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
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    CDK
    Raf
    JAK
  4. BI-1622

BI-1622 

Cat. No.: HY-150023 Purity: 98.97%
COA Handling Instructions

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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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].

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

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].

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

Appearance

Solid

Formula

C26H24N10O2
CAS No.
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)

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
10 mM 0.1966 mL 0.9832 mL 1.9665 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation
References
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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.

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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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