DCC-2618

C-Kit/PDGFR inhibtor CAS# 1225278-16-9

DCC-2618

Catalog No. BCC1520----Order now to get a substantial discount!

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Chemical structure

DCC-2618

3D structure

Chemical Properties of DCC-2618

Cas No. 1225278-16-9 SDF Download SDF
PubChem ID 46208890 Appearance Powder
Formula C26H21F2N5O3 M.Wt 489.47
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 100 mg/mL (204.30 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 1-N'-[2,5-difluoro-4-[2-(1-methylpyrazol-4-yl)pyridin-4-yl]oxyphenyl]-1-N-phenylcyclopropane-1,1-dicarboxamide
SMILES CN1C=C(C=N1)C2=NC=CC(=C2)OC3=C(C=C(C(=C3)F)NC(=O)C4(CC4)C(=O)NC5=CC=CC=C5)F
Standard InChIKey WWOXKWLDMLMYQY-UHFFFAOYSA-N
Standard InChI InChI=1S/C26H21F2N5O3/c1-33-15-16(14-30-33)21-11-18(7-10-29-21)36-23-13-19(27)22(12-20(23)28)32-25(35)26(8-9-26)24(34)31-17-5-3-2-4-6-17/h2-7,10-15H,8-9H2,1H3,(H,31,34)(H,32,35)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of DCC-2618

DescriptionDCC-2618 is a small-molecule inhibitor of KIT kinases with IC50 values of 6 nM, 9 nM, 18 nM, 5 nM, 14 nM and 9 nM for wt c-KIT, KIT V654A, KIT T670I, KIT D816H, KIT D816V and KIT JMD ΔVV/D816V respectively.
Targetswt c-KITKIT V654AKIT T670IKIT D816HKIT D816VKIT JMD ΔVV/D816V
IC506 nM9 nM18 nM5 nM14 nM9 nM

Protocol

Kinase Assay [1]
Activity of c-KIT kinase is determined by following the production of ADP from the kinase reaction through coupling with the pyruvate kinase/lactate dehydrogenase system. In this assay, the oxidation of NADH (thus the decrease at A340nm) is continuously monitored spectrophometrically. The reaction mixture (100 μL) contained c-KIT (cKIT residues T544-V976, from ProQinase, 5.4 nM), polyE4Y (1 mg/mL), MgC12 (10 mM), pyruvate kinase (4 units), lactate dehydrogenase (0.7 units), phosphoenol pyruvate (1 mM), and NADH (0.28 mM) in 90 mM Tris buffer containing 0.2 % octyl-glucoside and 1% DMSO, pH 7.5. Test compounds (e.g., c-Kit-IN-1) are incubated with c-KIT and other reaction reagents at 22°C for <2 min before ATP (200 μM) is added to start the reaction. The absorption at 340 nm is monitored continuously for 0.5 hours at 30°C on Polarstar Optima plate reader (BMG). The reaction rate is calculated using the 0 to 0.5 h time frame. Percent inhibition is obtained by comparison of reaction rate with that of a control (i.e. with no test compound). IC50 values are calculated from a series of percent inhibition values determined at a range of inhibitor concentrations using software routines as implemented in the GraphPad Prism software package[1].

Cell Assay [1]
A serial dilution of test compounds (e.g., c-Kit-IN-1) are dispensed into a 96-well black clear bottom plate. For each cell line, five thousand cells are added per well in 200 μL complete growth medium. Plates are incubated for 67 hours at 37 degrees Celsius, 5% CO2, 95% humidity. At the end of the incubation period 40 μL of a 440 μM solution of resazurin in PBS is added to each well and incubated for an additional 5 hours at 37 degrees Celsius, 5% CO2, 95% humidity. Plates are read on a Synergy2 reader using an excitation of 540 nM and an emission of 600 nM. Data is analyzed using Prism software to calculate IC50 values[1].

References:
[1]. Daniel L. Flynn, et al. Cyclopropane amides and analogs exhibiting anti-cancer and anti-proliferative activities. WO 2010051373 A1

DCC-2618 Dilution Calculator

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DCC-2618 Molarity Calculator

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Preparing Stock Solutions of DCC-2618

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.043 mL 10.2151 mL 20.4303 mL 40.8605 mL 51.0757 mL
5 mM 0.4086 mL 2.043 mL 4.0861 mL 8.1721 mL 10.2151 mL
10 mM 0.2043 mL 1.0215 mL 2.043 mL 4.0861 mL 5.1076 mL
50 mM 0.0409 mL 0.2043 mL 0.4086 mL 0.8172 mL 1.0215 mL
100 mM 0.0204 mL 0.1022 mL 0.2043 mL 0.4086 mL 0.5108 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on DCC-2618

IC50: 6 nM, 9 nM, 18 nM, 5 nM, 14 nM and 9 nM for wt c-KIT, KIT V654A, KIT T670I, KIT D816H, KIT D816V and KIT JMD ΔVV/D816V, respectively.

DCC-2618 is a small-molecule inhibitor of KIT kinases.

Gastrointestinal stromal tumors (GIST) are driven by gain-of-function mutations of the KIT (approx 90%) or PDGFR (approx 10%) receptor tyrosine kinases. DCC-2618 has been designed to effectively inhibit the imatinib and sunitinib-sensitive KIT juxtamenbrane domin mutants as well as secondary resistant KIT iniase-domain mutants.

In vitro: DCC-2618 is a kinase switch inhibitor that can control drug resistant mutants of KIT and PDGFR in GIST. DCC-2618 acts by imposing an inactive conformation (shape) of highly resistant and aggressive secondary mutations of KIT kinase [1].

In vivo: DCC-2618 inhibits KIT in GIST tumor xenografts after single dose. At the doses of 50 and 25 mpk, DCC-2618 showed promising potency on pKIT (Y703) with the inhibition ranging from 39% to 79% 2-12 hrs after the administration [1].

Clinical trial: A Phase I trial with refractory GIST patients is planned.

Reference:
[1] DCC-2618, a small molecule inhibitor of normal and mutant KIT kinasefor treatment of refractory gastrointestinal stromal tumors (GIST)Deciphera Pharmaceuticals, Lawrence, KS. 

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References on DCC-2618

BLU-285, DCC-2618 Show Activity against GIST.[Pubmed:28077435]

Cancer Discov. 2017 Feb;7(2):121-122.

Tyrosine kinase inhibitors may initially control gastrointestinal stromal tumors, but most patients eventually experience disease progression due to activation loop mutations, which are resistant to approved drugs. However, phase I trials suggest that the cancer is sensitive to two new agents: BLU-285 and DCC-2618. In addition, liquid biopsies, which were used to follow patients during the trials, may be valuable tools in tracking disease progression and assessing tumor heterogeneity.

Description

c-Kit-IN-1 is a potent inhibitor of c-Kit and c-Met with IC50s of <200 nM.

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