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MedKoo Cat#: 581025 | Name: CEP-40783
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

CEP-40783, also known as RXDX-106, is a potent, selective and orally available inhibitor of AXL and c-Met with IC50 values of 7 nM and 12 nM, respectively for use in breast, non-small cell lung (NSCLC), and pancreatic cancers.

Chemical Structure

CEP-40783
CEP-40783
CAS#1437321-24-8

Theoretical Analysis

MedKoo Cat#: 581025

Name: CEP-40783

CAS#: 1437321-24-8

Chemical Formula: C31H26F2N4O6

Exact Mass: 588.1820

Molecular Weight: 588.56

Elemental Analysis: C, 63.26; H, 4.45; F, 6.46; N, 9.52; O, 16.31

Price and Availability

Size Price Availability Quantity
10mg USD 150.00 Ready to ship
25mg USD 350.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,350.00 Ready to ship
500mg USD 2,950.00 Ready to ship
1g USD 4,850.00 Ready to ship
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Related CAS #
No Data
Synonym
CEP-40783; CEP40783; CEP 40783; RXDX-106; RXDX 106; RXDX106.
IUPAC/Chemical Name
N-[4-(6,7-Dimethoxyquinolin-4-yl)oxy-3-fluorophenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
InChi Key
FKCWHHYUMFGOPY-UHFFFAOYSA-N
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)
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
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
CEP-40783 is an inhibitor of AXL and c-Met with IC50 values of 7 nM and 12 nM, respectively.
In vitro activity:
To examine the target inhibitory effect of RXDX-106, MerTK and Axl expression was evaluated. In RXDX-106 sensitive cell line SNU-638, both p-MerTK and p-Axl were decreased in RXDX-106 treated cells. In addition, RXDX-106 treatment induced the p-ERK and p-AKT reductions in SNU-638 cells. On the other hand, p-ERK and p-AKT levels were not significantly altered in SNU-668 following RXDX-106 treatment. Collectively, these results suggested that RXDX-106, a MerTK inhibitor, has an anti-proliferative effect by reducing the p-ERK and p-AKT in MerTK activated cancer cells. Reference: Oncotarget. 2017 Nov 11;8(62):105727-105734. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5739674/
In vivo activity:
RXDX-106 efficacy in vivo was investigated using a classic transformation assay with NIH3T3 cells transduced with human TYRO3, AXL, or MER, allowing them to form tumors in mice. Mice implanted with NIH3T3_TYRO3, AXL, or MER cell lines treated with RXDX-106 showed rapid tumor regression, demonstrating in vivo efficacy of RXDX-106 (Fig. 1C). Reference: Cancer Res. 2019 Apr 15;79(8):1996-2008. https://cancerres.aacrjournals.org/content/79/8/1996.long
Solvent mg/mL mM
Solubility
DMF 20.0 33.89
DMF:PBS (pH 7.2) (1:2) 0.3 0.51
DMSO 6.0 10.26
Ethanol 2.0 3.40
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 588.56 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Kim JE, Kim Y, Li G, Kim ST, Kim K, Park SH, Park JO, Park YS, Lim HY, Lee H, Sohn TS, Kim KM, Kang WK, Lee J. MerTK inhibition by RXDX-106 in MerTK activated gastric cancer cell lines. Oncotarget. 2017 Nov 11;8(62):105727-105734. doi: 10.18632/oncotarget.22394. PMID: 29285287; PMCID: PMC5739674. 2. Yokoyama Y, Lew ED, Seelige R, Tindall EA, Walsh C, Fagan PC, Lee JY, Nevarez R, Oh J, Tucker KD, Chen M, Diliberto A, Vaaler H, Smith KM, Albert A, Li G, Bui JD. Immuno-oncological Efficacy of RXDX-106, a Novel TAM (TYRO3, AXL, MER) Family Small-Molecule Kinase Inhibitor. Cancer Res. 2019 Apr 15;79(8):1996-2008. doi: 10.1158/0008-5472.CAN-18-2022. Epub 2019 Feb 5. PMID: 30723115.
In vitro protocol:
1. Kim JE, Kim Y, Li G, Kim ST, Kim K, Park SH, Park JO, Park YS, Lim HY, Lee H, Sohn TS, Kim KM, Kang WK, Lee J. MerTK inhibition by RXDX-106 in MerTK activated gastric cancer cell lines. Oncotarget. 2017 Nov 11;8(62):105727-105734. doi: 10.18632/oncotarget.22394. PMID: 29285287; PMCID: PMC5739674.
In vivo protocol:
1. Yokoyama Y, Lew ED, Seelige R, Tindall EA, Walsh C, Fagan PC, Lee JY, Nevarez R, Oh J, Tucker KD, Chen M, Diliberto A, Vaaler H, Smith KM, Albert A, Li G, Bui JD. Immuno-oncological Efficacy of RXDX-106, a Novel TAM (TYRO3, AXL, MER) Family Small-Molecule Kinase Inhibitor. Cancer Res. 2019 Apr 15;79(8):1996-2008. doi: 10.1158/0008-5472.CAN-18-2022. Epub 2019 Feb 5. PMID: 30723115.
1: Sheila M, et al. CEP-40783: A potent and selective AXL/c-Met inhibitor for use in breast, non-small cell lung (NSCLC), and pancreatic cancers. [abstract]. In: Proceedings of the AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics; 2013 Oct 19-23; Boston, MA. Philadelphia (PA): AACR; Mol Cancer Ther 2013;12(11 Suppl):Abstract nr C275. 2: Jay F, et al. Antitumor activity of the dual AXL/c-Met inhibitor CEP-40783 in Champions primary TumorGraft™ models of human non-small cell lung cancer (NSCLC). [abstract]. In: Proceedings of the AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics; 2013 Oct 19-23; Boston, MA. Philadelphia (PA): AACR; Mol Cancer Ther 2013;12(11 Suppl):Abstract nr C272.