INCB3619

Cat. No.: HY-12636: FAQs
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INCB3619 is a selective and orally active ADAM inhibitor with IC₅₀ of 22 nM and 14 nM for ADAM10 and ADAM17, respectively. INCB3619 has anti-tumor activity.

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

INCB3619 Chemical Structure

CAS No. : 791826-72-7

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Purity & Documentation
References
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Description

INCB3619 is a selective and orally active ADAM inhibitor with IC₅₀ of 22 nM and 14 nM for ADAM10 and ADAM17, respectively. INCB3619 has anti-tumor activity^[1].

In Vitro

INCB3619 (0-10 μM, 96 h) can inhibit heregulin-dependent HER3-Akt pathway, but not ERK activity in A549 cells, and induce apoptosis in A549 cells^[1].
INCB3619 (0-10 μM, 72 h) can inhibit EGFR ligand signaling in the EGFR autocrine cell line NCI-H1666 and can be used in combination with other anti-EGFR drugs such as gefitinib^[1].
INCB3619 (2 µM) inhibits ERK1/2 expression in NCI-H1666 and make it sensitive to Gefitinib (HY-50895)^[1].

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

Apoptosis Analysis^[1].

Cell Line:	A549 cell
Concentration:	1, 10 μM
Incubation Time:
Result:	Induced about 3% apoptosis at a concentration of 1 μM and about 5% at a concentration of 10 μM.

Cell Viability Assay^[1].

Cell Line:	NCI-H1666 cell
Concentration:	0-10 μM
Incubation Time:	72 h
Result:	Inhibited proliferation of NCI-H1666 cells.

In Vivo

INCB3619 (subcutaneous injection, 60 mg/kg/d, 14 d) exhibits antitumor activity and sensitizes tumors to Gefitinib (HY-50895) in A549 xenografted BALB/c nu/nu mouse model^[1].

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

Animal Model:	BALB/c nu/nu mouse model of A549 xenograft
Dosage:	50, 60 mg/kg
Administration:	subcutaneous injection, daily, 14 d
Result:	Significant tumor growth inhibition and delay at 60 mg/kg dose, less active effect at 50 mg/kg.

Molecular Weight

413.47

Formula

C₂₂H₂₇N₃O₅

CAS No.

791826-72-7

SMILES

O=C(N([C@H](C(N1CC=C(C2=CC=CC=C2)CC1)=O)[C@@H](C(NO)=O)C3)CC43CC4)OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Bin-Bing S Zhou, et al. Targeting ADAM-mediated ligand cleavage to inhibit HER3 and EGFR pathways in non-small cell lung cancer. Cancer Cell. 2006 Jul;10(1):39-50. [Content Brief]

INCB3619 Related Classifications

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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:

INCB3619791826-72-7INCB 3619INCB-3619MMPApoptosisMatrix metalloproteinasesADAMADAM10ADAM17Anti-tumorInhibitorinhibitorinhibit

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