1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR
  3. BDTX-189

BDTX-189 

Cat. No.: HY-136789 Purity: 99.94%
Handling Instructions

BDTX-189 is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, including 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.

For research use only. We do not sell to patients.

BDTX-189 Chemical Structure

BDTX-189 Chemical Structure

CAS No. : 2414572-47-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 86 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 86 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
25 mg USD 250 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 750 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

BDTX-189 is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, including 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].

IC50 & Target[1]

EGFR

0.2 nM (Kd)

HER2

0.76 nM (Kd)

RIPK2

1.2 nM (Kd)

BLK

13 nM (Kd)

In Vitro

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].

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

In Vivo

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].

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

Clinical Trial
Molecular Weight

561.03

Formula

C₂₉H₂₉ClN₆O₄

CAS No.
SMILES

C=CC(NC1=CC2=C(NC3=CC=C(OCC4=NC=CC=C4)C(Cl)=C3)N=CN=C2C=C1OCCN5CCOCC5)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (74.27 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7824 mL 8.9122 mL 17.8244 mL
5 mM 0.3565 mL 1.7824 mL 3.5649 mL
10 mM 0.1782 mL 0.8912 mL 1.7824 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.08 mg/mL (3.71 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

BDTX-189BDTX189BDTX 189EGFREpidermal growth factor receptorErbB-1HER1allostericoralinsertionmutantsoncogene athymicnudemiceBa/F3Inhibitorinhibitorinhibit

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BDTX-189
Cat. No.:
HY-136789
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