2. Protein Tyrosine Kinase/RTK
  3. Bcr-Abl Src Btk
  4. PDD-87

PDD-87 是一种具有口服活性的、可透过血脑屏障的激酶抑制剂，对 ABL、SRC 家族及 BTK 激酶及其关键突变体的 IC50 值范围为 0.07 nM 至 0.72 nM。PDD-87 可在白血病和淋巴瘤细胞中诱导抗增殖作用，并在小鼠异种移植模型中抑制肿瘤生长。PDD-87 可用于白血病、淋巴瘤的研究。

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PDD-87

PDD-87 Chemical Structure

CAS No. : 2222129-13-5

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PDD-87 相关抗体

Top Publications Citing Use of Products

查看 Bcr-Abl 亚型特异性产品:

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Abl Bcr-Abl

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Lck Fyn Blk Fgr Hck Lyn Yes SRC-3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

PDD-87 (1-5 h) 可强效抑制纯化的 ABL、BTK 和 SRC 家族激酶，其 IC50 值范围为 0.07 至 0.72 nM；在 1 nM 浓度下对其他 SRC 家族成员的抑制率 >82%，在 10 nM 浓度下对 EPHB1 的抑制率约为 91%[1]。
PDD-87 (0.01-1000 nM；48 h) 可强效抑制 K-562、SU-DHL-4 和 SU-DHL-6 白血病/淋巴瘤细胞系的增殖，其 IC50 值分别为 0.30、4.9 和 6.1 nM[1]。
PDD-87 (0-60 min) 在小鼠、大鼠和犬肝微粒体中表现出比 Dasatinib (HY-10181) 更优的代谢稳定性，其内在清除率为低至中等水平；而在猴肝微粒体中，它表现出与 Dasatinib 相当的稳定性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PDD-87 相关抗体:

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.
药代动力学
(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 / / /
体内研究
(In Vivo)

PDD-87 (5-15 mg/kg；口服；每日一次；连续 15 天) 在小鼠 K-562G 异种移植模型中呈剂量依赖性抑制肿瘤生长，在 15 mg/kg 剂量下 TGI 达 81.7%，在 5 mg/kg 剂量下 TGI 达 47.8%[1]。
PDD-87 (50-200 mg/kg；口服；最长 2 周) 在雌性 BALB/c 裸鼠中耐受性良好，最高剂量为每日一次 200 mg/kg 未观察到毒性[1]。

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.
分子量

444.94

Formula

C20H21ClN6O2S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PDD-87 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

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

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