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Chemical Structure| 845272-21-1 Chemical Structure| 845272-21-1

Structure of Varlitinib
CAS No.: 845272-21-1

Chemical Structure| 845272-21-1

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Varlitinib is a selective and potent ErbB1 (EGFR) and ErbB2 (HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively.

Synonyms: ARRY-334543; ASLAN001

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Product Details of Varlitinib

CAS No. :845272-21-1
Formula : C22H19ClN6O2S
M.W : 466.94
SMILES Code : C[C@H]1N=C(NC2=CC3=C(NC4=CC=C(OCC5=NC=CS5)C(Cl)=C4)N=CN=C3C=C2)OC1
Synonyms :
ARRY-334543; ASLAN001
MDL No. :MFCD20275099

Safety of Varlitinib

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H318-H400
Precautionary Statements:P280-P305+P351+P338+P310
Class:9
UN#:3077
Packing Group:

Related Pathways of Varlitinib

RTK
JAK-STAT

Isoform Comparison

Biological Activity

Target
  • EGFR/ErbB1

    ErbB1, IC50:7 nM

  • HER2/ErbB2

    ErbB2, IC50:2 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Primary astrocytes 5 µM 5.5 h To evaluate the effect of Varlitinib on LPS-induced astrocyte inflammatory responses, results showed that Varlitinib significantly reduced LPS-induced il-1b mRNA levels, AKT signaling, and nlrp3 inflammasome activation. PMC9632417
BV2 microglial cells 5 µM 5.5 h To evaluate the effect of Varlitinib on LPS-induced inflammatory responses, results showed that Varlitinib significantly reduced LPS-stimulated il-1b and inos mRNA levels and downregulated AKT/FAK/NF-kB signaling. PMC9632417
KKU-100 2.5, 5, 10 µM 72 h Varlitinib significantly suppressed colony formation in KKU-100 cells at 10 µM and induced G1 phase arrest. PMC7296552
KKU-214 2.5, 5, 10 µM 72 h Varlitinib significantly inhibited colony formation of KKU-214 cells in a dose-dependent manner and induced G1 phase arrest, reducing S phase progression. PMC7296552
Primary astrocytes 5 µM 5.5 h To evaluate the effect of Varlitinib on LPS-induced astrocyte inflammatory responses, results showed that Varlitinib significantly reduced LPS-stimulated il-1b mRNA levels and downregulated AKT signaling and nlrp3 inflammasome activation. PMC9632417
BV2 microglial cells 5 µM 5.5 h To evaluate the effect of Varlitinib on LPS-induced inflammatory responses, results showed that Varlitinib significantly reduced LPS-stimulated il-1b and inos mRNA levels and downregulated AKT/FAK/NF-kB signaling. PMC9632417

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice LPS-treated mouse model Intraperitoneal injection 20 mg/kg Once daily for 7 consecutive days To evaluate the effect of Varlitinib on LPS-induced neuroinflammatory responses, results showed that Varlitinib significantly reduced LPS-stimulated glial activation and IL-1b/NLRP3 inflammasome formation. PMC9632417
BALB/c AJcl-nu/nu mice CCA xenograft model Oral 25, 50, 100 mg/kg Once daily for 15 days Varlitinib significantly suppressed tumor growth at doses of 50 mg/kg and 100 mg/kg without noticeable toxicity. PMC7296552
Mice Wild-type mice Intraperitoneal injection 20 mg/kg Daily for 7 consecutive days To evaluate the effect of Varlitinib on LPS-induced neuroinflammatory responses, results showed that Varlitinib significantly reduced LPS-stimulated glial activation and IL-1b/NLRP3 inflammasome formation. PMC9632417

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01614522 Stomach Neoplasms|Cancer of St... More >>omach|Cancer of the Stomach|Gastric Cancer|Gastric Neoplasms Less << PHASE2 COMPLETED 2025-03-13 Seoul National University Hosp... More >>ital, Bundang, Seoul, 463-707, Korea, Republic of|Seoul National University Hospital, Seoul, 110-744, Korea, Republic of Less <<
NCT03368846 Healthy Volunteers PHASE1 COMPLETED 2017-12-14 Quotient Clinical Ltd, Notting... More >>ham, United Kingdom Less <<
NCT02609958 Cholangiocarcinoma PHASE2 COMPLETED 2017-10-11 Seoul, Korea, Republic of|Sing... More >>apore, Singapore|Taipei, Taiwan Less <<
NCT03499626 Advanced/ Metastatic Hepatocel... More >>lular Carcinoma Less << PHASE1|PHASE2 UNKNOWN 2021-05-05 National University Hospital, ... More >>Singapore, 119228, Singapore Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.71mL

2.14mL

1.07mL

21.42mL

4.28mL

2.14mL

References

 

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