DCC-2618 (Synonyms: DCC2618;DCC 2618) |
| Catalog No.GC11171 |
A dual inhibitor of c-Kit and c-MET
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1225278-16-9
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
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Cell lines |
CHO and GIST cells |
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Preparation method |
Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reaction Conditions |
43 ~ 106 nM for CHO cells, 2 ~ 32 nM for GIST cells |
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Applications |
In CHO cells, DCC-2618 inhibited resistant Exon 17 KIT mutations with the IC50 values ranging from 43 to 106 nM. In GIST cells, DCC-2618 inhibited mutant KIT with the IC50 values ranging from 2 to 32 nM. |
| Animal experiment [1]: | |
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Animal models |
GIST xenografts |
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Dosage form |
25 and 50 mg/kg; p.o. |
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Applications |
DCC-2618 inhibited KIT in GIST xenografts after single dose. At the doses of 25 and 50 mg/kg, DCC-2618 showed promising potency on pKIT (Y703) with the inhibition ranging from 39% to 79% 2 ~ 12 hrs after the administration. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. DCC-2618, a small molecule inhibitor of normal and mutant KIT kinasefor treatment of refractory gastrointestinal stromal tumors (GIST)Deciphera Pharmaceuticals, Lawrence, KS. | |
| Cas No. | 1225278-16-9 | SDF | |
| Synonyms | DCC2618;DCC 2618 | ||
| Chemical Name | 1-N'-[2,5-difluoro-4-[2-(1-methylpyrazol-4-yl)pyridin-4-yl]oxyphenyl]-1-N-phenylcyclopropane-1,1-dicarboxamide | ||
| Canonical 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 | ||
| Formula | C26H21F2N5O3 | M.Wt | 489.47 |
| Solubility | >179.2mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.043 mL | 10.2151 mL | 20.4303 mL |
| 5 mM | 0.4086 mL | 2.043 mL | 4.0861 mL |
| 10 mM | 0.2043 mL | 1.0215 mL | 2.043 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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