Infigratinib phosphate
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 250mg | $680 | Check With Us |
| 500mg | $1150 | Check With Us |
| 1g | $1725 | Check With Us |
: Cat #: V4255 CAS #: 1310746-10-1 Purity ≥ 98%
Description: Infigratinib phosphate (formerly BGJ-398; BGJ398; NVP-BGJ398 phosphate; Truseltiq), the phosphate salt of Infigratinib, is an orally bioavailable FGFR (fibroblast growth factor receptors) inhibitor that has gained FDA approval in May 2021 to treat cholangiocarcinoma whose disease meets certain criteria.
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- Physicochemical and Storage Information
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- Related Biological Data
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| Molecular Weight (MW) | 658.47 |
|---|---|
| Molecular Formula | C26H34Cl2N7O7P |
| CAS No. | 1310746-10-1 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 10 mMr |
| Water: N/Ar | |
| Ethanol: N/A | |
| Solubility In Vivo | 30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/kg |
| SMILES Code | O=C(NC1=C(Cl)C(OC)=CC(OC)=C1Cl)N(C2=NC=NC(NC3=CC=C(N4CCN(CC)CC4)C=C3)=C2)C.O=P(O)(O)O |
| Synonyms | NVP-BGJ398 phosphate, NVP-BGJ-398; Truseltiq; BGJ398; NVPBGJ 398; NVP-BGJ 398; BGJ-398; NVP BGJ 398; NVPBGJ-398; BG J398; Infigratinib phosphate; 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea phosphate. |
| Protocol | In Vitro | Infigratinib phosphate inhibits FGFR1, FGFR2, and FGFR3 with IC50=~1 nM, FGFR3K650E with IC50=4.9 nM, and FGFR4 with IC50=60 nM. IC50 values for all other kinases are in the μM range (FYN, LCK, YES, and ABL, IC50=1.9, 2.5, 1.1, and 2.3 μM, respectively) except for VEGFR2, KIT, and LYN, which are inhibited at submicromolar concentrations (IC50=0.18, 0.75, and 0.3 μM, respectively). Infigratinib inhibits the proliferation of the FGFR1-, FGFR2-, and FGFR3-dependent BaF3 cells with IC50 values which are in the low nanomolar range and comparable to those observed for the inhibition of the receptors kinase activity in the enzymatic assay. For the remaining cells, all IC50 values are greater than 1.5 μM except for VEGFR2 (IC50 1449 and 938 nM), for which there is at least a 400-fold selectivity versus FGFR1, FGFR2, and FGFR3. |
|---|---|---|
| In Vivo | Infigratinib is administered to athymic nude mice implanted subcutaneously with RT112/luc1 tumors: either as a 5 mg/kg intravenous bolus in NMP/PEG200 (1:9, v/v) or orally by gavage as a suspension in PEG300/D5W (2:1, v/v) at a 20 mg/kg dose. The relevant pharmacokinetic (PK) parameters indicate that the oral bioavailability of Infigratinib in this study is 32%. After intravenous dosing, Infigratinib shows a rapid distribution from the vascular compartment into the peripheral tissues, translating into a high volume of distribution (26 L/kg). The plasma clearance is high at 3.3 L/h/kg (61% of liver blood flow). The ratio of tumor to plasma after oral dosing based on AUC is determined to be 10. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.5187 mL | 7.5934 mL | 15.1867 mL | 30.3734 mL |
| 5mM | 0.3037 mL | 1.5187 mL | 3.0373 mL | 6.0747 mL |
| 10mM | 0.1519 mL | 0.7593 mL | 1.5187 mL | 3.0373 mL |
| 20mM | 0.0759 mL | 0.3797 mL | 0.7593 mL | 1.5187 mL |
The molarity calculator equation
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The dilution calculator equation
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This equation is commonly abbreviated as: C1 V1 = C2 V2
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid concentration
mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (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.