2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. Oritinib

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 EGFRWT, EGFRL858R, EGFRL861Q, EGFRL858R/T790M, EGFRd746-750 and EGFRd746-750/T790M kinases, with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively.

For research use only. We do not sell to patients.

Oritinib Chemical Structure

Oritinib Chemical Structure

CAS No. : 2035089-28-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 487 In-stock
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10 mM * 1 mL in DMSO USD 487 In-stock
Solid
5 mg USD 410 In-stock
10 mg USD 610 In-stock
25 mg USD 990 In-stock
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100 mg USD 1800 In-stock
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Based on 1 publication(s) in Google Scholar

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Oritinib Related Antibodies

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Description

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 EGFRWT, EGFRL858R, EGFRL861Q, EGFRL858R/T790M, EGFRd746-750 and EGFRd746-750/T790M kinases, with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively[1].

IC50 & Target[1]

EGFR (WT)

18 nM (IC50)

EGFRL858R

0.7 nM (IC50)

EGFRL861Q

4 nM (IC50)

EGFRL858R/T790M

0.1 nM (IC50)

EGFRd746-750

1.4 nM (IC50)

EGFRd746-750/T790M

0.89 nM (IC50)

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.

Oritinib Related Antibodies

Cell Proliferation Assay[1]

Cell Line: A431 (EGFRWT), H3255 (EGFRL858R), PC-9 (EGFRd746-750) and NCI-H1975 (EGFRL858R/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 Tmax is 1.5-2 h, indicating rapidly distributed into tissues, including lung tumor tissues.
The AUC0–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
Molecular Weight

539.67

Formula

C31H37N7O2
CAS No.
Unlabeled CAS

Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8530 mL 9.2649 mL 18.5298 mL
5 mM 0.3706 mL 1.8530 mL 3.7060 mL
View the Complete Stock Solution Preparation Table

* 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.

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
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Oritinib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Oritinib2035089-28-0SH-1028SH1028SH 1028EGFREpidermal growth factor receptorErbB-1HER1EGFR-T790Mnon-small cell lung cancerpharmacodynamicsIrreversiblethird-generationEGFR TKImutant-selectiveInhibitorinhibitorinhibit

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