Savolitinib (Synonyms: Volitinib; HMPL-504; AZD-6094)

Name: Savolitinib
Brand: MedChemExpress
SKU: HY-15959
Rating: 5.0 (7 reviews)

製品番号: HY-15959 純度: 99.99% ee.: 98.12%: Data Sheet SDS COA 取扱説明書
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Technical Support

Savolitinib (AZD-6094) is a potent, highly selective, and orally bioavailable c-Met inhibitor with IC₅₀s of 5 nM and 3 nM for c-Met and p-Met, respectively. Savolitinib (AZD-6094) selectively binds to and inhibits the activation of c-Met in an ATP-competitive manner, and disrupts c-Met signal transduction pathways. Antineoplastic activity.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Savolitinib 構造式

CAS 番号 : 1313725-88-0

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 121	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 121	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$110	在庫あり	Estimated Time of Arrival: December 31
10 mg	$165	在庫あり	Estimated Time of Arrival: December 31
50 mg	$539	在庫あり	Estimated Time of Arrival: December 31
100 mg	$935	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

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

カスタマーレビュー

Based on 7 publication(s) in Google Scholar

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

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参考文献
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製品説明

IC₅₀ & Target

IC50: 5 nM (c-Met) and 3 nM (p-Met)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
NCI-H441	IC₅₀	0.003 3 Compound: 28	Inhibition of c-Met autophosphorylation in human NCI-H441 cells for 1 hr by ELISA Inhibition of c-Met autophosphorylation in human NCI-H441 cells for 1 hr by ELISA	[PMID: 25148209]
NCI-H441	IC₅₀	0.006 3 Compound: 28	Antiproliferative activity against human NCI-H441 cells assessed as HGF-induced proliferation after 72 hrs by MTT assay Antiproliferative activity against human NCI-H441 cells assessed as HGF-induced proliferation after 72 hrs by MTT assay	[PMID: 25148209]
NCI-H441	IC₅₀	0.003 3 Compound: 28	Inhibition of c-Met autophosphorylation in human NCI-H441 cells for 1 hr by ELISA Inhibition of c-Met autophosphorylation in human NCI-H441 cells for 1 hr by ELISA	[PMID: 25148209]
HepG2	IC₅₀	> 20 3 Compound: Savolitinib	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38086189]
NCI-H441	IC₅₀	0.006 3 Compound: 28	Antiproliferative activity against human NCI-H441 cells assessed as HGF-induced proliferation after 72 hrs by MTT assay Antiproliferative activity against human NCI-H441 cells assessed as HGF-induced proliferation after 72 hrs by MTT assay	[PMID: 25148209]
L02	IC₅₀	> 20 3 Compound: Savolitinib	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38086189]
MHCC97H	IC₅₀	2.46 1 Compound: Savolitinib	Antiproliferative activity against human MHCC97H cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MHCC97H cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38086189]
NCI-H441	IC₅₀	0.003 3 Compound: 28	Inhibition of c-Met autophosphorylation in human NCI-H441 cells for 1 hr by ELISA Inhibition of c-Met autophosphorylation in human NCI-H441 cells for 1 hr by ELISA	[PMID: 25148209]
NCI-H441	IC₅₀	0.006 3 Compound: 28	Antiproliferative activity against human NCI-H441 cells assessed as HGF-induced proliferation after 72 hrs by MTT assay Antiproliferative activity against human NCI-H441 cells assessed as HGF-induced proliferation after 72 hrs by MTT assay	[PMID: 25148209]

体内実験

Savolitinib (Compound 28; 1-10.0 mg/kg; oral administration; daily; for 21 days; athymic nude mice) demonstrates dose-dependent tumor growth inhibition in a U87MG subcutaneous xenograft model. In addition, none of the mice in the dosing groups exhibits body weight loss during the experiment^[1].

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

Animal Model:	U87MG xenograft model in athymic nude mice^[1]
Dosage:	1 mg/kg, 2.5 mg/kg and 10.0 mg/kg
Administration:	Oral administration; daily; for 21 days
Result:	Demonstrated dose-dependent tumor growth inhibition in a U87MG subcutaneous xenograft model.

臨床実験

分子量

345.36

分子式

C₁₇H₁₅N₉

CAS 番号

1313725-88-0

Appearance

Solid

Color

Off-white to yellow

SMILES

CN1N=CC(C2=CN=C3C(N([C@H](C4=CN5C(C=C4)=NC=C5)C)N=N3)=N2)=C1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

DMSO : ≥ 20.83 mg/mL (60.31 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8955 mL	14.4776 mL	28.9553 mL
5 mM	0.5791 mL	2.8955 mL	5.7911 mL
10 mM	0.2896 mL	1.4478 mL	2.8955 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (6.02 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.99% ee.: 98.12%

Select Batch:

データシート (281 KB) SDS (396 KB)

COA (257 KB) HNMR (266 KB) RP-HPLC (249 KB) NP-HPLC (88 KB) MS (69 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Jia H, et al. Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (volitinib) as a highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitor in clinical development for treatment of cancer. J Med Chem. 2014 Sep 25;57(18):7577-89. [Content Brief]

[2]. Gavine PR, et al. Volitinib, a potent and highly selective c-Met inhibitor, effectively blocks c-Met signaling and growth in c-MET amplified gastric cancer patient-derived tumor xenograft models. Mol Oncol. 2015 Jan;9(1):323-33. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.8955 mL	14.4776 mL	28.9553 mL	72.3882 mL
	5 mM	0.5791 mL	2.8955 mL	5.7911 mL	14.4776 mL
	10 mM	0.2896 mL	1.4478 mL	2.8955 mL	7.2388 mL
	15 mM	0.1930 mL	0.9652 mL	1.9304 mL	4.8259 mL
	20 mM	0.1448 mL	0.7239 mL	1.4478 mL	3.6194 mL
	25 mM	0.1158 mL	0.5791 mL	1.1582 mL	2.8955 mL
	30 mM	0.0965 mL	0.4826 mL	0.9652 mL	2.4129 mL
	40 mM	0.0724 mL	0.3619 mL	0.7239 mL	1.8097 mL
	50 mM	0.0579 mL	0.2896 mL	0.5791 mL	1.4478 mL
	60 mM	0.0483 mL	0.2413 mL	0.4826 mL	1.2065 mL

Savolitinib Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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.

Keywords:

Savolitinib1313725-88-0Volitinib HMPL-504 AZD-6094HMPL504HMPL 504HMPL-504AZD6094AZD 6094AZD-6094c-Met/HGFRInhibitorinhibitorinhibit

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Savolitinib (Synonyms: Volitinib; HMPL-504; AZD-6094)

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Savolitinib 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Savolitinib Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

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