Myoferlin inhibitor 1

Name: Myoferlin inhibitor 1
Brand: MedChemExpress
SKU: HY-143657
Rating: 4.5 (1 reviews)

Cat. No.: HY-143657 Purity: 99.88%: Data Sheet
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Myoferlin inhibitor 1 is a compound that exhibits reversible, concentration-dependent binding to the myoferlin MYOF-C2D protein, with a K_D of 0.094 μM. Myoferlin inhibitor 1 shows potent anti-invasion and anti-migration activities against different pancreatic cancer cells. Myoferlin inhibitor 1 inhibits pancreatic cancer metastasis through reversing mesenchymal transition (EMT), inhibiting the secretions of MMP1 and MMP2 and blocking the receptor tyrosine kinases. Myoferlin inhibitor 1 displays effective antimetastatic activities in pancreatic cancer in vitro and in vivo. Myoferlin inhibitor 1 can be used in research on preventing pancreatic cancer metastasis.

For research use only. We do not sell to patients.

Myoferlin inhibitor 1 Chemical Structure

CAS No. : 2366279-99-2

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Based on 1 publication(s) in Google Scholar

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View All MMP Isoform Specific Products:

View All Isoforms

MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8

Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
Capan-2	IC₅₀	2.85 μM Compound: 6y	Cytotoxicity against human Capan2 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay Cytotoxicity against human Capan2 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay	[PMID: 31026162]
MCF-10A	IC₅₀	27.56 μM Compound: 6y	Cytotoxicity against human MCF10A cells assessed as reduction in cell viability measured after 48 hrs by MTS assay Cytotoxicity against human MCF10A cells assessed as reduction in cell viability measured after 48 hrs by MTS assay	[PMID: 31026162]
MIA PaCa-2	IC₅₀	1.54 μM Compound: 6y	Cytotoxicity against human MIAPaCa2 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay Cytotoxicity against human MIAPaCa2 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay	[PMID: 31026162]
PANC-1	IC₅₀	0.11 μM Compound: 6y	Antimigratory activity against human PANC1 cells measured after 18 hrs in presence of mitomycin C using crystal violet staining by inverted microscopy-based transwell assay Antimigratory activity against human PANC1 cells measured after 18 hrs in presence of mitomycin C using crystal violet staining by inverted microscopy-based transwell assay	[PMID: 31026162]
PANC-1	IC₅₀	0.12 μM Compound: 6y	Antiinvasive activity against human PANC1 cells measured after 18 hrs in presence of mitomycin C using crystal violet staining by inverted microscopy-based matrigel coated transwell assay Antiinvasive activity against human PANC1 cells measured after 18 hrs in presence of mitomycin C using crystal violet staining by inverted microscopy-based matrigel coated transwell assay	[PMID: 31026162]
PANC-1	IC₅₀	0.84 μM Compound: 6y	Cytotoxicity against human PANC1 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay Cytotoxicity against human PANC1 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay	[PMID: 31026162]

In Vitro

Myoferlin inhibitor 1 (compound 6y) (18 h) inhibits the invasion of PANC1 cells with an IC₅₀ of 0.12 μM^[1].
Myoferlin inhibitor 1 (100-400 nM, 18-36 h) inhibits the migration of PANC1, MiaPaCa2, and Capan2 cells in a concentration-dependent manner^[1].
Myoferlin inhibitor 1 (48 h) exhibits cellular toxicity in three pancreatic cancer cell lines (PANC-1, MIA PaCa-2, and Capan-2) with IC₅₀ values of 0.84, 1.54, and 2.85 μM, and in three normal human cell lines (HAF, HPDE6-C7, and MCF-10A) with IC₅₀ values of 8.54, 14.64, and 27.56 μM, respectively^[1].
Myoferlin inhibitor 1 (0-400 nM, 18 h) exhibits an antimigration effect that is positively correlated with MYOF expression in PANC1 cells^[1].
Myoferlin inhibitor 1 (0-400 nM, 0-24 h) reverses pancreatic cancer cells to the epithelial state, inhibits the secretions of MMP1 and MMP2, and suppresses tumor metastasis in a dose-dependent manner through both VEGF and EGFR signaling pathways^[1].
Myoferlin inhibitor 1 (0.05-50 μM) exhibits weak inhibitory effects on the tested human CYP enzymes, with particularly reduced activity against CYP2C9^[1].

