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BLU-945

Catalog No. T9754 CAS 2660250-10-0

Synonyms: BLU945, BLU 945

BLU-945 is a potent, highly selective, reversible, and orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, effective against EGFR with L858R and/or exon 19 deletion mutations, T790M, and C797S mutations. It is utilized in lung cancer research, including non-small cell lung cancer (NSCLC).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

BLU-945, CAS 2660250-10-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 133.00
5 mg	In stock	$ 339.00
10 mg	In stock	$ 547.00
25 mg	In stock	$ 822.00
50 mg	In stock	$ 1,060.00
100 mg	In stock	$ 1,390.00

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Purity: 99.16%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	BLU-945 is a potent, highly selective, reversible, and orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, effective against EGFR with L858R and/or exon 19 deletion mutations, T790M, and C797S mutations. It is utilized in lung cancer research, including non-small cell lung cancer (NSCLC).
In vitro	BLU-945 has inhibitory activity against the EGFRm/T790M double and EGFRm/T790M/C797Striple mutants, IC50 value range from 1.2-4.4 nM[2]. BLU-945 (0- 10 mM, 4 h) inhibit EGFR phosphorylation in the EGFR L858R/T790M/C797S, and EGFR ex19del/T790M/C797S mutant cell lines[2].
In vivo	BLU-945 (oral, 0-100 mg/kg; bid) shows potent, robust EGFR pathway inhibition and anti-tumor activity in triple-mutant osimertinib-resistant Ba/F3 CDX and PDCX models[2].

Synonyms	BLU945, BLU 945
Molecular Weight	556.7
Formula	C28H37FN6O3S
CAS No.	2660250-10-0

Storage

store at low temperature,keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (179.6 mM), Sonication and heating to 60℃ are recommended.

References and Literature

1. John Emmerson Campbell, et al. Inhibitors of mutant forms of egfr. Patent WO2021133809A1. 2. Sun Min Lim, et al. BLU-945, a fourth-generation, potent and highly selective epidermal growth factor receptor tyrosine kinase inhibitor with intracranial activity, demonstrates robust in vivo anti-tumor activity in models of osimertinib-resistant non-sma 3. Meredith S Eno, et al. Discovery of BLU-945, a Reversible, Potent, and Wild-Type-Sparing Next-Generation EGFR Mutant Inhibitor for Treatment-Resistant Non-Small-Cell Lung Cancer. J Med Chem. 2022 Jul 28;65(14):9662-9677. 4. Elaine Shum. et al. A phase 1/2 study of BLU-945 in patients with common activating EGFRmutant non-small cell lung cancer (NSCLC) (SYMPHONY trial-in-progress)

Citations

1. Liang J, Bi G, Sui Q, et al.Transcription factor ZNF263 enhances EGFR-targeted therapeutic response and reduces residual disease in lung adenocarcinoma.Cell Reports.2024, 43(2).

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Drug Repurposing Compound Library Kinase Inhibitor Library Anti-Lung Cancer Compound Library Bioactive Compounds Library Max

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

BLU-945 2660250-10-0 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR BLU945 BLU 945 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.