitinib lactate Related Antibodies

11 Publications Citing Use of MCE Dovitinib lactate

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All VEGFR Isoform Specific Products:

View All PDGFR Isoform Specific Products:

Biological Activity

Protocol

순도&문서

References

고객리뷰

Dovitinib lactate Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Dovitinib lactate Related Classifications

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고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

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