BLU-945 (Synonyms: ZL-2313)

Name: BLU-945
Brand: MedChemExpress
SKU: HY-144680
Rating: 5.0 (0 reviews)

Cat. No.: HY-144680 Pureza: 99.61%: Ficha de datos
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SDS
Instrucciones de manejo
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BLU-945 is a potent, highly selective, reversible and orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKIs). BLU-945 can effectively inhibit EGFR with L858R and/or exon 19 deletion mutation, T790M mutation and C797S mutation. BLU-945 can be used for the research of lung cancer including non-small cell lung cancer (NSCLC).

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BLU-945 Estructura química

No. CAS : 2660250-10-0

Tamaño	Stock	Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	Obtener un presupuesto
500 mg	Obtener un presupuesto

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Based on 1 Customer Validation

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Ver todos los productos específicos de isoformas EGFR:

Ver todas las isoformas

EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Actividad biológica
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Referencias
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Descripciòn

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	3.2 1 Compound: 40; BLU-945	Inhibition of cell proliferation of mouse BaF3 cells expressing EGFR Del19/T790M/C797S mutant (unknown origin) Inhibition of cell proliferation of mouse BaF3 cells expressing EGFR Del19/T790M/C797S mutant (unknown origin)	[PMID: 36417820]
BaF3	IC₅₀	4 1 Compound: 40; BLU-945	Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay	[PMID: 36417820]

In Vitro

BLU-945 has inhibitory activity against the EGFRm/T790M double and EGFRm/T790M/C797Striple mutants with 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].

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

In Vivo

BLU-945 (oral, 0-100 mg/kg; bid) demonstrates potent, robust EGFR pathway inhibition and anti-tumor activity in triple-mutant Osimertinib (HY-15772)-resistant Ba/F3 CDX and PDCX models^[2].

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

Animal Model:	triple-mutant osimertinib-resistant Ba/F3 CDX and PDCX models^[2]
Dosage:	0-100 mg/kg
Administration:	oral, twice daily
Result:	Showed significant tumor regression in an osimertinib-resistant EGFR ex19del/T790M/C797S PDCX.

Ensayo clínico

Peso molecular

556.70

Fòrmula

C₂₈H₃₇FN₆O₃S

No. CAS

2660250-10-0

Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(C1=CC=C(N2[C@@H]([C@H](C2)CS(C)(=O)=O)C)C3=C1C=C(NC4=NC(N5C[C@@H]([C@@H](CC5)OC)F)=NC=C4)N=C3)C

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)

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (179.63 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	1.7963 mL	8.9815 mL	17.9630 mL
5 mM	0.3593 mL	1.7963 mL	3.5926 mL
10 mM	0.1796 mL	0.8981 mL	1.7963 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.

Calculadora de molaridad
Calculadora de dilución

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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 (4.49 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (3.74 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Pureza y Documentación

Purity: 99.61%

Select Batch:

Ficha de datos (276 KB) SDS (393 KB)

COA (251 KB) HNMR (276 KB) LCMS (96 KB)

Instrucciones de manejo (2659 KB)

Referencias

[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-small cell lung cancer.

[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. [Content Brief]

[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)

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7963 mL	8.9815 mL	17.9630 mL	44.9075 mL
	5 mM	0.3593 mL	1.7963 mL	3.5926 mL	8.9815 mL
	10 mM	0.1796 mL	0.8981 mL	1.7963 mL	4.4907 mL
	15 mM	0.1198 mL	0.5988 mL	1.1975 mL	2.9938 mL
	20 mM	0.0898 mL	0.4491 mL	0.8981 mL	2.2454 mL
	25 mM	0.0719 mL	0.3593 mL	0.7185 mL	1.7963 mL
	30 mM	0.0599 mL	0.2994 mL	0.5988 mL	1.4969 mL
	40 mM	0.0449 mL	0.2245 mL	0.4491 mL	1.1227 mL
	50 mM	0.0359 mL	0.1796 mL	0.3593 mL	0.8981 mL
	60 mM	0.0299 mL	0.1497 mL	0.2994 mL	0.7485 mL
	80 mM	0.0225 mL	0.1123 mL	0.2245 mL	0.5613 mL
	100 mM	0.0180 mL	0.0898 mL	0.1796 mL	0.4491 mL

BLU-945 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.

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BLU-945 (Synonyms: ZL-2313)

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BLU-945 Related Antibodies

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas EGFR:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

BLU-945 Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

BLU-945 Related Classifications

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