Galunisertib (Synonyms: LY2157299)

Name: Galunisertib
Brand: MedChemExpress
SKU: HY-13226
Rating: 5.0 (68 reviews)

製品番号: HY-13226 純度: 99.90%: Data Sheet SDS COA 取扱説明書
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Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC₅₀ of 56 nM.

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CAS 番号 : 700874-72-2

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 55	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$50	在庫あり	Estimated Time of Arrival: December 31
10 mg	$70	在庫あり	Estimated Time of Arrival: December 31
50 mg	$150	在庫あり	Estimated Time of Arrival: December 31
100 mg	$250	在庫あり	Estimated Time of Arrival: December 31
200 mg	$375	在庫あり	Estimated Time of Arrival: December 31
500 mg	$750	在庫あり	Estimated Time of Arrival: December 31
1 g	$1125	在庫あり	Estimated Time of Arrival: December 31
5 g		お問い合わせ
10 g		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 68 publication(s) in Google Scholar

Other Forms of Galunisertib:

Galunisertib (Standard) 在庫あり
Galunisertib monohydrate お問い合わせ

顧客検証

Flow Cytometry

In Vivo Imaging

RT-PCR

Cell Imaging/Staining

: Galunisertib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Oct 7;10(1):332. [Abstract]; LY2157299 (100 mg/kg; oral gavage). The frequencies of CD31⁺VE^-Cadherin⁺ECs within CD45-Ter119- BM cells from mice subjected to the specified treatments were assessed through flow cytometry.

: Galunisertib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Oct 7;10(1):332. [Abstract]; LY2157299 (100 μM; 24 h). The mRNA level of PTN in BM ECs treated with TGF-β1 alone or in combination with LY2157299 (LY) was assessed via qPCR.

: Galunisertib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Oct 7;10(1):332. [Abstract]; LY2157299 (100 μM; 24 h). Representative images of double-positive BM ECs (yellow) co-stained with DiI-AcLDL (red) and FITC-UEA I (green) following the indicated treatments.

: Galunisertib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2023 Oct 3;42(1):258. [Abstract]; Galunisertib (75 mg/kg; oral gavage). Representative bioluminescent images and BLI analysis of mice with intrasplenic injection of MKN45 cells showed the inhibitory effect of the anti-LBP antibody and galunisertib on LM in vivo.

: Galunisertib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2023 Oct 3;42(1):258. [Abstract]; Galunisertib (75 mg/kg; oral gavage). IF was applied to confirm that galunisertib inhibit the actin remodeling of MKN45 cells.

TGF-β Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B BMP

生物活性
プロトコル
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

製品説明

Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC₅₀ of 56 nM.

IC₅₀ & Target

IC50: 56 nM (TGF-βRI)^[4]

