2. Protein Tyrosine Kinase/RTK
  3. Bcr-Abl Src Btk
  4. 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.

For research use only. We do not sell to patients.

PDD-87

PDD-87 Chemical Structure

CAS No. : 2222129-13-5

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PDD-87 Related Antibodies

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Lck Fyn Blk Fgr Hck Lyn Yes SRC-3

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Description

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[1].

In Vitro

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.

PDD-87 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: K-562, SU-DHL-4, and SU-DHL-6 leukemia/lymphoma cell lines
Concentration: 0.01-1000 nM
Incubation Time: 48 h
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.

Cell Proliferation Assay[1]

Cell Line: 46 leukemia and lymphoma cell lines
Concentration: 10 μM and nine 3-fold serial dilutions
Incubation Time: 72 h
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.
Parmacokinetics
Species Dose Route Tmax T1/2 CL Vd F
Rat[1] 1.0 mg/kg i.v. / 1.6 h 405 mL/h/kg 0.9 L/kg /
Rat[1] 2.5 mg/kg p.o. 0.5 h 6.8 h / / 18.9 %
Mice[1] 5 mg/kg p.o. 1.0 (Plasma) h 2.5 (Plasma) h / / /
In Vivo

PDD-87 (5-15 mg/kg; p.o.; once daily; for 15 consecutive days) inhibits tumor growth in a dose-dependent manner in the mouse K-562G xenograft model, with a TGI of 81.7% at the 15 mg/kg dose and 47.8% at the 5 mg/kg dose[1].
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.

Animal Model: NOD.SCID (female, 12 weeks old, body weight 20.6-29.1 g, subcutaneous inoculation of imatinib-resistant K-562G cells)[1]
Dosage: 5 mg/kg; 15 mg/kg
Administration: p.o.; daily; 15 days
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.
Molecular Weight

444.94

Formula

C20H21ClN6O2S
CAS No.
SMILES

ClC1=CC=CC(C)=C1NC(C2=CN=C(NC3=NC(C)=NC(N4CC[C@H](O)C4)=C3)S2)=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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PDD-87 Related Classifications

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  • 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:

PDD-872222129-13-5PDD87PDD 87Bcr-AblSrcBtkBruton tyrosine kinaseBTKSRC family kinasesleukemialymphomaSU-DHL-4SU-DHL-6ABLmouse xenograft modelsEPHB1K-562Inhibitorinhibitorinhibit

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