Referencia número: HY-116437

Selatinib

1 Cited Publications

Revisión del cliente

Based on 1 publication(s) in Google Scholar

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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Pureza: 98.56%
No. CAS: 1275595-86-2
Fòrmula: C₂₉H₂₆ClFN₄O₃S
Peso molecular:565.06

Almacenamiento:

4°C, protect from light

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

Selatinib Chemical Structure

No. CAS: 1275595-86-2

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
- Ensayo clínico
Chemical Information
Publications (1)
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

EGFR

13 nM (IC₅₀)

HER2

8.5 nM (IC₅₀)

Ver todos los productos específicos de isoformas EGFR :

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.

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	T_max	C_max	AUC_0-t	AUC_0-∞	MRT	T_1/2	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.

Ensayo clínico

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

Chemical Information

No. CAS 1275595-86-2
Appearance Solid
Peso molecular 565.06
Fòrmula C₂₉H₂₆ClFN₄O₃S
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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, protect from light

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

Publications (1)

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Journal Impact Factor

Cell Death Differ

CRISPR/Cas9 library screening uncovered CCT2 as a critical driver of acquired resistance to EGFR-targeted therapy by stabilizing TMX1 in non-small cell lung cancer. [Abstract]

2025 Oct 30. PMID: 41168408

Solvente y solubilidad

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)

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

1.7697 mL

8.8486 mL

17.6972 mL

5 mM

0.3539 mL

1.7697 mL

3.5394 mL

10 mM

0.1770 mL

0.8849 mL

1.7697 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 (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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Wang MN, et al. First-in-human, phase I single-ascending-dose study of the safety, pharmacokinetics, and relative bioavailability of selatinib, a dual EGFR-ErbB2 inhibitor in healthy subjects. Invest New Drugs. 2020;38(6):1826-1835. [Content Brief]

[2]. Zhang L, et al. Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer. Eur J Med Chem. 2013;69:833-841. [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

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

Keywords

Selatinib

1 Cited Publications

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Selatinib

Immunology/Inflammation Compound Library

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Publications Citing Use of MedChemExpress (MCE) Selatinib

Ver todos los productos específicos de isoformas EGFR

Actividad biológica

Chemical Information

Publications (1)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Selatinib Related Classifications

HY-116437 Related Classifications