Crenigacestat (Synonyms: LY3039478)

Name: Crenigacestat
Brand: MedChemExpress
SKU: HY-12449
Rating: 5.0 (7 reviews)

製品番号: HY-12449 純度: 99.01%: Data Sheet SDS COA 取扱説明書
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Crenigacestat (LY3039478) is an orally active Notch and γ-secretase inhibitor, with an IC₅₀ of 1 nM in most of the tumor cell lines tested.

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CAS 番号 : 1421438-81-4

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 153	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 153	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$71	在庫あり	Estimated Time of Arrival: December 31
5 mg	$150	在庫あり	Estimated Time of Arrival: December 31
10 mg	$250	在庫あり	Estimated Time of Arrival: December 31
25 mg	$450	在庫あり	Estimated Time of Arrival: December 31
50 mg	$750	在庫あり	Estimated Time of Arrival: December 31
100 mg	$1250	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

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Based on 7 publication(s) in Google Scholar

顧客検証

•ACS Comb Sci. 2019 Dec 9;21(12):805-816. [Abstract]

Flow Cytometry

: Crenigacestat purchased from MedChemExpress. Usage Cited in: Mol Cell Biochem. 2025 Jun 11. [Abstract]; After treating GC cells with the Notch inhibitor Crenigacestat (10 μM) for 2 hours, FOXM1 cells were transfected, and Western blot analysis was performed to detect that Crenigacestat treatment reduced the expression levels of Notch signaling pathway-related proteins.

: Crenigacestat purchased from MedChemExpress. Usage Cited in: Mol Cell Biochem. 2025 Jun 11. [Abstract]; Western blot analysis revealed that treatment with Crenigacestat (10 μM) reduced the expression of PD-L1 protein.

: Crenigacestat purchased from MedChemExpress. Usage Cited in: Mol Cell Biochem. 2025 Jun 11. [Abstract]; The results of CFSE staining confirmed that Crenigacestat (10 μM) treatment partially increased the proliferative capacity of CD8 + T cells.

: Crenigacestat purchased from MedChemExpress. Usage Cited in: Mol Cell Biochem. 2025 Jun 11. [Abstract]; Flow cytometry confirmed that Crenigacestat (10 μM) treatment partially reduced the apoptosis rate of CD8 + T cells.

: Crenigacestat purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2022 Dec;19(12):1373-1391. [Abstract]; Crenigacestat (8 mg/kg). Representative confocal images of primary tumor sections stained with anti-α-SMA antibody.

: Crenigacestat purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2019 May;120(5):6972-6987. [Abstract]; The Western blot analysis results show that LY3039478 inhibits not only Notch1 but also APRIL.

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製品説明

Crenigacestat (LY3039478) is an orally active Notch and γ-secretase inhibitor, with an IC₅₀ of 1 nM in most of the tumor cell lines tested^[1]^[2]^[3]^[4].