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	CC₅₀	> 20 μM Compound: LY-2157299	Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 38626523]
4T1	IC₅₀	> 0.1 μM Compound: 5, LY-2157299	Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay	[PMID: 24786585]
BEAS-2B	CC₅₀	12.96 μM Compound: LY-2157299	Cytotoxicity against human BEAS-2B cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Cytotoxicity against human BEAS-2B cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 38626523]
HEK-293T	CC₅₀	> 20 μM Compound: LY-2157299	Cytotoxicity against HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Cytotoxicity against HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 38626523]
HaCaT	IC₅₀	> 0.1 μM Compound: 5, LY-2157299	Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay	[PMID: 24786585]
HepG2	CC₅₀	5.46 μM Compound: LY-2157299	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 38626523]
Kasumi 1	CC₅₀	3.12 μM Compound: LY-2157299	Antiproliferative activity against human Kasumi 1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human Kasumi 1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 38626523]
L02	CC₅₀	17.38 μM Compound: LY-2157299	Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 38626523]
MCF-10A	CC₅₀	19.88 μM Compound: LY-2157299	Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 38626523]
MDA-MB-231	CC₅₀	> 20 μM Compound: LY-2157299	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 38626523]
MV4-11	CC₅₀	> 20 μM Compound: LY-2157299	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 38626523]
PANC-1	CC₅₀	> 20 μM Compound: LY-2157299	Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 38626523]
Panc02	CC₅₀	> 20 μM Compound: LY-2157299	Antiproliferative activity against mouse Panc02 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse Panc02 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 38626523]
Sf9	IC₅₀	0.119 μM Compound: 3; LY-2157299	Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by radiometric assay Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by radiometric assay	[PMID: 31299584]
Sf9	IC₅₀	0.119 μM Compound: 4; LY-2157299	Inhibition of recombinant GST-tagged human ALK5 expressed in baculovirus infected Sf9 insect cells Inhibition of recombinant GST-tagged human ALK5 expressed in baculovirus infected Sf9 insect cells	[PMID: 31810777]
Sf9	IC₅₀	0.129 μM Compound: 3; LY-2157299	Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by scintillation counting method Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by scintillation counting method	[PMID: 31303386]
Sf9	IC₅₀	69.4 nM Compound: 4; LY-2157299	Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase assay Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase assay	[PMID: 26483198]
U-251	CC₅₀	16.96 μM Compound: LY-2157299	Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 38626523]

体外実験

Galunisertib (LY2157299) (0.1, 1, 10, and 100 μM) displays a slight dose-dependent potentiation of Bay 43-9006 in SK-Sora, HepG2, and Hep3B cell lines but not in JHH6, SK-HEP1, and HuH7 cell lines^[2].

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

体内実験

Human xenografts Calu6 (non-small cell lung cancer) and MX1 (breast cancer) are implanted subcutaneously in nude mice. After oral administration of 75 mg/kg, Galunisertib (LY2157299) induces a 70% decrease in pSmad for both types of cell lines. The time at which pSmad recovered 80% of baseline is approximately 6 h after administration^[3].

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

臨床実験

分子量

369.42

分子式

C₂₂H₁₉N₅O

CAS 番号

700874-72-2

Appearance

Solid

Color

White to yellow

SMILES

CC1=CC=CC(C2=NN3C(CCC3)=C2C4=CC=NC5=C4C=C(C=C5)C(N)=O)=N1

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 : 100 mg/mL (270.69 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	2.7069 mL	13.5347 mL	27.0695 mL
5 mM	0.5414 mL	2.7069 mL	5.4139 mL
10 mM	0.2707 mL	1.3535 mL	2.7069 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: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 5.75 mg/mL (15.56 mM); Clear solution
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.63 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 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.63 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 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 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.63 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: 99.95%

Select Batch:

データシート (282 KB) SDS (396 KB)

COA (252 KB) LCMS (121 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Cong L, et al. Targeting the TGF-β receptor with kinase inhibitors for scleroderma therapy. Arch Pharm (Weinheim). 2014 Sep;347(9):609-15. [Content Brief]

[2]. Serova M, et al. Effects of TGF-beta signalling inhibition with galunisertib (LY2157299) in hepatocellular carcinoma models and in ex vivo whole tumor tissue samples from patients. Oncotarget. 2015 Aug 28;6(25):21614-27 [Content Brief]

[3]. Bueno L, et al. Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-beta kinase antagonist, in mice. Eur J Cancer. 2008 Jan;44(1):142-50. [Content Brief]

[4]. Herbertz S, et al. Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway. Drug Des Devel Ther. 2015 Aug 10;9:4479-99. [Content Brief]

