2. Metabolic Enzyme/Protease Apoptosis
  3. MMP Apoptosis
  4. INCB3619

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

INCB3619 Chemical Structure

CAS No. : 791826-72-7

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Based on 1 publication(s) in Google Scholar

INCB3619 Related Antibodies

Top Publications Citing Use of Products

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

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].

Cellular Effect
Cell Line Type Value Description References
A549 IC50
1 μM
Compound: INCB3619
Inhibition of ADAM17 in human A549 cells assessed as potentiation of gefitinib-mediated inhibition of cell viability by measuring gefitinib IC50 at 10 uM after 96 hrs by CellTiter-Glo assay (Rvb = 8 microM)
Inhibition of ADAM17 in human A549 cells assessed as potentiation of gefitinib-mediated inhibition of cell viability by measuring gefitinib IC50 at 10 uM after 96 hrs by CellTiter-Glo assay (Rvb = 8 microM)
[PMID: 26192023]
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.

INCB3619 Related Antibodies

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.
Appearance

Solid

Color

White to off-white

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
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (241.86 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 2.4186 mL 12.0928 mL 24.1856 mL
5 mM 0.4837 mL 2.4186 mL 4.8371 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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Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.46%

SDS (251 KB)

COA (252 KB) HNMR (264 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4186 mL 12.0928 mL 24.1856 mL 60.4639 mL
5 mM 0.4837 mL 2.4186 mL 4.8371 mL 12.0928 mL
10 mM 0.2419 mL 1.2093 mL 2.4186 mL 6.0464 mL
15 mM 0.1612 mL 0.8062 mL 1.6124 mL 4.0309 mL
20 mM 0.1209 mL 0.6046 mL 1.2093 mL 3.0232 mL
25 mM 0.0967 mL 0.4837 mL 0.9674 mL 2.4186 mL
30 mM 0.0806 mL 0.4031 mL 0.8062 mL 2.0155 mL
40 mM 0.0605 mL 0.3023 mL 0.6046 mL 1.5116 mL
50 mM 0.0484 mL 0.2419 mL 0.4837 mL 1.2093 mL
60 mM 0.0403 mL 0.2015 mL 0.4031 mL 1.0077 mL
80 mM 0.0302 mL 0.1512 mL 0.3023 mL 0.7558 mL
100 mM 0.0242 mL 0.1209 mL 0.2419 mL 0.6046 mL
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INCB3619 Related Classifications

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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