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.48 nM Compound: 1	Inhibition of gamma-secretase mediated cleavage of Notch 1 in human A375 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA Inhibition of gamma-secretase mediated cleavage of Notch 1 in human A375 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA	[PMID: 24900678]
A2780	IC₅₀	1.03 nM Compound: 1	Inhibition of gamma-secretase mediated cleavage of Notch 1 in human A2780 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA Inhibition of gamma-secretase mediated cleavage of Notch 1 in human A2780 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA	[PMID: 24900678]
BXPC-3	IC₅₀	0.39 nM Compound: 1	Inhibition of gamma-secretase mediated cleavage of Notch 1 in human BxPC3 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA Inhibition of gamma-secretase mediated cleavage of Notch 1 in human BxPC3 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA	[PMID: 24900678]
CCRF-CEM	IC₅₀	0.76 nM Compound: 1	Inhibition of gamma-secretase mediated cleavage of Notch 1 in human CCRF-CEM cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA Inhibition of gamma-secretase mediated cleavage of Notch 1 in human CCRF-CEM cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA	[PMID: 24900678]
DLD-1	IC₅₀	0.98 nM Compound: 1	Inhibition of gamma-secretase mediated cleavage of Notch 1 in human DLD1 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA Inhibition of gamma-secretase mediated cleavage of Notch 1 in human DLD1 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA	[PMID: 24900678]
HCT-116	IC₅₀	0.72 nM Compound: 1	Inhibition of gamma-secretase mediated cleavage of Notch 1 in human HCT 116 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA Inhibition of gamma-secretase mediated cleavage of Notch 1 in human HCT 116 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA	[PMID: 24900678]
Jurkat	IC₅₀	5.95 nM Compound: 1	Inhibition of gamma-secretase mediated cleavage of Notch 1 in human Jurkat cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA Inhibition of gamma-secretase mediated cleavage of Notch 1 in human Jurkat cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA	[PMID: 24900678]
K562	IC₅₀	0.74 nM Compound: 1	Inhibition of gamma-secretase mediated cleavage of Notch 1 in human K562 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA Inhibition of gamma-secretase mediated cleavage of Notch 1 in human K562 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA	[PMID: 24900678]
MDA-MB-231	IC₅₀	0.5 nM Compound: 1	Inhibition of gamma-secretase mediated cleavage of Notch 1 in human MDA-MB-231 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA Inhibition of gamma-secretase mediated cleavage of Notch 1 in human MDA-MB-231 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA	[PMID: 24900678]
MIA PaCa-2	IC₅₀	0.71 nM Compound: 1	Inhibition of gamma-secretase mediated cleavage of Notch 1 in human MIAPaCa2 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA Inhibition of gamma-secretase mediated cleavage of Notch 1 in human MIAPaCa2 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA	[PMID: 24900678]
MOLT-3	IC₅₀	0.61 nM Compound: 1	Inhibition of gamma-secretase mediated cleavage of Notch 1 in human MOLT-3 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA Inhibition of gamma-secretase mediated cleavage of Notch 1 in human MOLT-3 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA	[PMID: 24900678]
MOLT-4	IC₅₀	0.74 nM Compound: 1	Inhibition of gamma-secretase mediated cleavage of Notch 1 in human MOLT-4 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA Inhibition of gamma-secretase mediated cleavage of Notch 1 in human MOLT-4 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA	[PMID: 24900678]
SUP-T1	IC₅₀	1.24 nM Compound: 1	Inhibition of gamma-secretase mediated cleavage of Notch 1 in human SUP-T1 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA Inhibition of gamma-secretase mediated cleavage of Notch 1 in human SUP-T1 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA	[PMID: 24900678]
SW480	IC₅₀	0.1 nM Compound: 1	Inhibition of gamma-secretase mediated cleavage of Notch 1 in human SW480 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA Inhibition of gamma-secretase mediated cleavage of Notch 1 in human SW480 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA	[PMID: 24900678]
U-87MG ATCC	IC₅₀	0.28 nM Compound: 1	Inhibition of gamma-secretase mediated cleavage of Notch 1 in human U-87-MG cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA Inhibition of gamma-secretase mediated cleavage of Notch 1 in human U-87-MG cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA	[PMID: 24900678]

体外実験

Crenigacestat (100 nM) exhibits anti-cancer activity in K07074 cells (a primary mouse liver tumor cell line)^[2].
Crenigacestat (LY3039478) decreases expression of Myc and cyclin A1 (part of the NOTCH-driven proliferative signature) in murine and human model systems. Crenigacestat (LY3039478) treatment also leads to G0/G1 cell cycle arrest in CCRCC cells^[3].

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

Cell Viability Assay^[2].

Cell Line:	K07074 cells.
Concentration:	100 nM.
Incubation Time:	24-96 hours.
Result:	Effectively reduced the growth of K07074 cells.

