[CAS NO. 1265229-25-1] Zoligratinib
PRODUCTS SPECIFICATIONS [1265229-25-1]
DESCRIPTION [1265229-25-1]
Overview
| MDL | MFCD28502053 |
|---|---|
| Molecular Weight | 356.38 |
| Molecular Formula | C20H16N6O |
| SMILES | O=C(C1=C(N)N(C2=CC=C3N=C(C)NC3=C2)N=C1)C(N4)=CC5=C4C=CC=C5 |
2 Publications Citing Use of MCE
Summary
IC50 & Target
|
FGFR1 9.3 nM (IC 50 ) |
FGFR2 7.6 nM (IC 50 ) |
FGFR3 22 nM (IC 50 ) |
FGFR4 290 nM (IC 50 ) |
In Vitro
Zoligratinib is well balanced in cellular antiproliferative activity against SNU-16 and stability in human liver microsome. The selectivity of 8 to inhibit FGFR over KDR is suggested to be caused by the difference in the interaction with M535 in FGFR1 and L889 in KDR [1] . The IC 50 of Zoligratinib is 29 nM for FGF-dependent proliferation and 780 nM for VEGF-dependent proliferation [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Zoligratinib treatment shows a dose-dependent tumor regression (tumor growth inhibition (TGI)=106% at 30 mg/kg and 147% at 100 mg/kg) without apparent body weight loss. Zoligratinib treatment also shows significant in vivo efficacy in xenograft mice models with FGFR genetic alterations, such as KG1 (leukemia, FGFR1OP-FGFR1 fusion), MFE280 (endometrial cancer, FGFR2 S252W mutation), UM-UC-14 (bladder cancer, FGFR3 S249C mutation), and RT112/84 (bladder cancer, FGFR3-TACC3 fusion) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT03834220 | Debiopharm International SA|Caris Life Sciences|Optimal Research (Just In Time sites) |
Solid Tumor
|
March 22, 2019 | Phase 2 |
| NCT03344536 | Memorial Sloan Kettering Cancer Center|Debiopharm International SA |
Breast Cancer
|
November 10, 2017 | Phase 1|Phase 2 |
| NCT01948297 | Debiopharm International SA |
Solid Tumours
|
August 2013 | Phase 1 |
Appearance
Solid
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
DMSO : 25 mg/mL ( 70.15 mM ; ultrasonic and warming and heat to 50°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.8060 mL | 14.0300 mL | 28.0599 mL |
| 5 mM | 0.5612 mL | 2.8060 mL | 5.6120 mL |
| 10 mM | 0.2806 mL | 1.4030 mL | 2.8060 mL |
References
- [1] Nakanishi Y, et al. The fibroblast growth factor receptor genetic status as a potential predictor of the sensitivity to CH5183284/Debio 1347, a novel selective FGFR inhibitor. Mol Cancer Ther. 2014 Nov;13(11):2547-58.
- [2] Nakanishi Y, et al. Mechanism of Oncogenic Signal Activation by the Novel Fusion Kinase FGFR3-BAIAP2L1. Mol Cancer Ther. 2015 Mar;14(3):704-12.
- [3] Nakanishi Y, et al. ERK Signal Suppression and Sensitivity to CH5183284/Debio 1347, a Selective FGFR Inhibitor. Mol Cancer Ther. 2015 Dec;14(12):2831-9.