Canertinib (CI-1033; PD-183805)
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 |
|---|---|---|
| 500mg | $280 | Check With Us |
| 1g | $450 | Check With Us |
| 5g | $1140 | Check With Us |
: Cat #: V0539 CAS #: 267243-28-7 Purity ≥ 98%
Description: Canertinib (formerly CI-1033; CI1033; PD183805; PD-183805) is an irreversible/covalent, quinazoline-based and orally bioavailable pan-ErbB inhibitor for EGFR and ErbB2 with potential antineoplastic activity.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 485.94 |
|---|---|
| Molecular Formula | C24H25ClFN5O3 |
| CAS No. | 267243-28-7 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 9 mg/mL (18.5 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 2 mg/mL (4.1 mM) | |
| Solubility In Vivo | 30% propylene glycol, 5% Tween 80, 65% D5W: 10mg/mL |
| SMILES Code | C=CC(NC1=CC2=C(NC3=CC=C(F)C(Cl)=C3)N=CN=C2C=C1OCCCN4CCOCC4)=O |
| Synonyms | Canertinib; Canertinib free base; PD-183805; CI1033; CI1 033; CI-1033; PD 183805; PD183805; |
| Protocol | In Vitro | Canertinib significantly inhibits growth of cultured melanoma cells, RaH3 and RaH5, in a dose-dependent manner. IC50 is approximately 0.8 μM and by 5μM both cell lines are completely growth-arrested within 72 h of treatment. Incubation of exponentially growing RaH3 and RaH5 with 1 μM canertinib accumulated the cells in the G1-phase of the cell cycle within 24 h of treatment without induction of apoptosis. 1 μM canertinib inhibits ErbB1-3 receptor phosphorylation with a concomitant decrease of Akt-, Erk1/2- and Stat3 activity in both cell lines. |
|---|---|---|
| In Vivo | Canertinib shows superior in vivo antitumor activity, giving growth delays in A431 xenografts exceeding 50 days following oral administration. |
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 | 2.0579 mL | 10.2893 mL | 20.5787 mL | 41.1573 mL |
| 5mM | 0.4116 mL | 2.0579 mL | 4.1157 mL | 8.2315 mL |
| 10mM | 0.2058 mL | 1.0289 mL | 2.0579 mL | 4.1157 mL |
| 20mM | 0.1029 mL | 0.5145 mL | 1.0289 mL | 2.0579 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start)
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Volume(start)
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Volume(final)
This equation is commonly abbreviated as: C1 V1 = C2 V2
Concentration(start)
C1
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V1
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C2
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Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
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.