体内実験

Crenigacestat (8 mg/kg, oral gavage three times a week) resulted in significantly increases survival and delayed tumor growth in independent cohorts of mice demonstrating in vivo efficacy in CCRCC^[3].

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

Animal Model:	CCRCC xenografts were established in NOD-scid IL2R null mice with subcutaneous implantation using the 769-P cell line^[3].
Dosage:	8 mg/kg.
Administration:	Oral gavage three times a week.
Result:	Resulted in increased overall survival when compared with vehicle control in CCRCC xenografts.

臨床実験

分子量

464.44

分子式

C₂₂H₂₃F₃N₄O₄

CAS 番号

1421438-81-4

Appearance

Solid

Color

White to off-white

SMILES

O=C(N[C@@H](C)C(N[C@H]1C2=CC=CC=C2C3=CC=CN=C3N(CCO)C1=O)=O)CCC(F)(F)F

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 (215.31 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	2.1531 mL	10.7657 mL	21.5313 mL
5 mM	0.4306 mL	2.1531 mL	4.3063 mL
10 mM	0.2153 mL	1.0766 mL	2.1531 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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: ≥ 5 mg/mL (10.77 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (10.77 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (10.77 mM); Clear solution

This protocol yields a clear solution of ≥ 5 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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μL

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

Please enter your animal formula composition:

DMSO +

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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: 99.01%

Select Batch:

データシート (281 KB) SDS (393 KB)

COA (254 KB) RP-HPLC (217 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Yuen E, et al. Evaluation of the effects of an oral notch inhibitor, crenigacestat (LY3039478), on QT interval, and bioavailability studies conducted in healthy subjects. Cancer Chemother Pharmacol. 2019 Mar;83(3):483-492. [Content Brief]

[2]. Mäemets-Allas K, et al. The inhibition of Akt-Pdpk1 interaction efficiently suppresses the growth of murine primary liver tumor cells. Biochem Biophys Res Commun. 2016 May 20;474(1):118-125. [Content Brief]

[3]. Bhagat TD, et al. Notch Pathway Is Activated via Genetic and Epigenetic Alterations and Is a Therapeutic Target in Clear Cell Renal Cancer. J Biol Chem. 2017 Jan 20;292(3):837-846. [Content Brief]

[4]. Mark H. Bender, et al. Abstract 1131: Novel inhibitor of Notch signaling for the treatment of cancer. Experimental and Molecular Therapeutics. 2013.

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.1531 mL	10.7657 mL	21.5313 mL	53.8283 mL
	5 mM	0.4306 mL	2.1531 mL	4.3063 mL	10.7657 mL
	10 mM	0.2153 mL	1.0766 mL	2.1531 mL	5.3828 mL
	15 mM	0.1435 mL	0.7177 mL	1.4354 mL	3.5886 mL
	20 mM	0.1077 mL	0.5383 mL	1.0766 mL	2.6914 mL
	25 mM	0.0861 mL	0.4306 mL	0.8613 mL	2.1531 mL
	30 mM	0.0718 mL	0.3589 mL	0.7177 mL	1.7943 mL
	40 mM	0.0538 mL	0.2691 mL	0.5383 mL	1.3457 mL
	50 mM	0.0431 mL	0.2153 mL	0.4306 mL	1.0766 mL
	60 mM	0.0359 mL	0.1794 mL	0.3589 mL	0.8971 mL
	80 mM	0.0269 mL	0.1346 mL	0.2691 mL	0.6729 mL
	100 mM	0.0215 mL	0.1077 mL	0.2153 mL	0.5383 mL

Crenigacestat 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:

Crenigacestat1421438-81-4LY3039478LY 3039478LY-3039478Notchγ-secretaseGamma secretaseliverCCRCCInhibitorinhibitorinhibit

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Crenigacestat (Synonyms: LY3039478)

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Crenigacestat 関連抗体

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Complete Stock Solution Preparation Table

Crenigacestat Related Classifications

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The molarity calculator equation

The dilution calculator equation

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