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

Cell Migration Assay ^[1]

Cell Line:	PANC1, MiaPaCa2, and Capan2 cells
Concentration:	100, 200, and 400 nM
Incubation Time:	18 h for PANC1, 24 h for MiaPaCa2, and 36 h for Capan2
Result:	Reduced migrated cell numbers of PANC1, MiaPaCa2 and Capan2 cells in a concentration-dependent manner.

Western Blot Analysis^[1]

Cell Line:	PANC1 cells
Concentration:	100, 200, and 400 nM
Incubation Time:	15, 30, 60, 120 min and 24 h
Result:	Increased the expression of the epithelial marker E-cadherin and decreased that of the mesenchymal marker fibronectin in a concentration-dependent manner. Decreased the levels of MMP1 and MMP2 in PANC1 cells in a concentration-dependent manner. Depressed the phosphorylation of VEGFR induced by VEGF. Caused sustained EGFR phosphorylation upon 10 ng/mL EGF stimulation, thereby preventing the deactivation of the EGFR signaling pathway.

In Vivo

Myoferlin inhibitor 1 (25 and 50 mg/kg, i.p., daily for 21 days) possesses potent antimetastatic activities and can improve overall survival without significant toxicity in pancreatic cancer lung metastasis mice model^[1].

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

Animal Model:	BALB/c nude mice (8 weeks old) intravenously injected with PANC1-luc cancer cells^[1]
Dosage:	25 and 50 mg/kg
Administration:	i.p., daily for 21 days
Result:	Dose-dependently inhibited pancreatic cancer pulmonary metastasis with superior antitumor metastatic activity compared to the positive control at the same dosage. Significantly prolonged the overall survival, resulting in survival rates of 75 % at 25 mg/kg and 87.5 % at 50 mg/kg. Revealed no significant toxicity in the major organs (heart, lung, liver, spleen, and kidney).

Molecular Weight

456.54

Formula

C₂₆H₂₈N₆O₂

CAS No.

2366279-99-2

Appearance

Solid

Color

White to off-white

SMILES

O=C(NCCCCC1=CC=CC=C1)C2=CC=CC(N3N=C(CC)N=C3C4=NC=C(OC)C=N4)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (109.52 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	2.1904 mL	10.9519 mL	21.9039 mL
5 mM	0.4381 mL	2.1904 mL	4.3808 mL
10 mM	0.2190 mL	1.0952 mL	2.1904 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.

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Purity & Documentation

Purity: 99.88%

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Data Sheet (276 KB) SDS (251 KB)

COA (248 KB) HNMR (269 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Li Y, et al. Modification and Biological Evaluation of a Series of 1,5-Diaryl-1,2,4-triazole Compounds as Novel Agents against Pancreatic Cancer Metastasis through Targeting Myoferlin. J Med Chem. 2019 May 23;62(10):4949-4966. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.1904 mL	10.9519 mL	21.9039 mL	54.7597 mL
	5 mM	0.4381 mL	2.1904 mL	4.3808 mL	10.9519 mL
	10 mM	0.2190 mL	1.0952 mL	2.1904 mL	5.4760 mL
	15 mM	0.1460 mL	0.7301 mL	1.4603 mL	3.6506 mL
	20 mM	0.1095 mL	0.5476 mL	1.0952 mL	2.7380 mL
	25 mM	0.0876 mL	0.4381 mL	0.8762 mL	2.1904 mL
	30 mM	0.0730 mL	0.3651 mL	0.7301 mL	1.8253 mL
	40 mM	0.0548 mL	0.2738 mL	0.5476 mL	1.3690 mL
	50 mM	0.0438 mL	0.2190 mL	0.4381 mL	1.0952 mL
	60 mM	0.0365 mL	0.1825 mL	0.3651 mL	0.9127 mL
	80 mM	0.0274 mL	0.1369 mL	0.2738 mL	0.6845 mL
	100 mM	0.0219 mL	0.1095 mL	0.2190 mL	0.5476 mL