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BDTX-189 (Synonyms: BDTX-189)

Catalog No.GC60629 Copy One-Click Copy Product Info

BDTX-189 (BDTX-189) es un inhibidor potente, activo por vÍa oral y selectivo de las mutaciones oncogénicas alostéricas de EGFR y HER2, incluidos los mutantes de inserciÓn del exÓn 20 de EGFR/HER2. BDTX-189 muestra KD de 0,2, 0,76, 13 y 1,2 nM para EGFR, HER2, BLK y RIPK2, respectivamente. Actividad anticancerÍgena.

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BDTX-189 Chemical Structure

Cas No.: 2414572-47-5

Tamaño Precio Disponibilidad Cantidad
5mg
63,00 $
Disponible
10mg
108,00 $
Disponible
25mg
225,00 $
Disponible
50mg
405,00 $
Disponible
100mg
675,00 $
Disponible

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Sample solution is provided at 25 µL, 10mM.



Description of BDTX-189

BDTX-189 is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, includes EGFR/HER2 exon 20 insertion mutants. BDTX-189 shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity[1].

BDTX-189 is a masterKey inhibitor of the ERBB allosteric mutant oncogene family with antiproliferative activity (IC50<100 nM for ERBB allosteric mutant oncogene family)[1].

BDTX-189 (0-100 mg/kg; p.o.; daily for 15 dyas) shows dose-dependent tumor growth inhibition and regression in in athymic nude mice bearing HER2 S310F Ba/F3 allograft tumors[1].BDTX-189 (1-50 mg/kg.p.o.; daily for 15 days) shows dose-dependent tumor growth inhibition and regression in athymic nude mice bearing CUTO-14 PDX tumors that express the EGFR mutation EGFR ASV[1].

[1]. Elizabeth Buck, et al. BDTX-189, a Potent and Selective Inhibitor of Allosteric EGFR and HER2 Oncogenic Mutations.

Chemical Properties of BDTX-189

Cas No. 2414572-47-5 SDF
Sinónimos BDTX-189
Canonical SMILES C=CC(NC1=CC2=C(NC3=CC=C(OCC4=NC=CC=C4)C(Cl)=C3)N=CN=C2C=C1OCCN5CCOCC5)=O
Formula C29H29ClN6O4 M.Wt 561.03
Solubility Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of BDTX-189

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1 mg 5 mg 10 mg
1 mM 1.7824 mL 8.9122 mL 17.8244 mL
5 mM 356.5 μL 1.7824 mL 3.5649 mL
10 mM 178.2 μL 891.2 μL 1.7824 mL
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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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Review for BDTX-189

Average Rating: 5 ★★★★★ (Based on Reviews and 9 reference(s) in Google Scholar.)

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