PDD-87
PDD-87 is an orally active, blood-brain barrier permeable kinase inhibitor, with IC50 values ranging from 0.07 nM to 0.72 nM against ABL, SRC family, BTK kinases and their key mutants. PDD-87 induces antiproliferative effects in leukemia and lymphoma cells, and inhibits tumor growth in mouse xenograft models. PDD-87 can be used for the research of leukemia and lymphoma.
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- CAS No.: 2222129-13-5
- Formule: C20H21ClN6O2S
- Masse moléculaire:444.94
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
PDD-87 (1-5 h) potently inhibits purified ABL, BTK and SRC family kinases, with IC50 values ranging from 0.07 to 0.72 nM; it exhibits an inhibition rate of >82% against other SRC family members at a concentration of 1 nM, and an inhibition rate of approximately 91% against EPHB1 at a concentration of 10 nM[1].
PDD-87 (0.01-1000 nM; 48 h) potently inhibits the proliferation of K-562, SU-DHL-4 and SU-DHL-6 leukemia/lymphoma cell lines, with IC50 values of 0.30, 4.9 and 6.1 nM, respectively[1].
PDD-87 (0-60 min) exhibits better metabolic stability than Dasatinib (HY-10181) in mouse, rat and dog liver microsomes, with low to moderate intrinsic clearance; while in monkey liver microsomes, it shows comparable stability to Dasatinib[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K-562, SU-DHL-4, and SU-DHL-6 leukemia/lymphoma cell lines
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Concentration:0.01-1000 nM
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Incubation Time:48 h
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Result:Inhibited K-562 cell proliferation with an IC50 of 0.30 nM.
Inhibited SU-DHL-4 cell proliferation with an IC50 of 4.9 nM.
Inhibited SU-DHL-6 cell proliferation with an IC50 of 6.1 nM.
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Cell Line:46 leukemia and lymphoma cell lines
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Concentration:10 μM and nine 3-fold serial dilutions
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Incubation Time:72 h
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Result:Exhibited potent inhibition (IC50 < 0.1 μM) in KU812, MEG-01, K-562, SU-DHL-4, Pfeiffer, WSU-NHL, DOHH-2, SU-DHL-6, and Daudi cell lines.
Exhibited moderate inhibition (IC50 0.1-1 μM) in U-2932, SU-DHL-5, OCI-LY7, JVM-2, HBL-1, SUP-B15, and KARPAS-422 cell lines.
Exhibited inhibition with IC50 1-10 μM in NALM-6, JVM-3, NAMALWA, CA46, A3/KAW, Z-138, and JK28 cell lines.
Showed IC50 exceeding 10 μM for the remaining tested cell lines.
PDD-87 (50-200 mg/kg; p.o.; up to 2 weeks) is well tolerated in female BALB/c nude mice, with no toxicity observed at the highest dose of 200 mg/kg once daily[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD.SCID (female, 12 weeks old, body weight 20.6-29.1 g, subcutaneous inoculation of imatinib-resistant K-562G cells)[1]
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Dosage:5 mg/kg; 15 mg/kg
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Administration:p.o.; daily; 15 days
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Result:Reduced mean tumor weight from 1572.8 mg (vehicle control) to 820.6 mg, resulting in a tumor growth index (TGI) of 47.8% and a treatment-to-control ratio (T/C) of 52.2% (p = 0.008).
Reduced mean tumor weight to 287.1 mg, achieving a TGI of 81.7% and a T/C of 18.3% (p < 0.001).
Showed no body weight reduction during treatment.
Chemical Information
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CAS No. 2222129-13-5
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Masse moléculaire 444.94
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Formule C20H21ClN6O2S
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SMILES
ClC1=CC=CC(C)=C1NC(C2=CN=C(NC3=NC(C)=NC(N4CC[C@H](O)C4)=C3)S2)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PDD-87 Related Classifications
HY-183103 Related Classifications
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