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 番号: 1005781-50-9
- 分子式: C19H15N5O2
- 分子量:345.35
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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.
化学情報
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CAS 番号 1005781-50-9
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分子量 345.35
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
TPKI-39 関連分類
HY-181754 関連分類
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