2. Protein Tyrosine Kinase/RTK Apoptosis
  3. FGFR Apoptosis
  4. LHQ490

LHQ490 is a selective FGFR2 inhibitor, with an IC50 of 5.2 nM. LHQ490 efficiently inhibits the proliferation of BaF3-FGFR2 cells with an IC50 value of 1.4 nM. LHQ490 inhibits FGFR2-driven cancer cell proliferation and induces apoptosis of FGFR2-driven cancer cells.

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LHQ490

LHQ490 Chemical Structure

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Description

LHQ490 is a selective FGFR2 inhibitor, with an IC50 of 5.2 nM. LHQ490 efficiently inhibits the proliferation of BaF3-FGFR2 cells with an IC50 value of 1.4 nM. LHQ490 inhibits FGFR2-driven cancer cell proliferation and induces apoptosis of FGFR2-driven cancer cells[1].

Cellular Effect
Cell Line Type Value Description References
A204 IC50
683 nM
Compound: 9d; LHQ490
Antiproliferation activity against human A204 cells harboring FGFR2 amplification incubated for 72 hrs by CCK8 assay
Antiproliferation activity against human A204 cells harboring FGFR2 amplification incubated for 72 hrs by CCK8 assay
[PMID: 38718625]
BaF3 IC50
1.4 nM
Compound: 9d; LHQ490
Antiproliferation activity against mouse BaF3 cells expressing FGFR2 incubated for 72 hrs by CCK8 assay
Antiproliferation activity against mouse BaF3 cells expressing FGFR2 incubated for 72 hrs by CCK8 assay
[PMID: 38718625]
BaF3 IC50
98.7 nM
Compound: 9d; LHQ490
Antiproliferation activity against mouse BaF3 cells expressing FGFR1 incubated for 72 hrs by CCK8 assay
Antiproliferation activity against mouse BaF3 cells expressing FGFR1 incubated for 72 hrs by CCK8 assay
[PMID: 38718625]
BaF3 IC50
> 1000 nM
Compound: 9d; LHQ490
Antiproliferation activity against mouse BaF3 cells incubated for 72 hrs by CCK8 assay
Antiproliferation activity against mouse BaF3 cells incubated for 72 hrs by CCK8 assay
[PMID: 38718625]
MDA-MB-453 IC50
> 10000 nM
Compound: 9d; LHQ490
Antiproliferation activity against human MDA-MB-453 cells harboring FGFR4 Y367C mutant incubated for 72 hrs by CCK8 assay
Antiproliferation activity against human MDA-MB-453 cells harboring FGFR4 Y367C mutant incubated for 72 hrs by CCK8 assay
[PMID: 38718625]
RT-112 IC50
1790 nM
Compound: 9d; LHQ490
Antiproliferation activity against human RT-112 cells harboring FGFR3-TACC3 incubated for 72 hrs by CCK8 assay
Antiproliferation activity against human RT-112 cells harboring FGFR3-TACC3 incubated for 72 hrs by CCK8 assay
[PMID: 38718625]
SNU-16 IC50
12.9 nM
Compound: 9d; LHQ490
Antiproliferation activity against human SNU-16 cells harboring FGFR2 amplification incubated for 72 hrs by CCK8 assay
Antiproliferation activity against human SNU-16 cells harboring FGFR2 amplification incubated for 72 hrs by CCK8 assay
[PMID: 38718625]
Molecular Weight

528.62

Formula

C30H33FN6O2
SMILES

C=CC(NC1=CC=C(C=C1)C2=C(C3=C(N=CN=C3N2C)N)C4=CC=C(C(F)=C4)C5(COC5)N(C(C)C)CC)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LHQ490 Related Classifications

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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.

Keywords:

LHQ490LHQ 490LHQ-490FGFRApoptosisFibroblast growth factor receptorBaF3-FGFR2proliferationapoptosisInhibitorinhibitorinhibit

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