Agerafenib (CEP-32496; RXDX-105; AC013773)
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 |
|---|---|---|
| 100mg | $600 | Check With Us |
| 500mg | $1850 | Check With Us |
| 1g | $2775 | Check With Us |
: Cat #: V1013 CAS #: 1188910-76-0 Purity ≥ 98%
Description: Agerafenib (formerly RXDX105; AC013773; RXDX-105; CEP-32496; AC-01377) is a potent and orally bioactive inhibitor of BRAFV600E and c-Raf with potential antitumor activity.
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| Molecular Weight (MW) | 517.46 |
|---|---|
| Molecular Formula | C24H22F3N5O5 |
| CAS No. | 1188910-76-0 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 9 mg/mL (17.4 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| Solubility In Vivo | 15% Captisol: 15 mg/mL |
| SMILES Code | O=C(NC1=NOC(C(C)(C)C(F)(F)F)=C1)NC2=CC=CC(OC3=C4C=C(OC)C(OC)=CC4=NC=N3)=C2 |
| Synonyms | Agerafenib; CEP32496; CEP 32496; RXDX 105; RXDX105; AC013773; RXDX-105; CEP-32496; AC 013773; AC-013773. |
| Protocol | In Vitro | Agerafenib (CEP-32496) exhibits high potency against several BRAFV600E-dependent cell lines and selective cytotoxicity for tumor cell lines expressing mutant BRAFV600E versus those containing wild-type BRAF. Agerafenib exhibits potent binding (BRAFV600E Kd=14 nM) and cellular activity (pMEK IC50=82 nM and A375 proliferation IC50=78 nM), with activity in the proliferation assay. Agerafenib also exhibits a favorable CYP450 inhibition profile, with measured IC50 values greater than 10 μM versus the CYP1A2, CYP2C9, CYP2D6, and CYP3A4 isoforms and an IC50=3.4 μM versus CYP2C19. |
|---|---|---|
| In Vivo | Oral administration of Agerafenib (CEP-32496) to Colo-205 tumor xenograft-bearing mice results in significant inhibition of pMEK in tumor cell lysates. For instance, a single 30 mg/kg (po) dose of Agerafenib leads to a 50 and 75% inhibition of normalized pMEK in tumor lysates at the 2 and 6 h postdose time point, respectively (p<0.03), while a 55 mg/kg (po) dose resulted in a 75% to 57% (p<0.03) inhibition of pMEK at 2 through 10 h post administration, with normalization to baseline by 24 h. Agerafenib exhibits an exceptional PK profile in mouse, dog, and cynomolgus monkey. Administration of Agerafenib to beagle dogs (single dose of 1 mg/kg iv and 10 mg/kg po) results in low clearance (CL=5.0 (mL/min)/kg) and excellent bioavailability (%F=100). Similarly, in cynomolgus monkey, the administration of Agerafenib (single dose of 1 mg/kg iv and 10 mg/kg po) leads to high oral exposure due to low clearance (CL=6.7 mL/min/kg) and excellent bioavailability (%F=100). |
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 | 1.9325 mL | 9.6626 mL | 19.3252 mL | 38.6503 mL |
| 5mM | 0.3865 mL | 1.9325 mL | 3.8650 mL | 7.7301 mL |
| 10mM | 0.1933 mL | 0.9663 mL | 1.9325 mL | 3.8650 mL |
| 20mM | 0.0966 mL | 0.4831 mL | 0.9663 mL | 1.9325 mL |
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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
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,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.