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CEP-40783

Catalog No. T4426 CAS 1437321-24-8

Synonyms: CEP 40783, RXDX-106

CEP-40783 (RXDX-106) is an effective, specific and orally active AXL/c-Met inhibitor (IC50: 7/12 nM). It also inhibits MER and TYRO3 (IC50: 29/19 nM).

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CEP-40783, CAS 1437321-24-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 122.00
25 mg	In stock	$ 288.00
50 mg	In stock	$ 369.00
100 mg	In stock	$ 531.00
200 mg	In stock	$ 768.00
1 mL * 10 mM (in DMSO)	In stock	$ 100.00

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Purity: 99.64%

Purity: 99.45%

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Description	CEP-40783 (RXDX-106) is an effective, specific and orally active AXL/c-Met inhibitor (IC50: 7/12 nM). It also inhibits MER and TYRO3 (IC50: 29/19 nM).
Targets&IC50	Tyro3:19 nM (Biochemical), Mer:29 nM (Biochemical), Axl:7 nM (Biochemical), c-Met:12 nM (Biochemical)
In vitro	In AXL-transfected 293 gT cells, CEP-40783 is 27-fold more active compared to the recombinant enzyme (IC50: 0.26 nM). In GTL-16 cells, CEP-40783 also has superior activity against c-Met (IC50: 6 nM). The enhanced inhibitory activity of CEP-40783 in cells is attributed to its extended residence time on both c-Met and AXL, similar 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)[1].
In vivo	CEP-40783 showed 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. In AXL/NIH3T3 xenografts, 0.3 mg/kg po resulted in complete tumor regressions. CEP-40783 was also efficacious in reducing spontaneous lymph node and pulmonary metastatic tumor burden in the MDA-MB-231-luc and 4T1-luc orthotopic breast cancer models, respectively, at 10 and 30 mg/kg po. PK/PD evaluation of the c-Met activity of CEP-40783 (10, 30, 55 mg/kg po qdX5d) showed significant to complete inhibition of c-Met phosphorylation in GTL-16 gastric carcinoma xenografts. Efficacy studies in GTL-16 xenografts demonstrated significant anti-tumor efficacy (tumor stasis and regressions) at 10 and 30 mg/kg po. In EBC-1 NSCL xenografts, administration of CEP-40783 (3, 10 and 30 mg/kg, po qd) resulted in dose-related efficacy, with tumor stasis at 3 mg/kg, tumor regressions and >96% TGI at 10 mg/kg.

Synonyms	CEP 40783, RXDX-106
Molecular Weight	588.56
Formula	C31H26F2N4O6
CAS No.	1437321-24-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: Insoluble

Ethanol: 2 mg/mL

DMSO: 5.89 mg/mL (10 mM), Sonication is recommended.

References and Literature

1. Miknyoczki S, Cheng M, Hudkins R, et al. Abstract C275: CEP-40783: A potent and selective AXL/c-Met inhibitor for use in breast, non-small cell lung (NSCLC), and pancreatic cancers.[J]. Molecular Cancer Therapeutics, 2013, 12(11_Supplement):C275-C275. 2. Franovic A, Schairer A E, Uryu S, et al. 65 – RXDX-106 Is an orally-available, potent and selective TAM/MET inhibitor demonstrating preClinicalal efficacy in MET-dependent human malignancies[J]. European Journal of Cancer, 2016, 69:S28–S29.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Membrane Protein-targeted Compound Library Reprogramming Compound Library Preclinical Compound Library Hematonosis Compound Library Anti-Colorectal Cancer Compound Library Bioactive Compounds Library Max

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Keywords

CEP-40783 1437321-24-8 Tyrosine Kinase/Adaptors c-Met/HGFR TAM Receptor Mer Inhibitor RXDX 106 CEP 40783 Tyro3 RXDX106 CEP40783 RXDX-106 inhibit Axl inhibitor

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