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Oritinib

Catalog No. T60076   CAS 2035089-28-0
Synonyms: SH-1028

Oritinib (SH-1028) is an inhibitor of EGFR with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM for EGFR (wt), EGFR (L858R), EGFR (L861Q), EGFR (L858R/T790M), EGFR (d746-750), EGFR (d746-750/T790M), respectively. Oritinib can be used in studies about the treatment of non-small cell lung cancer.

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Oritinib Chemical Structure
Oritinib, CAS 2035089-28-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 163.00
5 mg In stock $ 413.00
10 mg In stock $ 618.00
25 mg In stock $ 985.00
50 mg In stock $ 1,330.00
100 mg In stock $ 1,790.00
1 mL * 10 mM (in DMSO) In stock $ 455.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Oritinib (SH-1028) is an inhibitor of EGFR with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM for EGFR (wt), EGFR (L858R), EGFR (L861Q), EGFR (L858R/T790M), EGFR (d746-750), EGFR (d746-750/T790M), respectively. Oritinib can be used in studies about the treatment of non-small cell lung cancer.
In vitro Oritinib (0.001, 0.01, 0.1, 1, and 10 μM) selectively inhibits EGFR-mutated NCI-H1975, H3255 and PC-9 cells, with IC50s of 3.932, 9.39 and 7.63 nM, respectively. Oritinib (0.1 μM) continuously inhibits the phosphorylation of EGFR in PC-9 and NCI-H1975 cells[1].
In vivo In female mice bearing NCI-H1975 and A431 xenograft models, Oritinib (2.5, 5, and 15 mg/kg; oral) significantly inhibits proliferation of tumor cells with no TKI-induced weight loss. In NCI-H1975 tumor-bearing mice, Oritinib (2.5, 5, and 15 mg/kg; oral) shows good bioavailability(Tmax = 1.5-2 h) and extensive distribution from the plasma to the tissues. The AUC0–t values in plasma are 118, 300 and 931 ng×h/mL on Day 1, while 272, 308 and 993 ng×h/ml on Day 14, respectively[1].
Synonyms SH-1028
Molecular Weight 539.67
Formula C31H37N7O2
CAS No. 2035089-28-0

Storage

keep away from direct sunlight

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

Solubility Information

DMSO: 120 mg/mL (222.36 mM), sonification is recommended.

TargetMolReferences and Literature

1. Luwei Han, et al. SH-1028, An Irreversible Third-Generation EGFR TKI, Overcomes T790M-Mediated Resistance in Non-Small Cell Lung Cancer. Front Pharmacol. 2021 Apr 27;12:665253.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Anti-Ovarian Cancer Compound Library Clinical Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library Drug Repurposing Compound Library Anti-Breast Cancer Compound Library

Related Products

Related compounds with same targets
EGFR-IN-79 CNX-2006 FIIN-3 JCN037 PD173074 Poziotinib hydrochloride Nezutatug Neolinine

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Keywords

Oritinib 2035089-28-0 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR pharmacodynamics non-small cell lung cancer EGFR-T790M EGFR TKI Irreversible mutant-selective SH1028 HER1 inhibit SH-1028 Inhibitor Epidermal growth factor receptor SH 1028 ErbB-1 third-generation inhibitor

 

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