2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. SSR128129E

SSR128129E is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.

For research use only. We do not sell to patients.

SSR128129E Chemical Structure

SSR128129E Chemical Structure

CAS No. : 848318-25-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 121 In-stock
Solution
10 mM * 1 mL in DMSO USD 121 In-stock
Solid
5 mg USD 70 In-stock
10 mg USD 110 In-stock
25 mg USD 220 In-stock
50 mg USD 350 In-stock
100 mg USD 550 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of SSR128129E:

SSR128129E Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE SSR128129E

View All FGFR Isoform Specific Products:

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FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

SSR128129E is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.

IC50 & Target[1]

FGFR1

1.9 μM (IC50)

FGFR2

 

FGFR3

 

FGFR4

 

In Vitro

SSR128129E inhibits FGF2-induced EC proliferation with an IC50 of 31±1.6 nM, migration with an IC50 of 15.2±4.5 nM, and lamellipodia formation in a dose dependent manner. SSR128129E inhibits responses mediated by FGFR1-4. For instance, SSR128129E blocks EC migration in response to FGF1, a ligand of FGFR1 and FGFR4, and capillary tube formation in response to FGF19, a ligand of FGFR4. Proliferation and migration of the murine pancreatic Panc02 tumor cell line in response to FGF7 are also blocked by SSR128129E, showing that SSR128129E inhibits FGFR subtypes of other species as well. SSR128129E blocks different FGFR subtypes in various cell lines with nanomolar potency[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SSR128129E Related Antibodies
In Vivo

Oral delivery of SSR128129E (30 mg/kg/day, from day 3) inhibits growth of orthotopic Panc02 tumors by 44% and delays growth of Lewis lung carcinoma. oral SSR128129E (30 mg/kg/day, from day 5) reduces tumor size and weight by 53% and 40%, respectively. SSR128129E inhibits the growth of subcutaneous CT26 colon tumors by 34% and of the multidrug resistant MCF7/ADR breast cancer xenograft model by 40%. SSR128129E reduces tumor invasiveness and metastasis of Panc02 tumor cells to peritoneal lymph nodes[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

346.31

Formula

C18H15N2NaO4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(O[Na])C1=CC(C(C2=C(C)C(OC)=C3C=CC=CN23)=O)=CC=C1N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 54 mg/mL (155.93 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8876 mL 14.4379 mL 28.8759 mL
5 mM 0.5775 mL 2.8876 mL 5.7752 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 (sealed storage, away from moisture). 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.22 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.22 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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
References
Cell Assay
[1]

HUVECs, freshly isolated from different donors and used between passage two and five, are cultured in M199 medium supplemented with 20% fetal bovine serum (FBS), 2 mM L-glutamine, 30 mg/L endothelial cell growth factor supplements (EGCS), 10 units/mL heparin, and penicillin/streptomycin. For proliferation, ECs are starved overnight in growth factor-depleted M199 medium containing 2% FBS and stimulated for 24 hr with 10 ng/mL bFGF with SSR128129E or DMSO. Proliferation is assessed the last 2 hr by incubation with 1 μCi/mL [3H]thymidine[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice: Anesthetized BALB/c mice are inoculated with murine 4T1 mammary carcinoma cells. After randomization of tumor bearing mice for tumor size on day 5 after tumor cell inoculation, SSR128129E or vehicle (0.6 % methylcellulose) is administered daily via oral gavage at a dose of 30 mg/kg until the end of the experiment at day 21. Tumor volume is measured. At the end of the experiment, mice are sacrificed by pentobarbital injection, and lungs and tumors are dissected. Visible metastatic nodules on the lungs are counted by using a dissecting microscope[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 (sealed storage, away from moisture). 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 2.8876 mL 14.4379 mL 28.8759 mL 72.1897 mL
5 mM 0.5775 mL 2.8876 mL 5.7752 mL 14.4379 mL
10 mM 0.2888 mL 1.4438 mL 2.8876 mL 7.2190 mL
15 mM 0.1925 mL 0.9625 mL 1.9251 mL 4.8126 mL
20 mM 0.1444 mL 0.7219 mL 1.4438 mL 3.6095 mL
25 mM 0.1155 mL 0.5775 mL 1.1550 mL 2.8876 mL
30 mM 0.0963 mL 0.4813 mL 0.9625 mL 2.4063 mL
40 mM 0.0722 mL 0.3609 mL 0.7219 mL 1.8047 mL
50 mM 0.0578 mL 0.2888 mL 0.5775 mL 1.4438 mL
60 mM 0.0481 mL 0.2406 mL 0.4813 mL 1.2032 mL
80 mM 0.0361 mL 0.1805 mL 0.3609 mL 0.9024 mL
100 mM 0.0289 mL 0.1444 mL 0.2888 mL 0.7219 mL
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SSR128129E Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SSR128129E848318-25-2SSRFGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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