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Purity: ≥98%
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. In assays for peptide phosphorylation and in vitro kinase binding, it demonstrated low nanomolar biochemical activity and a slow (T1/2 >120 min) inhibitor off-rate, respectively. In comparison to SOC agents, CEP-40783 exhibits greater efficacy both by itself and in conjunction with erlotinib in Champions TumorGraft™ models of NSCLC, which encourages the development of CEP-40783 for the treatment of erlotinib-resistant NSCLC.
| Targets |
Axl (IC50 = 7 nM); c-Met (IC50 = 12 nM); Tyro3 (IC50 = 19 nM); MER (IC50 = 29 nM); Tyro3 (IC50 = 29 nM)
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| Enzyme Assay |
RXDX-106, also referred to as CEP-40783, is a highly available oral Type II inhibitor of AXL and c-Met with IC50 values of 7 nM and 12 nM, respectively. It is nanomolar potent and highly kinase-selective. In vitro kinase binding assays and peptide phosphorylation assays, it demonstrated a slow (T1/2 >120 min) inhibitor off-rate and low nanomolar biochemical activity, respectively.
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| Cell Assay |
After 30 minutes of either vehicle alone or RXDX-106 incubation, the phosphorylation of the receptors in 3T3 cells expressing Tyro3, Axl, or Mer is observed.
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| Animal Protocol |
Mice: For 10 to 34 days, mice with established Champions TumorGrafts are given oral doses of 10 mg/kg and 30 mg/kg qd of CEP-40783, and the anti-tumor efficaciousness and tolerability are assessed[2].
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| References |
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| Molecular Formula |
C31H26F2N4O6
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| Molecular Weight |
588.56
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| Exact Mass |
588.18
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| Elemental Analysis |
C, 63.26; H, 4.45; F, 6.46; N, 9.52; O, 16.31
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| CAS # |
1437321-24-8
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CC(C)N1C=C(C(=O)N(C1=O)C2=CC=C(C=C2)F)C(=O)NC3=CC(=C(C=C3)OC4=C5C=C(C(=CC5=NC=C4)OC)OC)F
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| InChi Key |
FKCWHHYUMFGOPY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H26F2N4O6/c1-17(2)36-16-22(30(39)37(31(36)40)20-8-5-18(32)6-9-20)29(38)35-19-7-10-26(23(33)13-19)43-25-11-12-34-24-15-28(42-4)27(41-3)14-21(24)25/h5-17H,1-4H3,(H,35,38)
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| Chemical Name |
N-[4-(6,7-dimethoxyquinolin-4-yl)oxy-3-fluorophenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6991 mL | 8.4953 mL | 16.9906 mL | |
| 5 mM | 0.3398 mL | 1.6991 mL | 3.3981 mL | |
| 10 mM | 0.1699 mL | 0.8495 mL | 1.6991 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
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