Referencia número: HY-153268

Silevertinib

(Synonyms: BDTX-1535; EGFR-IN-76)

3 Cited Publications

Revisión del cliente

Based on 3 publication(s) in Google Scholar

Silevertinib (BDTX-1535) is an irreversible, brain-penetrant, selective and orally active EGFR inhibitor with wild-type EGFR-sparing. Silevertinib targets key EGFR resistance mutations, including the kinase domain (C797S, L718Q, G724S, S768I), extracellular domain (EGFRvIII, A289X), and EGFR amplification. Silevertinib exerts anti-tumor activity with well tolerated in vivo. Silevertinib can be used for non-small cell lung cancer (NSCLC) and glioblastoma (GBM) research.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 99.74%
No. CAS: 2607829-38-7
Fòrmula: C₃₀H₃₀ClFN₆O₂
Peso molecular:561.05

Almacenamiento:

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

Silevertinib Chemical Structure

No. CAS: 2607829-38-7

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (3)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

C797S

L718Q

G724S

S768I

A289X

EGFRvIII

Ver todos los productos específicos de isoformas EGFR :

In Vitro

Silevertinib targets the EGFR C797S mutation (including C797S/L858R; C797S/del19; C797S/T790M) with an IC⁵⁰ <10 nM^[4].

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

In Vivo

Silevertinib consistently achieves tumor regression without significant wild-type EGFR-associated toxicities in mouse PDX^[2].
Silevertinib shows a central nervous system (CNS) Kpuu of 0.55 and 0.48 in rat and dog, respectively^[2].
Silevertinib is active in an intracranial PDX model^[2].
Silevertinib (o.p., once) suppresses phosphorylation of EGFR mutants for greater than 24h^[3].
Silevertinib achieves a broad antitumor efficacy across NsCLC/GBM PDX tumors expressing a family of EGFR oncogenic mutations^[3].

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

Ensayo clínico

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

Chemical Information

No. CAS 2607829-38-7
Appearance Solid
Peso molecular 561.05
Fòrmula C₃₀H₃₀ClFN₆O₂
Color Light yellow to yellow
SMILES

O=C(/C=C/CN1CCOCC1)NC2=CC3=C(N=CN=C3NC4=C(C(Cl)=CC=C4)F)C=C2C#C[C@]56[C@](CN(C6)C)([H])C5
Synonyms

BDTX-1535; EGFR-IN-76
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (3)

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Journal Impact Factor

Cancer Res

Enozertinib is a Selective, Brain-penetrant EGFR inhibitor for Treating Non-small Cell Lung Cancers with EGFR Exon 20 and Atypical Mutations. [Abstract]

2025 Nov 6. PMID: 41196054
Redox Biol

C-terminal interleukin 1 alpha (IL-1α) overexpression drives EMT and a vulnerability to ferroptosis in HNSCC. [Abstract]

2026 Jun:93:104172. PMID: 42013543
Cancer Lett

Targeting inosine metabolism to enhance EGFR-targeted therapy in lung adenocarcinoma. [Abstract]

2025 Dec 1:634:218069. PMID: 41033606

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (178.24 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

1.7824 mL

8.9119 mL

17.8237 mL

5 mM

0.3565 mL

1.7824 mL

3.5647 mL

10 mM

0.1782 mL

0.8912 mL

1.7824 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.

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)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.46 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (281 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 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]. O'Connor M, et al. Discovery of BDTX-1535, a novel 4th generation, irreversible, potent, wild type sparing EGFR MasterKey inhibitor that targets oncogenic kinase domain mutations as well as extracellular domain alterations for the treatment of NSCLC and GBM[J]. Cancer Research, 2023, 83(7_Supplement): 3396-3396.

[2]. Lucas M, et al. BDTX-1535, a fourth generation EGFR inhibitor, targeting intrinsic and acquired resistance mutations in NSCL. European Journal of Cancer, 2022, 174: S22.

[3]. Lucas, M.C., et al. a CNS penetrant, irreversible inhibitor of intrinsic and acquired resistance EGFR mutations, demonstrates preclinical efficacy in NSCLC and GBM PDX models. Annals of Oncology, 2022,

[4]. Dempke WCM, et al. Targeting C797S mutations and beyond in non-small cell lung cancer-a mini-review. Transl Cancer Res. 2024 Nov 30;13(11):6540-6549.

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	1.7824 mL	8.9119 mL	17.8237 mL	44.5593 mL
	5 mM	0.3565 mL	1.7824 mL	3.5647 mL	8.9119 mL
	10 mM	0.1782 mL	0.8912 mL	1.7824 mL	4.4559 mL
	15 mM	0.1188 mL	0.5941 mL	1.1882 mL	2.9706 mL
	20 mM	0.0891 mL	0.4456 mL	0.8912 mL	2.2280 mL
	25 mM	0.0713 mL	0.3565 mL	0.7129 mL	1.7824 mL
	30 mM	0.0594 mL	0.2971 mL	0.5941 mL	1.4853 mL
	40 mM	0.0446 mL	0.2228 mL	0.4456 mL	1.1140 mL
	50 mM	0.0356 mL	0.1782 mL	0.3565 mL	0.8912 mL
	60 mM	0.0297 mL	0.1485 mL	0.2971 mL	0.7427 mL
	80 mM	0.0223 mL	0.1114 mL	0.2228 mL	0.5570 mL
	100 mM	0.0178 mL	0.0891 mL	0.1782 mL	0.4456 mL

Keywords

Silevertinib

3 Cited Publications

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Silevertinib

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Publications Citing Use of MedChemExpress (MCE) Silevertinib

Ver todos los productos específicos de isoformas EGFR

Actividad biológica

Chemical Information

Publications (3)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Silevertinib Related Classifications

HY-153268 Related Classifications