BFH772
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1300 | Check With Us |
| 500mg | $1900 | Check With Us |
| 1g | $2850 | Check With Us |
: Cat #: V2674 CAS #: 890128-81-1 Purity ≥ 98%
Description: BFH772 (also known as BFH-772) is a novel and potent orally bioavailable VEGFR2 inhibitor that targets VEGFR2 kinase with IC50 of 3 nM.
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| Molecular Weight (MW) | 439.39 |
|---|---|
| Molecular Formula | C23H16F3N3O3 |
| CAS No. | 890128-81-1 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 87 mg/mL (198.0 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 87 mg/mL (198.0 mM) | |
| SMILES Code | O=C(C1=C2C=CC(OC3=NC=NC(CO)=C3)=CC2=CC=C1)NC4=CC=CC(C(F)(F)F)=C4 |
| Synonyms | BFH 772; BFH-772; BFH772 |
| Protocol | In Vitro | BFH772 is highly selective; apart from inhibiting VEGFR2 at 3 nM IC50, it also targets B-RAF, RET, and TIE-2, albeit with at least 40-fold lower potency. BFH772 is inactive (IC50>10 μM; >2 μM for cKIT) against all other tyrosine specific- and serine/threonine-specific protein kinases tested. BFH772 inhibits VEGFR2 with IC50 of 4.6±0.6 nM in CHO cells. BFH772 inhibits VEGFR2 with IC50 of 3 nM in HUVEC cells. BFH772 inhibits the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases, with IC50 values ranging between 30 and 160 nM. BFH772 is selective (IC50 values >0.5 μM) against the kinases of EGFR, ERBB2, INS-R, and IGF-1R and against the cytoplasmic BCR-ABL kinase. IC50 of BFH772 (<0.01 nM, n=2) demonstrates that they abrogated VEGF induced proliferation at remarkably low nM concentrations. |
|---|---|---|
| In Vivo | BFH772 at 3 mg/kg orally dosed once per day potently inhibits melanoma growth (by 54-90% for primary tumor and 71-96% for metastasis growth) as depicted by treatment to control ratios. Dose–response curves of BFH772 at 0.3, 1, and 3 mg/kg demonstrate that even at the lowest concentrations, this naphthalene-1-carboxamide inhibits VEGF induced tissue weight and TIE-2 levels but only reaches statistical significance at 1 mg/kg and above. |
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 | 2.2759 mL | 11.3794 mL | 22.7588 mL | 45.5176 mL |
| 5mM | 0.4552 mL | 2.2759 mL | 4.5518 mL | 9.1035 mL |
| 10mM | 0.2276 mL | 1.1379 mL | 2.2759 mL | 4.5518 mL |
| 20mM | 0.1138 mL | 0.5690 mL | 1.1379 mL | 2.2759 mL |
The molarity calculator equation
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The dilution calculator equation
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
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%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
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Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
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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.