2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Cell Cycle/DNA Damage MAPK/ERK Pathway Stem Cell/Wnt Epigenetics
  3. EGFR Itk PI4K Btk CDK Raf JAK
  4. BI-1622

BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile.

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

BI-1622 Chemical Structure

BI-1622 Chemical Structure

CAS No. : 2681392-19-6

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Based on 1 publication(s) in Google Scholar

BI-1622 Related Antibodies

Top Publications Citing Use of Products

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

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PI4KIIIβ PI4KIIIα PI4K PI4KII

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

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BRaf c-Raf Raf

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JAK1 JAK2 JAK3 Tyk2 JAK

  • Biological Activity

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Description

BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile[1].

IC50 & Target

HER2

7 nM (IC50)

ErbB4

 

EGFR

 

CDK11B

 

JAK3

 

In Vitro

BI-1622 (0-5 µM, 72 h or 96 h) inhibits the proliferation of HER2-dependent cell lines[1].
BI-1622 induces a dose-dependent decrease in pHER2 and pERK levels in NCI-H2170 HER2YVMA and PC-9 HER2YVMA cells with an accompanying decrease in DUSP6 messenger RNA levels[1].
BI-1622 displays good permeability and no PgP-mediated efflux liability[1].
BI-1622 shows good in vitro clearance in mouse liver microsomes and mouse hepatocytes[1].

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

BI-1622 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Ba/F3 cells
Concentration: 0-5 µM
Incubation Time: 72 h or 96 h
Result: Potently inhibited the proliferation of cancer cell lines dependent on amplified HER2 or an NRG-1 fusion. Inhibited different HER2 oncogenic variants and HER2WT with IC50 values below 50 nM in tumor cell lines, while sparing EGFRWT-driven cells.
In Vivo

BI-1622 (1 mg/kg, IV; 10 and 100 mg/kg, Orally; once) shows moderate clearance, a moderate volume of distribution, and good to moderate bioavailability[1].
BI-1622 (0-100 mg/kg, orally, twice daily) inhibits tumor growth and inhibits oncogenic signaling in vivo[1].

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

Animal Model: Female NMRI-Foxn1nu mice (6-8 weeks old, 8-10 mice per cage, engrafted subcutaneously with PC-9 HER2YVMA, NCI-H2170 HER2YVMA or NCI-N87 cells)[1]
Dosage: 10, 30 and 100 mg/kg
Administration: orally, twice daily
Result: In the NCI-H2170 HER2YVMA mechanistic model, 100 mg/kg twice daily BI-1622 resulted in a delay in tumor growth (73% TGI). In the ST3107 HER2 exon 20 mutant model, both BI-4142 (100 mg/kg twice daily) resulted in tumor regressions.
Animal Model: NMRI Foxn1nu mice (n=3 per group)[1]
Dosage: 1 mg/kg (IV); 10 and 100 mg/kg (Orally)
Administration: IV, Orally; once (Pharmacokinetic Analysis)
Result: Showed moderate in vivo clearance (50% hepatic blood flow), a moderate volume of distribution, and good to moderate bioavailability of up to 68%.
Molecular Weight

508.53

Formula

C26H24N10O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N1CCN(CC1)C2=NC3=C(NC4=CC=C(C(C)=C4)OC5=CC6=NC=NN6C=C5)N=CN=C3C=N2)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 (196.65 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 1.9665 mL 9.8323 mL 19.6645 mL
5 mM 0.3933 mL 1.9665 mL 3.9329 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.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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 1.9665 mL 9.8323 mL 19.6645 mL 49.1613 mL
5 mM 0.3933 mL 1.9665 mL 3.9329 mL 9.8323 mL
10 mM 0.1966 mL 0.9832 mL 1.9665 mL 4.9161 mL
15 mM 0.1311 mL 0.6555 mL 1.3110 mL 3.2774 mL
20 mM 0.0983 mL 0.4916 mL 0.9832 mL 2.4581 mL
25 mM 0.0787 mL 0.3933 mL 0.7866 mL 1.9665 mL
30 mM 0.0655 mL 0.3277 mL 0.6555 mL 1.6387 mL
40 mM 0.0492 mL 0.2458 mL 0.4916 mL 1.2290 mL
50 mM 0.0393 mL 0.1966 mL 0.3933 mL 0.9832 mL
60 mM 0.0328 mL 0.1639 mL 0.3277 mL 0.8194 mL
80 mM 0.0246 mL 0.1229 mL 0.2458 mL 0.6145 mL
100 mM 0.0197 mL 0.0983 mL 0.1966 mL 0.4916 mL
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BI-1622 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-16222681392-19-6BI1622BI 1622EGFRItkPI4KBtkCDKRafJAKEpidermal growth factor receptorErbB-1HER1Interleukin-2 inducible T-cell kinaseIL2 inducible T-cell kinasePhosphatidylinositol 4 kinasesPI4 kinasesBruton tyrosine kinaseCyclin dependent kinaseRaf kinasesJanus kinaseBa/F3 cellsNCI-H1781 cellsHEK 293 cellsH2170PC9 cellsorally activeantitumorInhibitorinhibitorinhibit

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