FGFR1/DDR2 inhibitor 1

Name: FGFR1/DDR2 inhibitor 1
Brand: MedChemExpress
SKU: HY-114311
Rating: 4.5 (1 reviews)

Cat. No.: HY-114311 Purity: 98.26%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

FGFR1/DDR2 inhibitor 1 Chemical Structure

CAS No. : 2308497-58-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 309	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 309	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 740	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1020	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1490	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE FGFR1/DDR2 inhibitor 1

•Arch Pharm (Weinheim). 2024 Sep;357(9):e2400066. [Abstract]

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FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

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DDR1 DDR2

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

FGFR1

31.1 nM (IC₅₀)

DDR2

3.2 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
KG-1	IC₅₀	108.4 nM Compound: 11k	Antiproliferative activity against human KG1 cells after 72 hrs by CCK8 assay Antiproliferative activity against human KG1 cells after 72 hrs by CCK8 assay	[PMID: 30572178]
KG-1	IC₅₀	108.4 nM Compound: 11k	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	[PMID: 30572178]
NCI-H2286	IC₅₀	93 nM Compound: 11k	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	[PMID: 30572178]
NCI-H2286	IC₅₀	93 nM Compound: 11k	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	[PMID: 30572178]
NCI-H716	IC₅₀	31.8 nM Compound: 11k	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	[PMID: 30572178]
SNU-16	IC₅₀	93.4 nM Compound: 11k	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	[PMID: 30572178]

In Vitro

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.

In Vivo

FGFR1/DDR2 inhibitor 1 (10-20 mg/kg; p.o.; once daily for 7 days) has profound anti-tumor efficacy in NCI-H1581 tumor model^[1].
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.

Animal Model:	Nude mice bearing NCI-H1581 tumors^[1]
Dosage:	10 or 20 mg/kg
Administration:	P.o.; once daily for 7 days
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.

Molecular Weight

501.50

Formula

C₂₈H₂₂F₃N₅O

CAS No.

2308497-58-5

Appearance

Solid

Color

Off-white to light yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9940 mL	9.9701 mL	19.9402 mL
5 mM	0.3988 mL	1.9940 mL	3.9880 mL
10 mM	0.1994 mL	0.9970 mL	1.9940 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 98.26%

Select Batch:

Data Sheet (272 KB) SDS (251 KB)

COA (248 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. Wang Q, et al. Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma. Eur J Med Chem. 2019 Feb 1;163:671-689. [Content Brief]

Complete Stock Solution Preparation Table

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