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| Size | Price | Stock |
|---|---|---|
| 250mg | $1250 | Check With Us |
| 500mg | $1850 | Check With Us |
| 1g | $2775 | Check With Us |
: Cat #: V3288 CAS #: 1708971-55-4 Purity ≥ 98%
Description: Roblitinib (FGF-401) is a potent and highly selective inhibitor of human fibroblast growth factor receptor 4 (FGFR4) with an IC50 of 1.9 nM and with potential antineoplastic/anticancer activity.
References: Nicole Buschmann, et al. Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors. WO2015059668A1.
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| Molecular Weight (MW) | 506.57 |
|---|---|
| Molecular Formula | C25H30N8O4 |
| CAS No. | 1708971-55-4 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 10 mg/mLr |
| Water: N/Ar | |
| Ethanol: N/A | |
| SMILES Code | CN1CC(N(CC2=CC(CCCN3C(NC4=CC(NCCOC)=C(C#N)C=N4)=O)=C3N=C2C=O)CC1)=O |
| Synonyms | Roblitinib; FGF401; FGF-401; FGF 401 |
| Protocol | In Vitro | Roblitinib inhibits HUH7 (IC50=12 nM), Hep3B (IC50=9 nM), JHH7 (IC50=9 nM), HEPG2 (IC50>10 uM), JHH (IC50>10 uM). Roblitinib shows no activity FGFR1, FGFR2, FGFR3, rat FGFR4, C552A FGFR4 (all IC50>10 uM). Roblitinib (FGF-401; Compound Example 83) is a highly selective and potent FGFR4 inhibitor (IC50= 1.9 nM). |
|---|---|---|
| In Vivo | Roblitinib (iv at 0.5 mg/kg; po at 3 mg/kg) has a T1/2 of 4.4 hours, a CL of 19 mL/min•kg, and a Vss of 3.9 L/kg for male SD rats. Roblitinib (iv at 1 mg/kg; po at 3 mg/kg) has a T1/2 of 1.4 hours, a CL of 28 mL/min•kg, and a Vss of 2.3 L/kg for Male mice (C57BL/6). Roblitinib causes blood concentrations dropped below the IC90 threshold level within 8 h of dosing, and controlles tumor growth to the level of stasis at the lowest dose of 10 mg/kg for 6 days. Roblitinib (gavage; 10-100 mg/kg; b.i.d.; for 10 days) with the 30 mg/kg has the maximal level of inhibition of FGFR4-dependent tumor growth in the Hep3B xenograft model. |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.9741 mL | 9.8703 mL | 19.7406 mL | 39.4812 mL |
| 5mM | 0.3948 mL | 1.9741 mL | 3.9481 mL | 7.8962 mL |
| 10mM | 0.1974 mL | 0.9870 mL | 1.9741 mL | 3.9481 mL |
| 20mM | 0.0987 mL | 0.4935 mL | 0.9870 mL | 1.9741 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.