BBT-176
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BBT-176 is an orally active EGFR tyrosine kinase inhibitor. BBT-176 is a reversible ATP-competitive inhibitor with a unique binding mode, and it exhibits selectivity for mutant EGFR over wild-type EGFR. BBT-176 inhibits tumor growth, induces tumor regression, upregulates EGFR expression, and does not trigger secondary EGFR gene mutations. BBT-176 can be used in research related to non-small cell lung cancer.
For research use only. We do not sell to patients.
- Purity : 98.98%
- CAS No.: 2254805-44-0
- Formula: C28H37ClN8O3S
- Molecular Weight:601.16
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
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Biological Activity
Description
BBT-176 is an orally active EGFR tyrosine kinase inhibitor. BBT-176 is a reversible ATP-competitive inhibitor with a unique binding mode, and it exhibits selectivity for mutant EGFR over wild-type EGFR. BBT-176 inhibits tumor growth, induces tumor regression, upregulates EGFR expression, and does not trigger secondary EGFR gene mutations. BBT-176 can be used in research related to non-small cell lung cancer[1].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| BaF3 | IC50 |
27 nM
Compound: 8; BBT-176
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Inhibition of cell growth in mouse BaF3 cells harboring EGFR del19/T790M/C797S mutant incubated for 72 hrs by fluorescence based assay
Inhibition of cell growth in mouse BaF3 cells harboring EGFR del19/T790M/C797S mutant incubated for 72 hrs by fluorescence based assay
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[PMID: 38908104] |
In Vitro
Anti-cancerOthers
Anti-cancer
BBT-176 (0.01-10000 nM; 72 h) potently inhibits the growth of Ba/F3 cells expressing C797S-containing mutant EGFR, with greatest activity against 19Del-based mutants (IC50 < 50 nM) and reduced potency against L858R-based mutants and wild-type EGFR cells[1].
BBT-176 (0.01-1000 nM; 72 h)-resistant Ba/F3 clones (derived from EGFR 19Del, 19Del/C797S, and 19Del/T790M/C797S cells) show only 2- to 5-fold higher IC50 values for BBT-176 compared to parental cells, with resistance driven by increased EGFR signaling rather than secondary EGFR mutations[1].
BBT-176 (0.01-1000 nM, 12.35 nM, 13.7 nM; 72 h) combined with Cetuximab (HY-P99050) potently enhances growth inhibition of both parental and BBT-176-resistant EGFR19Del/T790M/C797S-expressing Ba/F3 cells, achieving sub-nanomolar to low-nanomolar IC50 values[1].
BBT-176 (0.01-1000 nM; 72 h)-resistant Ba/F3 clones (derived from EGFR 19Del, 19Del/C797S, and 19Del/T790M/C797S cells) show only 2- to 5-fold higher IC50 values for BBT-176 compared to parental cells, with resistance driven by increased EGFR signaling rather than secondary EGFR mutations[1].
BBT-176 (0.01-1000 nM, 12.35 nM, 13.7 nM; 72 h) combined with Cetuximab (HY-P99050) potently enhances growth inhibition of both parental and BBT-176-resistant EGFR19Del/T790M/C797S-expressing Ba/F3 cells, achieving sub-nanomolar to low-nanomolar IC50 values[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
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Cell Line:Engineered Ba/F3 cells expressing mutant EGFR (19Del/C797S, 19Del/T790M/C797S, L858R/C797S, L858R/T790M/C797S, wild-type), parental Ba/F3 cells, human NSCLC cell lines with wild-type EGFR (A-431, A549, LoVo, NCI-H1299, NCI-H2073)
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Concentration:0.1-1000 nM
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Incubation Time:72 h
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Result:Inhibited growth of Ba/F3 cells expressing EGFR 19Del/C797S with an IC50 of 42 nM.
Inhibited growth of Ba/F3 cells expressing EGFR 19Del/T790M/C797S with an IC50 of 49 nM.
Inhibited growth of Ba/F3 cells expressing EGFR L858R/C797S with an IC50 of 183 nM.
Inhibited growth of Ba/F3 cells expressing EGFR L858R/T790M/C797S with an IC50 of 202 nM.
Cell Viability Assay[1]
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Cell Line:BBT-176-resistant Ba/F3 clones (derived from EGFR 19Del, 19Del/C797S, and 19Del/T790M/C797S-expressing cells via ENU mutagenesis), parental Ba/F3 cells
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Concentration:0.1-1000 nM
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Incubation Time:72 h
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Result:Inhibited growth of EGFR 19Del-resistant clones with IC50 values of 31 nM and 39 nM (parental IC50 = 18 nM).
Inhibited growth of EGFR 19Del/C797S-resistant clones with IC50 values of 109 nM and 113 nM (parental IC50 = 42 nM).
Inhibited growth of EGFR 19Del/T790M/C797S-resistant clones with IC50 values of 240 nM and 242 nM (parental IC50 = 49 nM).
Detected enhanced phosphorylated EGFR levels in EGFR 19Del/T790M/C797S-resistant clones via Western blot analysis.
Detected no secondary EGFR mutations in any resistant clones.
