FGFR1/DDR2 inhibitor 1
Based on 2 publication(s) in Google Scholar
FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM and 3.2 nM, respectively. Antitumor activity.
For research use only. We do not sell to patients.
- Purity: 98.26%
- CAS No.: 2308497-58-5
- Formula: C28H22F3N5O
- Molecular Weight:501.50
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) FGFR1/DDR2 inhibitor 1
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Biological Activity
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FGFR1 31.1 nM (IC50) |
DDR2 3.2 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KG-1 | IC50 |
108.4 nM
Compound: 11k
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Antiproliferative activity against FGFR1 fused human KG1 cells after 72 hrs by CCK8 assay
Antiproliferative activity against FGFR1 fused human KG1 cells after 72 hrs by CCK8 assay
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[PMID: 30572178] |
| KG-1 | IC50 |
108.4 nM
Compound: 11k
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Antiproliferative activity against human KG1 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human KG1 cells after 72 hrs by CCK8 assay
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[PMID: 30572178] |
| NCI-H2286 | IC50 |
93 nM
Compound: 11k
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Antiproliferative activity against human NCI-H2286 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human NCI-H2286 cells after 72 hrs by CCK8 assay
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[PMID: 30572178] |
| NCI-H2286 | IC50 |
93 nM
Compound: 11k
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Antiproliferative activity against human NCI-H2286 cells harboring DDR2 mutation after 72 hrs by CCK8 assay
Antiproliferative activity against human NCI-H2286 cells harboring DDR2 mutation after 72 hrs by CCK8 assay
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[PMID: 30572178] |
| NCI-H716 | IC50 |
31.8 nM
Compound: 11k
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Antiproliferative activity against FGFR2 amplified human NCI-H716 cells after 72 hrs by CCK8 assay
Antiproliferative activity against FGFR2 amplified human NCI-H716 cells after 72 hrs by CCK8 assay
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[PMID: 30572178] |
| SNU-16 | IC50 |
93.4 nM
Compound: 11k
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Antiproliferative activity against FGFR2 amplified human SNU16 cells after 72 hrs by CCK8 assay
Antiproliferative activity against FGFR2 amplified human SNU16 cells after 72 hrs by CCK8 assay
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[PMID: 30572178] |
FGFR1/DDR2 inhibitor 1 (compound 11k) (25-200 μM; 2 hours) shows significant inhibition of FGFR2 phosphorylation in a dose-dependent manner in SNU16 cells. FGFR1/DDR2 inhibitor 1 shows (60-250 μM; 2 hours) significant inhibition of DDR2 phosphorylation in a dose-dependent manner in H2286 cells[1].
FGFR1/DDR2 inhibitor 1 significantly inhibits the proliferation of FGFR-driven cancer cell lines with IC50s of 108.4, 93.4, 31.8 and 306.6 nM against KG-1, SNU-16, NCI-H716 and UMUC14 respectively. FGFR1/DDR2 inhibitor 1 demonstrates substantially activity against the DDR2-driven cancer cell line NCI-H2286 (93.0 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SCID mice bearing NCI-H2286 tumors were randomized and treated with FGFR1/DDR2 inhibitor 1 at doses of 10 mg/kg for 10 consecutive days. FGFR1/DDR2 inhibitor 1 could suppress tumor growth with tumor growth inhibition rates (TGI) of 82.8%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice bearing NCI-H1581 tumors[1]
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Dosage:10 or 20 mg/kg
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Administration:P.o.; once daily for 7 days
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Result:Suppressed tumor growth in a dose-dependent manner with tumor growth inhibition rates (TGI) of 59.7% and 98.1% at doses of 10 and 20 mg/kg, respectively.
Chemical Information
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CAS No. 2308497-58-5
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Appearance Solid
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Molecular Weight 501.50
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Formula C28H22F3N5O
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Color Off-white to light yellow
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SMILES
O=C(NC1=CC=CC(C(F)(F)F)=C1)C2=CC=C(C)C(C3=CC4=C(C=C3)C(C5=CN(C6CC6)N=C5)=NN4)=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Signal
ARTN drives CD8+ T cell exhaustion via the GFRα3-RET-PI3K/AKT Axis to promote TNBC progression. [Abstract]2026 May:141:112397. PMID: 41610967 -
Arch Pharm (Weinheim)
Discovery of potent CSK inhibitors through integrated virtual screening and molecular dynamic simulation. [Abstract]2024 Sep;357(9):e2400066. PMID: 38809025
Solvent & Solubility
DMSO : 250 mg/mL (498.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.15 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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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 | 1.9940 mL | 9.9701 mL | 19.9402 mL | 49.8504 mL |
| 5 mM | 0.3988 mL | 1.9940 mL | 3.9880 mL | 9.9701 mL | |
| 10 mM | 0.1994 mL | 0.9970 mL | 1.9940 mL | 4.9850 mL | |
| 15 mM | 0.1329 mL | 0.6647 mL | 1.3293 mL | 3.3234 mL | |
| 20 mM | 0.0997 mL | 0.4985 mL | 0.9970 mL | 2.4925 mL | |
| 25 mM | 0.0798 mL | 0.3988 mL | 0.7976 mL | 1.9940 mL | |
| 30 mM | 0.0665 mL | 0.3323 mL | 0.6647 mL | 1.6617 mL | |
| 40 mM | 0.0499 mL | 0.2493 mL | 0.4985 mL | 1.2463 mL | |
| 50 mM | 0.0399 mL | 0.1994 mL | 0.3988 mL | 0.9970 mL | |
| 60 mM | 0.0332 mL | 0.1662 mL | 0.3323 mL | 0.8308 mL | |
| 80 mM | 0.0249 mL | 0.1246 mL | 0.2493 mL | 0.6231 mL | |
| 100 mM | 0.0199 mL | 0.0997 mL | 0.1994 mL | 0.4985 mL |
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