2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. BI-4142

BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC50 of 5 nM.

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

BI-4142 Chemical Structure

BI-4142 Chemical Structure

CAS No. : 2682003-36-5

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1 mg USD 220 In-stock
5 mg USD 560 In-stock
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25 mg USD 1450 In-stock
50 mg USD 1980 In-stock
100 mg USD 2980 In-stock
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Based on 1 publication(s) in Google Scholar

BI-4142 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC50 of 5 nM[1].

IC50 & Target

HER2

5 nM (IC50)

In Vitro

BI-4142 shows inhibition with IC50 values of 10 nM, 18 nM, 270 nM and 2400 nM against HEK HER2YVMA, Ba/F3 HER2YVMA, HEK EGFRWT and Ba/F3 EGFRWT, respectively[1].
BI-4142 (1 nM-5 μM, 72 h or 96 h) shows antiproliferative activity against tumor cells[1].
BI-4142 displays good permeability and no PgP-mediated efflux liability in the CaCo-2 assay[1].
BI-4142 inhibits HER2-dependent cell lines and inhibits downstream signaling[1].

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

BI-4142 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: NCI-H2170 HER2WT, NCI-H2170 HER2YVMA, A431 EGFRWT, Ba/F3 HER2YVMA, Ba/F3 HER2YVMA,S783C, Ba/F3 EGFRWT and Ba/F3 EGFRC775S cells
Concentration: 1 nM-5 μM
Incubation Time: 72 h or 96 h
Result: Showed antiproliferative effect with IC50 values of 16 nM, 82 nM, >5 µM, 4 nM, 24 nM, 718 nM and 43 nM against NCI-H2170 HER2WT, NCI-H2170 HER2YVMA, A431 EGFRWT, Ba/F3 HER2YVMA, Ba/F3 HER2YVMA,S783C, Ba/F3 EGFRWT and Ba/F3 EGFRC775S, respectively.
In Vivo

BI-4142 (0-100 mg/kg; p.o.; twice per day for 40 days) inhibits tumor growth and inhibits oncogenic signaling[1].

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

Animal Model: NMRI-Foxn1nu mice, PC-9 HER2YVMA xenograft model[1]
Dosage: 3, 10, 30 and 100 mg/kg
Administration: Oral administration, twice per day for 40 days
Result: Resulted in tumor regressions in a dose-dependent manner (113%, 126%, 153% and 166% tumor growth inhibition at 3, 10, 30 and 100 mg/kg, respectively).
Animal Model: BomTac:NMRI Foxn1nu mice[1]
Dosage: 1 mg/kg or 10mg/kg and 100 mg/kg
Administration: IV for 1 mg/kg, PO for 10mg/kg and 100 mg/kg (Pharmacokinetic Analysis)
Result: In vivo mouse PK data for BI-4142[1]
Compound Dose iv/po
(mg/kg)		 tmax
(h)		 Cmax
(nM)		 AUD
(h•nM)		 Plasma CL
(mL/min/kg)		 % F
i.v., 1mg/kg n/a n/a 3,280 9.69 n/a
BI-4142 p.o., 10 mg/kg 0.83 8,600 23,200 n/a 71
p.o., 100 mg/kg 0.67 36,400 196,000 n/a 60
Molecular Weight

521.57

Formula

C28H27N9O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N1CCN(CC1)C2=NC=C3N=CN=C(C3=N2)NC4=CC=C(C(C)=C4)OC5=CC(N=CN6C)=C6C=C5)C=C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (191.73 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 1.9173 mL 9.5864 mL 19.1729 mL
5 mM 0.3835 mL 1.9173 mL 3.8346 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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V1

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C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.39%

COA (247 KB) LCMS (173 KB)

Handling Instructions (2659 KB)
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9173 mL 9.5864 mL 19.1729 mL 47.9322 mL
5 mM 0.3835 mL 1.9173 mL 3.8346 mL 9.5864 mL
10 mM 0.1917 mL 0.9586 mL 1.9173 mL 4.7932 mL
15 mM 0.1278 mL 0.6391 mL 1.2782 mL 3.1955 mL
20 mM 0.0959 mL 0.4793 mL 0.9586 mL 2.3966 mL
25 mM 0.0767 mL 0.3835 mL 0.7669 mL 1.9173 mL
30 mM 0.0639 mL 0.3195 mL 0.6391 mL 1.5977 mL
40 mM 0.0479 mL 0.2397 mL 0.4793 mL 1.1983 mL
50 mM 0.0383 mL 0.1917 mL 0.3835 mL 0.9586 mL
60 mM 0.0320 mL 0.1598 mL 0.3195 mL 0.7989 mL
80 mM 0.0240 mL 0.1198 mL 0.2397 mL 0.5992 mL
100 mM 0.0192 mL 0.0959 mL 0.1917 mL 0.4793 mL
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BI-4142 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.

Keywords:

BI-41422682003-36-5BI4142BI 4142EGFREpidermal growth factor receptorErbB-1HER1HEKBa/F3PC-9antitumorInhibitorinhibitorinhibit

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