細胞実験 ^[2]	Cell survival is determined using the MTT assay. The conversion of yellow water-soluble tetrazolium MTT into purple insoluble formazan is catalyzed by mitochondrial dehydrogenases and used to estimate the number of viable cells. In brief, cells are seeded in 96-well tissue culture plates at a density of 2×10³ cells/well. After drug exposure, cells are incubated with 0.4 mg/mL MTT for 4 hours at 37°C. After incubation, the supernatant is discarded, insoluble formazan precipitates are dissolved in 0.1 mL of DMSO, and the absorbance is measured at 560 nm by use of a microplate reader. Wells with untreated cells or with drug-containing medium without cells are used as positive and negative controls respectively. For proliferation assay, MTT assay is done daily to determine the number of viable cells in untreated control andGalunisertib (LY2157299) (0.1, 1, 10, and 10 μM)-treated group^[2]. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[3]	Mice^[3] Charles River nude mice (weight 25 mg) are used. Galunisertib (LY2157299) is given orally as a single dose or in a multiple dosing design. The value of the dose levels given in a single dose manner is 10 (n=3), 30 (n=8), 50 (n=26), 75 (n=69), 100 (n=3), 150 (n=21) and 300 (n=3) mg/kg. Animals are sacrificed at the following times: 0.5, 1, 1.5, 2, 4, 8 and 16 h after administration, then the tumor is removed and blood is recovered. In the multiple dosing study, Galunisertib (LY2157299) is administered twice a day (bid) at the dose of 75 mg/kg every 12 h for 20 consecutive days to 31 mice. Animals are sacrificed at 2 h after the last administration at days 10, 15, 20 and 25, and the tumor is removed for pSmad determination and the blood is recovered for determination of drug levels in plasma. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[1]. Cong L, et al. Targeting the TGF-β receptor with kinase inhibitors for scleroderma therapy. Arch Pharm (Weinheim). 2014 Sep;347(9):609-15. [Content Brief] [2]. Serova M, et al. Effects of TGF-beta signalling inhibition with galunisertib (LY2157299) in hepatocellular carcinoma models and in ex vivo whole tumor tissue samples from patients. Oncotarget. 2015 Aug 28;6(25):21614-27 [Content Brief] [3]. Bueno L, et al. Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-beta kinase antagonist, in mice. Eur J Cancer. 2008 Jan;44(1):142-50. [Content Brief] [4]. Herbertz S, et al. Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway. Drug Des Devel Ther. 2015 Aug 10;9:4479-99. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.7069 mL	13.5347 mL	27.0695 mL	67.6736 mL
	5 mM	0.5414 mL	2.7069 mL	5.4139 mL	13.5347 mL
	10 mM	0.2707 mL	1.3535 mL	2.7069 mL	6.7674 mL
	15 mM	0.1805 mL	0.9023 mL	1.8046 mL	4.5116 mL
	20 mM	0.1353 mL	0.6767 mL	1.3535 mL	3.3837 mL
	25 mM	0.1083 mL	0.5414 mL	1.0828 mL	2.7069 mL
	30 mM	0.0902 mL	0.4512 mL	0.9023 mL	2.2558 mL
	40 mM	0.0677 mL	0.3384 mL	0.6767 mL	1.6918 mL
	50 mM	0.0541 mL	0.2707 mL	0.5414 mL	1.3535 mL
	60 mM	0.0451 mL	0.2256 mL	0.4512 mL	1.1279 mL
	80 mM	0.0338 mL	0.1692 mL	0.3384 mL	0.8459 mL
	100 mM	0.0271 mL	0.1353 mL	0.2707 mL	0.6767 mL

Galunisertib 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:

Galunisertib700874-72-2LY2157299LY 2157299LY-2157299TGF-β ReceptorTransforming growth factor beta receptorsInhibitorinhibitorinhibit

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Galunisertib (Synonyms: LY2157299)

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Complete Stock Solution Preparation Table

Galunisertib Related Classifications

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The molarity calculator equation

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Galunisertib (Synonyms: LY2157299)

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Other Forms of Galunisertib:

Galunisertib 関連抗体

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おすすめ

•関連スクリーニングライブラリ:

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TGF-β Receptor アイソフォーム固有の製品をすべて表示:

生物活性

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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

Galunisertib 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Galunisertib Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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