TPKI-39
TPKI-39 is a DDR1, DDR2, and FLT1 inhibitor, with a human DDR1 IC50 of 380 nM, human DDR1 Ka of 24 nM, human DDR2 IC50 of 120 nM, human FLT1 IC50 of 65 nM, and human FLT1 Ka of 91 nM.TPKI-39 inhibits DDR1 enzymatic activity and autophosphorylation, DDR2 enzymatic activity, and FLT1 enzymatic activity in cells.TPKI-39 inhibits collagen-induced DDR1 autophosphorylation in cells.
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- CAS No.: 1005781-50-9
- 화학식: C19H15N5O2
- 분자량:345.35
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
TPKI-39 (1 μM; dose-response) potently engages DDR1, DDR2, and FLT1 in live HEK293 cells, with minimal to no engagement of most kinases identified as high-affinity binders in cell-free assays, and uniquely engages DDR2 in cells but not in cell-free systems[1].
TPKI-39 (0.313-5 μM; 1 h pretreatment, 24 h cotreatment with collagen I) potently inhibits DDR1 signaling (autophosphorylation) in HeLa cells stimulated with collagen I[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells (transiently transfected with DDR1b-encoding cDNA)
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Concentration:0.313-5 μM (pretreated; cotreated with collagen I)
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Incubation Time:1 h (pretreatment); 24 h (cotreatment with collagen I)
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Result:Dose-dependently inhibited collagen-induced DDR1 autophosphorylation.
Reduced phosphorylation to basal levels (observed without collagen activation) at concentrations ≥1.25 μM, comparable to the established DDR1 inhibitor DDR1-IN-1.
Chemical Information
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CAS No. 1005781-50-9
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분자량 345.35
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화학식 C19H15N5O2
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SMILES
O=C(NC1=CC=CC(OC2=NN3C=CN=C3C=C2)=C1)NC4=CC=CC=C4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TPKI-39 Related Classifications
HY-181754 Related Classifications
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