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

Selatinib is an orally active EGFR and HER2 tyrosine kinase inhibitor with IC50 values of 13.0 nM and 8.5 nM, respectively. Selatinib undergoes oxidative metabolism in vivo to produce Lapatinib (HY-50898). Selatinib inhibits the growth of breast, gastric and ovarian tumors. Selatinib can be used in research related to gastric cancer, breast cancer and ovarian cancer.

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Selatinib

Selatinib Chemical Structure

CAS No. : 1275595-86-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Selatinib Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Selatinib

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  • Biological Activity

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Description

Selatinib is an orally active EGFR and HER2 tyrosine kinase inhibitor with IC50 values of 13.0 nM and 8.5 nM, respectively. Selatinib undergoes oxidative metabolism in vivo to produce Lapatinib (HY-50898). Selatinib inhibits the growth of breast, gastric and ovarian tumors. Selatinib can be used in research related to gastric cancer, breast cancer and ovarian cancer[1][2].

IC50 & Target[1]

EGFR

13 nM (IC50)

HER2

8.5 nM (IC50)

In Vitro

Selatinib (serial dilution concentrations; 1 h) potently inhibits the tyrosine kinase activity of purified EGFR, with an IC50 of 13 nM[2].
Selatinib (serial gradient dilution; 1 h) potently inhibits the tyrosine kinase activity of purified HER-2, with an IC50 of 8.5 nM[2].
Selatinib (serial dilution concentrations; 72 h) inhibits the proliferation of gastric adenocarcinoma NCI-N87 cells, with an IC50 of 29.4 nM[2].
Selatinib (serial dilution concentrations; 72 h) potently inhibits the proliferation of breast cancer BT-474 cells, with an IC50 of 22.5 nM, and its activity is significantly higher than that of Lapatinib (HY-50898)[2].

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

Selatinib Related Antibodies

Cell Proliferation Assay[2]

Cell Line: human gastric adenocarcinoma NCI-N87 cells
Concentration: Serially diluted concentrations
Incubation Time: 72 h
Result: Inhibited NCI-N87 cell proliferation with an IC50 of 29.4 nM.

Cell Proliferation Assay[2]

Cell Line: human breast carcinoma BT-474 cells
Concentration: Serially diluted concentrations
Incubation Time: 72 h
Result: Inhibited BT-474 cell proliferation with an IC50 of 22.5 nM, which was significantly more active than lapatinib (P < 0.05).
Parmacokinetics
Species Dose Route Tmax Cmax AUC0-t AUC0-∞ MRT T1/2 Bioavailability
Rat[2] 100 mg/kg p.o. 3.5 h 8881 ng/mL 50,299 ng·h/mL 53,236 ng·h/mL 5.38 h 2.32 h 187 %
In Vivo

Selatinib (200 mg/kg; p.o.; daily; 28 days) inhibits NCI-N87 gastric xenograft tumor growth by 94.8% with no observed overt toxicity[2].
Selatinib (200 mg/kg; p.o.; daily; 21 days) inhibits SK-OV-3 ovarian xenograft tumor growth by 85.7% with no observed overt toxicity[2].

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

Animal Model: BALB/c athymic (female, 4-6 weeks old)[2]
Dosage: 200 mg/kg
Administration: p.o.; daily; 28 days
Result: Achieved a 94.8% tumor growth inhibition rate.
Induced significant tumor regression in all 6 treated mice.
Caused no overt toxicity (hematuria, bloody stool) or weight loss.
Animal Model: BALB/c athymic (female, 4-6 weeks old)[2]
Dosage: 200 mg/kg
Administration: p.o.; daily; 21 days
Result: Achieved an 85.7% tumor growth inhibition rate.
Induced significant tumor regression in 2 of the treated mice.
Caused no overt toxicity (hematuria, bloody stool) or weight loss.
Clinical Trial
Molecular Weight

565.06

Formula

C29H26ClFN4O3S
CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

O=S(C)CCNCC1=CC=C(O1)C2=CC3=C(N=CN=C3C=C2)NC4=CC=C(C(Cl)=C4)OCC5=CC=CC(F)=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (176.97 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 1.7697 mL 8.8486 mL 17.6972 mL
5 mM 0.3539 mL 1.7697 mL 3.5394 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

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g

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(per animal)

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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 (protect from light). 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 1.7697 mL 8.8486 mL 17.6972 mL 44.2431 mL
5 mM 0.3539 mL 1.7697 mL 3.5394 mL 8.8486 mL
10 mM 0.1770 mL 0.8849 mL 1.7697 mL 4.4243 mL
15 mM 0.1180 mL 0.5899 mL 1.1798 mL 2.9495 mL
20 mM 0.0885 mL 0.4424 mL 0.8849 mL 2.2122 mL
25 mM 0.0708 mL 0.3539 mL 0.7079 mL 1.7697 mL
30 mM 0.0590 mL 0.2950 mL 0.5899 mL 1.4748 mL
40 mM 0.0442 mL 0.2212 mL 0.4424 mL 1.1061 mL
50 mM 0.0354 mL 0.1770 mL 0.3539 mL 0.8849 mL
60 mM 0.0295 mL 0.1475 mL 0.2950 mL 0.7374 mL
80 mM 0.0221 mL 0.1106 mL 0.2212 mL 0.5530 mL
100 mM 0.0177 mL 0.0885 mL 0.1770 mL 0.4424 mL
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Selatinib 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:

Selatinib1275595-86-2EGFREpidermal growth factor receptorErbB-1HER1ErbB2BT-474NCI-N87gastric cancernon-small cell lung cancerovarian cancerSK-OV-3breast cancertyrosine kinaseInhibitorinhibitorinhibit

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