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c-Kit-IN-1

Catalog No. T4332 CAS 1225278-16-9

Synonyms: PDGFR inhibitor 1, DCC-2618

c-Kit-IN-1 (DCC-2618) is an effective inhibitor of c-Met and c-Kit (IC50s<200 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

c-Kit-IN-1, CAS 1225278-16-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 147.00
25 mg	In stock	$ 320.00
50 mg	In stock	$ 571.00
100 mg	In stock	$ 819.00
500 mg	In stock	$ 1,690.00
1 mL * 10 mM (in DMSO)	In stock	$ 95.00

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Purity: 98.72%

Purity: 98.16%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	c-Kit-IN-1 (DCC-2618) is an effective inhibitor of c-Met and c-Kit (IC50s<200 nM).
Targets&IC50	c-Kit:<200 nM, c-Met:<200 nM
In vitro	DCC-2618 also inhibits KDR and PDGFR α/β (IC50s: <2 μM, <10 μM and <10 μM).
Kinase Assay	The 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 A340 nM) is continuously monitored spectrophotometrically. 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., DCC-2618) 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).
Cell Research	DCC-2618 is prepared in DMSO and stored, and then diluted with the appropriate medium before use.A serial dilution of test compounds (e.g., DCC-2618) is 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.

Synonyms	PDGFR inhibitor 1, DCC-2618
Molecular Weight	489.47
Formula	C26H21F2N5O3
CAS No.	1225278-16-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 88 mg/mL(179.8 mM)

References and Literature

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

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Approved Drug Library Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Inhibitor Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library FDA-Approved Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Cytokine Inhibitor Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

c-Kit-IN-1 1225278-16-9 Tyrosine Kinase/Adaptors c-Met/HGFR c-Kit PDGFR inhibitor 1 CD117 DCC-2618 Inhibitor DCC 2618 DCC2618 cKitIN1 SCFR inhibit c Kit IN 1 inhibitor

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