product name Entrectinib
Description: Entrectinib (also known as RXDX-101) is an orally available small molecule pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Entrectinib has demonstrated potent pharmacological activity in preclinical studies and has the potential to be first-in-class against the Trk family of kinases. PXDX-101 has been well tolerated in patients with advanced solid tumors. Entrectinib is currently in clinical trials, and is being developed by Ignyta.
References: Expert Opin Investig Drugs. 2015;24(11):1493-500.
560.64
Formula
C31H34F2N6O2
CAS No.
1108743-60-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (178.4 mM)
Water: <1 mg/mL
Ethanol: 100 mg/mL (178.4 mM)
Solubility (In vivo)
Synonyms
RXDX-101, NMS-E628
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19399267
| In Vitro |
In vitro activity: Entrectinib selectively blocks proliferation of ALK-dependent cell lines and potently inhibits ALK‐dependent signaling. Entrectinib also highly inhibits cell growth of the NSCLC cell line NCI‐H2228 bearing the EML4-ALK rearrangement. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In mice bearing Karpas-299 and SR-786 xenografts, Entrectinib (p.o.) induces complete tumor regression. In NPM-ALK transgenic mice, Entrectinib induces complete regression of tumor masses observed in the thymus and in lymph nodes. In the NB xenograft model, Entrectinib cotreatment enhanced the efficacy of conventional chemotherapy. |
| Animal model | |
| Formulation & Dosage | |
| References | Expert Opin Investig Drugs. 2015;24(11):1493-500; Cancer Res 2013;73(8 Suppl): Abstract nr 2092. doi:10.1158/1538-7445.AM2013-2092. |
Related Posts
product name Entrectinib
Description: Entrectinib (also known as RXDX-101) is an orally available small molecule pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Entrectinib has demonstrated potent pharmacological activity in preclinical studies and has the potential to be first-in-class against the Trk family of kinases. PXDX-101 has been well tolerated in patients with advanced solid tumors. Entrectinib is currently in clinical trials, and is being developed by Ignyta.
References: Expert Opin Investig Drugs. 2015;24(11):1493-500.
560.64
Formula
C31H34F2N6O2
CAS No.
1108743-60-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (178.4 mM)
Water: <1 mg/mL
Ethanol: 100 mg/mL (178.4 mM)
Solubility (In vivo)
Synonyms
RXDX-101, NMS-E628
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19399267
| In Vitro |
In vitro activity: Entrectinib selectively blocks proliferation of ALK-dependent cell lines and potently inhibits ALK‐dependent signaling. Entrectinib also highly inhibits cell growth of the NSCLC cell line NCI‐H2228 bearing the EML4-ALK rearrangement. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In mice bearing Karpas-299 and SR-786 xenografts, Entrectinib (p.o.) induces complete tumor regression. In NPM-ALK transgenic mice, Entrectinib induces complete regression of tumor masses observed in the thymus and in lymph nodes. In the NB xenograft model, Entrectinib cotreatment enhanced the efficacy of conventional chemotherapy. |
| Animal model | |
| Formulation & Dosage | |
| References | Expert Opin Investig Drugs. 2015;24(11):1493-500; Cancer Res 2013;73(8 Suppl): Abstract nr 2092. doi:10.1158/1538-7445.AM2013-2092. |