标签归档：lactate

Dovitinib lactate(Synonyms: 多韦替尼乳酸盐; CHIR-258 lactate; TKI-258 lactate)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Dovitinib lactate (Synonyms: 多韦替尼乳酸盐; CHIR-258 lactate; TKI-258 lactate) 纯度: 99.62%

Dovitinib lactate (TKI258 lactate) 是多靶点的酪氨酸激酶抑制剂，抑制 FLT3，c-Kit，FGFR1/3，VEGFR1/2/3 和 PDGFRα/β 的 IC50 值分别为 1，2，8/9，10/13/8，27/210 nM。

Dovitinib lactate(Synonyms: 多韦替尼乳酸盐; CHIR-258 lactate; TKI-258 lactate)

Dovitinib lactate Chemical Structure

CAS No. : 692737-80-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥605 In-stock
5 mg ￥550 In-stock
10 mg ￥880 In-stock
50 mg ￥2650 In-stock
100 mg ￥4400 In-stock
200 mg ￥7700 In-stock
500 mg ￥15000 In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

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生物活性

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[1].

IC50 & Target

FGFR3

9 nM (IC50)

FGFR1

8 nM (IC50)

VEGFR1

1 nM (IC50)

VEGFR2

13 nM (IC50)

VEGFR3

8 nM (IC50)

PDGFRα

27 nM (IC50)

PDGFRβ

210 nM (IC50)

FLT3

1 nM (IC50)

c-Kit

2 nM (IC50)

体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

482.51

Formula

C24H27FN6O4
CAS 号

692737-80-7
中文名称

多韦替尼乳酸盐
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

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

DMSO : ≥ 30 mg/mL (62.17 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 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

*

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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.

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

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
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.

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

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Panobinostat lactate(Synonyms: LBH589 lactate; NVP-LBH589 lactate)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Panobinostat lactate (Synonyms: LBH589 lactate; NVP-LBH589 lactate)

Panobinostat lactate 是一种有效的口服非选择性 HDAC 抑制剂，具有抗肿瘤活性。Panobinostat lactate 可有效干扰HIV潜伏期。Panobinostat lactate 诱导细胞凋亡 (apoptosis) 和自噬 (autophagy)。Panobinostat lactate 可用于难治性或复发性多发性骨髓瘤的研究。

Panobinostat lactate(Synonyms: LBH589 lactate; NVP-LBH589 lactate)

Panobinostat lactate Chemical Structure

CAS No. : 960055-56-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Panobinostat lactate 的其他形式现货产品:

Panobinostat

生物活性

Panobinostat lactate is a potent and orally active non-selective HDAC inhibitor. Panobinostat lactate has antineoplastic activities. Panobinostat lactate effectively disrupts HIV latency. Panobinostat lactate induces cell apoptosis and autophagy. Panobinostat lactate can be used for the study of refractory or relapsed multiple myeloma[1][2][3][4][5].

IC50 & Target

HDAC

 

HIV-1

 

体外研究
(In Vitro)

Panobinostat lactate induces apoptosis of both MOLT-4 and Reh cells in a time- and dose-dependent manner. Panobinosta lactate results in histone (H3K9 and H4K8) hyperacetylation and regulation of cell-cycle control genes in Reh cells[1].
Panobinostat lactate exhibites potent antiproliferative activity in human NSCLC cell lines with the IC50 ranging from 5 to 100 nM[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Panobinosta lactate (10, 20 mg/kg, i.p.) significantly slows tumor growth derived from Meso and NSCLC cells in vivo models. Panobinosta lactate markedly increases acetylation of histone H3 and H4 of H69 human SCLC cells harvest from SCID mice[2].
Panobinostat lactate (5, 10 and 20 mg/kg i.p.) demonstrates a clear benefit of decreased tumor burden, significantly improves TTE and reduces bone density loss in a disseminated multiple myeloma mouse model[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

439.50

Formula

C24H29N3O5
CAS 号

960055-56-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Scuto A, et al. The novel histone deacetylase inhibitor, LBH589, induces expression of DNA damage response genes and apoptosis in Ph- acute lymphoblastic leukemia cells. Blood. 2008 May 15;111(10):5093-100.

    [2]. Crisanti MC, et al. The HDAC inhibitor panobinostat (LBH589) inhibits mesothelioma and lung cancer cells in vitro and in vivo with particular efficacy for small cell lung cancer. Mol Cancer Ther. 2009 Aug;8(8):2221-31.

    [3]. Ocio EM, et al. In vitro and in vivo rationale for the triple combination of panobinostat (LBH589) and dexamethasone with either bortezomib or lenalidomide in multiple myeloma. Haematologica. 2010 May;95(5):794-803.

    [4]. Banerjee NS, et al. Vorinostat, a pan-HDAC inhibitor, abrogates productive HPV-18 DNA amplification. Proc Natl Acad Sci U S A. 2018 Nov 20;115(47):E11138-E11147.

    [5]. Barton K, et al. Broad activation of latent HIV-1 in vivo. Nat Commun. 2016;7:12731. Published 2016 Sep 8.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Dovitinib lactate hydrate(Synonyms: TKI258 lactate hydrate; CHIR-258 lactate hydrate)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Dovitinib lactate hydrate (Synonyms: TKI258 lactate hydrate; CHIR-258 lactate hydrate)

Dovitinib lactate hydrate (TKI258 lactate hydrate) 是多靶点的酪氨酸激酶抑制剂，抑制 FLT3，c-Kit，FGFR1/3，VEGFR1/2/3 和 PDGFRα/β 的 IC50 值分别为 1，2，8/9，10/13/8，27/210 nM。

Dovitinib lactate hydrate(Synonyms: TKI258 lactate hydrate; CHIR-258 lactate hydrate)

Dovitinib lactate hydrate Chemical Structure

CAS No. : 915769-50-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Dovitinib lactate hydrate 的其他形式现货产品:

Dovitinib lactate Dovitinib

生物活性

Dovitinib lactate hydrate (TKI258 lactate hydrate) 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[1].

IC50 & Target[1]

FGFR1

8 nM (IC50)

FGFR3

9 nM (IC50)

VEGFR1

1 nM (IC50)

VEGFR2

13 nM (IC50)

VEGFR3

8 nM (IC50)

PDGFRα

27 nM (IC50)

PDGFRβ

210 nM (IC50)

FLT3

1 nM (IC50)

c-Kit

2 nM (IC50)

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

500.52

Formula

C24H29FN6O5
CAS 号

915769-50-5
中文名称

多韦替尼乳酸盐水合物
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务