Referencia número: HY-144680

BLU-945

(Synonyms: ZL-2313)

Revisión del cliente

Based on 1 Customer Validation

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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Pureza: 99.61%
No. CAS: 2660250-10-0
Fòrmula: C₂₈H₃₇FN₆O₃S
Peso molecular:556.70

Almacenamiento:

4°C, protect from light

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

BLU-945 Chemical Structure

No. CAS: 2660250-10-0

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Actividad biológica
- Descripciòn
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Ver todos los productos específicos de isoformas EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	3.2 nM 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 nM 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

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

Chemical Information

No. CAS 2660250-10-0
Appearance Solid
Peso molecular 556.70
Fòrmula C₂₈H₃₇FN₆O₃S
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
Synonyms

ZL-2313
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)

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

1.7963 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

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)

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 (4.49 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.

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.

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 (276 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]. 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)

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	1.7963 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

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BLU-945

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Posttranslational Modification Library

Ver todos los productos específicos de isoformas EGFR

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

BLU-945 Related Classifications

HY-144680 Related Classifications