Cell Viability Assay[1]
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Cell Line:EGFR 19Del/T790M/C797S-expressing Ba/F3 cells, BBT-176-resistant EGFR 19Del/T790M/C797S Ba/F3 clones
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Concentration:0.1-1000 nM (BBT-176 alone or with 10 μg/mL cetuximab); 12.35 nM, 13.7 nM (fixed BBT-176 with 10 μg/mL cetuximab)
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Incubation Time:72 h
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Result:Reduced IC50 of parental EGFR 19Del/T790M/C797S Ba/F3 cells from 49 nM to 0.63 nM when combined with 10 μg/mL cetuximab, a 78-fold decrease, and showed synergistic growth suppression.
Reduced IC50 values of BBT-176-resistant EGFR 19Del/T790M/C797S clones from 240 nM and 242 nM to 4.5 nM and 4.3 nM, respectively, when combined with 10 μg/mL cetuximab, and showed synergistic growth suppression.
In Vivo
Anti-cancer
BBT-176 (60-90 mg/kg; p.o.; daily; indicated time period) induces potent tumor growth inhibition, complete growth inhibition, or tumor regression in EGFR-mutant non-small cell lung cancer patient-derived xenograft models, with up to 90% TGI and significant suppression of p-EGFR at 90 mg/kg[1].
BBT-176 (60-90 mg/kg; p.o.; daily) suppresses tumor growth in a dose-dependent manner in Ba/F3 xenograft models of Osimertinib (HY-15772)-resistant EGFR-mutant non-small cell lung cancer, with complete growth inhibition and 101.3% TGI at 90 mg/kg in the EGFR19Del/C797S model[1].
BBT-176 (60-90 mg/kg; p.o.; daily) suppresses tumor growth in a dose-dependent manner in Ba/F3 xenograft models of Osimertinib (HY-15772)-resistant EGFR-mutant non-small cell lung cancer, with complete growth inhibition and 101.3% TGI at 90 mg/kg in the EGFR19Del/C797S model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 35-42 days); nu/nu (female, 35-42 days)[1]
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Dosage:60 mg/kg (LU1235 EGFR 19Del PDX model); 90 mg/kg (LD1-0025-200717 EGFR 19Del/T790M/C797S PDX model)
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Administration:p.o.; daily; indicated time period
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Result:Induced complete tumor growth inhibition with 90% tumor growth index (TGI) in the LD1-0025-200717 EGFR 19Del/T790M/C797S PDX model.
Induced tumor regression with only a small decline in body weight in the LU1235 EGFR 19Del PDX model.
Inhibited phosphorylated EGFR (p-EGFR) by 66.5% to 77.5% in tumor samples from mice treated with 90 mg/kg.
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Animal Model:unstated[1]
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Dosage:60 mg/kg; 90 mg/kg
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Administration:p.o.; daily
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Result:Resulted in 64.4% TGI in Ba/F3 EGFR 19Del/C797S xenografts.
Achieved complete tumor growth inhibition with 101.3% TGI in Ba/F3 EGFR 19Del/C797S xenografts at 90 mg/kg.
Resulted in 66% TGI in Ba/F3 EGFR 19Del/T790M/C797S xenografts at 60 mg/kg.
Resulted in 77% TGI in Ba/F3 EGFR 19Del/T790M/C797S xenografts at 90 mg/kg.
Chemical Information
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CAS No. 2254805-44-0
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Appearance Solid
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Molecular Weight 601.16
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Formula C28H37ClN8O3S
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Color White to off-white
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SMILES
O=S(NC1=C(NC2=NC(NC3=CC=C(N4CCC(CC4)N5CCN(CC5)C)C=C3OC)=NC=C2Cl)C=CC=C1)(C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (83.17 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
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Concentration
Solvent
Mass
1 mg
5 mg
10 mg
Concentration
Solvent
Mass
1 mM
1.6635 mL
8.3173 mL
16.6345 mL
5 mM
0.3327 mL
1.6635 mL
3.3269 mL
10 mM
0.1663 mL
0.8317 mL
1.6635 mL
Molarity Calculator
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Dilution Calculator
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Purity & Documentation
Select Batch:
Purity:
99.98%
Assay:
99.98%
ee.:
99.98%
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Data Sheet (297 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6635 mL | 8.3173 mL | 16.6345 mL | 41.5863 mL |
| 5 mM | 0.3327 mL | 1.6635 mL | 3.3269 mL | 8.3173 mL | |
| 10 mM | 0.1663 mL | 0.8317 mL | 1.6635 mL | 4.1586 mL | |
| 15 mM | 0.1109 mL | 0.5545 mL | 1.1090 mL | 2.7724 mL | |
| 20 mM | 0.0832 mL | 0.4159 mL | 0.8317 mL | 2.0793 mL | |
| 25 mM | 0.0665 mL | 0.3327 mL | 0.6654 mL | 1.6635 mL | |
| 30 mM | 0.0554 mL | 0.2772 mL | 0.5545 mL | 1.3862 mL | |
| 40 mM | 0.0416 mL | 0.2079 mL | 0.4159 mL | 1.0397 mL | |
| 50 mM | 0.0333 mL | 0.1663 mL | 0.3327 mL | 0.8317 mL | |
| 60 mM | 0.0277 mL | 0.1386 mL | 0.2772 mL | 0.6931 mL | |
| 80 mM | 0.0208 mL | 0.1040 mL | 0.2079 mL | 0.5198 mL |
BBT-176 Related Classifications
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