Art. -Nr.: HY-139920

Oritinib

(Synonyms: SH-1028)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Oritinib (SH-1028), an irreversible third-generation EGFR TKI, overcomes T790M-mediated resistance in non-small cell lung cancer. Oritinib (SH-1028), a mutant-selective inhibitor of EGFR kinase activity, inhibits EGFR^WT, EGFR^L858R, EGFR^L861Q, EGFR^L858R/T790M, EGFR^d746-750 and EGFR^{d746-750/T790M} kinases, with IC₅₀s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively.

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Reinheit: 99.59%
CAS. Nr.: 2035089-28-0
Formel: C₃₁H₃₇N₇O₂
Molecular Weight:539.67

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Oritinib Chemical Structure

CAS. Nr.: 2035089-28-0

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Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

EGFR (WT)

18 nM (IC₅₀)

EGFR^L858R

0.7 nM (IC₅₀)

EGFR^L861Q

4 nM (IC₅₀)

EGFR^L858R/T790M

0.1 nM (IC₅₀)

EGFR^d746-750

1.4 nM (IC₅₀)

EGFR^{d746-750/T790M}

0.89 nM (IC₅₀)

Alle EGFR Isoform-spezifische Produkte anzeigen :

In Vitro

Oritinib (SH-1028) binds irreversibly to EGFR kinase by targeting cysteine-797 residue in the ATP binding site via covalent bond formation^[1].
Oritinib (0.001-10 μM) potently and selectively targets mutant EGFR cell lines in vitro^[1].
Oritinib (0.1 μM) continuously inhibits the phosphorylation of EGFR in PC-9 and NCI-H1975 cells at lower concentrations or even drug-free for at least 6 h^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

A431 (EGFR^WT), H3255 (EGFR^L858R), PC-9 (EGFR^d746-750) and NCI-H1975 (EGFR^L858R/T790M) cells
Concentration:

0.001, 0.01, 0.1, 1, and 10 μM
Incubation Time:

72 hours
Result:

Selectively inhibited EGFR-mutated NCI-H1975, H3255 and PC-9 cells, with IC₅₀s of 3.93±1.12, 9.39±0.88 and 7.63±0.18 nmol/L, respectively, which were about 198-, 83- and 102-fold more sensitive than the inhibition of wild-type EGFR in A431 cells (IC₅₀=778.89±134.74 nM).

In Vivo

Oral administration of Oritinib at a daily dose of 5 mg/kg significantly inhibits proliferation of tumor cells with EGFR sensitive mutation (exon 19 del) and resistant mutation (T790 M) for consecutive 14 days, with no TKI-induced weight loss in mouse xenograft models^[1].
Oritinib shows good bioavailability, and is distributed extensively from the plasma to the tissues^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

6-8 weeks old female mice bearing NCI-H1975 and A431 xenograft models ^[1]
Dosage:

2.5, 5, and 15 mg/kg
Administration:

Orally administrated once daily for consecutive 14 days
Result:

Led to a significant inhibition of tumor cell growth in both PC-9 (exon 19 del) and NCI-H1975 (L858R/T790M) xenograft models.

Animal Model:

NCI-H1975 tumor-bearing mice^[1]
Dosage:

2.5, 5, and 15 mg/kg (Pharmacokinetic Analysis)
Administration:

Oral administration for 1 day or 14 consecutive days.
Result:

The T_max is 1.5-2 h, indicating rapidly distributed into tissues, including lung tumor tissues.
The AUC_0–t values in plasma were 118, 300 and 931 ng×h/mL on Day 1, while 272, 308 and 993 ng×h/ml on Day 14, respectively.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2035089-28-0
Appearance Solid
Molecular Weight 539.67
Formel C₃₁H₃₇N₇O₂
Color Off-white to light yellow
SMILES

O=C(NC1=CC(NC2=NC(C3=C(CCCC4)N4C5=C3C=CC=C5)=CC=N2)=C(C=C1N(CCN(C)C)C)OC)C=C
Synonyms

SH-1028
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Journal Impact Factor

J Med Chem

Profiling and Optimizing Targeted Covalent Inhibitors through EGFR-Guided Studies. [Abstract]

2025 Aug 28;68(16):17917-17932. PMID: 40801664

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (231.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8530 mL

9.2649 mL

18.5298 mL

5 mM

0.3706 mL

1.8530 mL

3.7060 mL

10 mM

0.1853 mL

0.9265 mL

1.8530 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8530 mL	9.2649 mL	18.5298 mL	46.3246 mL
	5 mM	0.3706 mL	1.8530 mL	3.7060 mL	9.2649 mL
	10 mM	0.1853 mL	0.9265 mL	1.8530 mL	4.6325 mL
	15 mM	0.1235 mL	0.6177 mL	1.2353 mL	3.0883 mL
	20 mM	0.0926 mL	0.4632 mL	0.9265 mL	2.3162 mL
	25 mM	0.0741 mL	0.3706 mL	0.7412 mL	1.8530 mL
	30 mM	0.0618 mL	0.3088 mL	0.6177 mL	1.5442 mL
	40 mM	0.0463 mL	0.2316 mL	0.4632 mL	1.1581 mL
	50 mM	0.0371 mL	0.1853 mL	0.3706 mL	0.9265 mL
	60 mM	0.0309 mL	0.1544 mL	0.3088 mL	0.7721 mL
	80 mM	0.0232 mL	0.1158 mL	0.2316 mL	0.5791 mL
	100 mM	0.0185 mL	0.0926 mL	0.1853 mL	0.4632 mL

Keywords

Oritinib

1 Cited Publications

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Oritinib

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High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Oritinib

Alle EGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Oritinib Related Classifications

HY-139920 Related Classifications