CEP-40783 (RXDX-106)
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 | $950 | Check With Us |
| 500mg | $1550 | Check With Us |
| 1g | $2325 | Check With Us |
: Cat #: V2760 CAS #: 1437321-24-8 Purity ≥ 98%
Description: RXDX-106 (also known as CEP-40783) is an orally bioavailable, nanomolar potent and highly kinase-selective Type II inhibitor of AXL and c-Met with IC50 values of 7 nM and 12 nM, respectively.
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| Molecular Weight (MW) | 588.56 |
|---|---|
| Molecular Formula | C31H26F2N4O6 |
| CAS No. | 1437321-24-8 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 10 mg/mL (16.99 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 2 mg/mL (3.39 mM) | |
| SMILES Code | O=C(C1=CN(C(C)C)C(N(C2=CC=C(F)C=C2)C1=O)=O)NC3=CC=C(OC4=CC=NC5=CC(OC)=C(OC)C=C45)C(F)=C3 |
| Synonyms | CEP-40783; CEP40783; CEP 40783; RXDX-106; RXDX 106; RXDX106 |
| Protocol | In Vitro | In AXL-transfected 293GT cells, CEP-40783 is 27-fold more active compared to recombinant enzyme with an IC50 value of 0.26 nM. CEP-40783 also demonstrates superior activity against c-Met in GTL-16 cells (IC50=6 nM). The increased inhibitory activity of CEP-40783 in cells could be attributed to its extended residence time on both AXL and c-Met, consistent with a Type II mechanism. CEP-40783 shows high kinome selectivity against 298 kinases with an S90 of 0.04 (fraction of kinases showing >90% inhibition at 1 µM). |
|---|---|---|
| In Vivo | CEP-40783 shows dose- and time-dependent inhibition of AXL phosphorylation using NCI-H1299 NSCL xenografts with 80% target inhibition at 0.3 mg/kg 6 h post dose and complete target inhibition to >90% inhibition at 1 mg/kg between 6-24 h, while a 10 mg/kg po dose resulted in complete AXL inhibition up to 48 h post dosing. |
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 | 1.6991 mL | 8.4953 mL | 16.9906 mL | 33.9812 mL |
| 5mM | 0.3398 mL | 1.6991 mL | 3.3981 mL | 6.7962 mL |
| 10mM | 0.1699 mL | 0.8495 mL | 1.6991 mL | 3.3981 mL |
| 20mM | 0.0850 mL | 0.4248 mL | 0.8495 mL | 1.6991 mL |
The molarity calculator equation
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The dilution calculator equation
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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
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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.