1. Protein Tyrosine Kinase/RTK Apoptosis PI3K/Akt/mTOR Cell Cycle/DNA Damage
  2. PDGFR FLT3 Apoptosis Akt PERK Bcl-2 Family
  3. Ki11502

Ki11502 是一种多靶点受体酪氨酸激酶 (RTK) 抑制剂,能选择性抑制 PDGF β/α 受体的活性 (IC50 均小于 10 nM)。Ki11502 能选择性的抑制人血管平滑肌细胞中 PDGF β 受体磷酸化、增殖和蛋白聚糖合成。Ki11502 能诱导细胞凋亡 (Apoptosis),对包括具有 Imatinib (HY-15463) 耐药突变在内的特定白血病亚群具有显著的抗增殖作用。Ki11502 非常适合研究 PDGF 在血管疾病中的作用,特别是蛋白聚糖在动脉粥样硬化中的作用。

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Ki11502 Chemical Structure

Ki11502 Chemical Structure

CAS No. : 347155-76-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ki11502 is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the activity of PDGF β/α receptors with IC50 values less than 10 nM. Ki11502 selectively inhibits PDGF β receptor phosphorylation, proliferation, and proteoglycan synthesis in human vascular smooth muscle cells. Ki11502 can induce Apoptosis) and exhibits profound antiproliferative effects on select subsets of leukemia, including those with Imatinib (HY-15463) resistant mutations. Ki11502 is highly suitable for studying the role of PDGF in vascular diseases, particularly the role of proteoglycans in atherosclerosis[1][2].

IC50 & Target

PDGFRα

<10 nM (IC50)

PDGFRβ

<10 nM (IC50)

KIT

86.81 nM (IC50)

KIT670I

427.8 nM (IC50)

FLT3

37.54 nM (IC50)

FLT3D835Y

541.6 nM (IC50)

KDR

210 nM (IC50)

体外研究
(In Vitro)

Ki11502 (0.1-1 nM; 2 天) 在携带激活的 FIP1 样 1/PDGFRα 融合基因的嗜酸性白血病 EOL-1 细胞中显著导致生长停滞、G0/G1 细胞周期停滞和凋亡 (Apoptosis)[2]
Ki11502 (0.1-1 nM; 3 h) 有效降低 EOL-1 细胞中 p-PDGFRα 及其下游信号 (包括 p-Akt、p-ERK 和 p-STAT5) 的水平[2]

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

Western Blot Analysis[2]

Cell Line: EOL-1, MOLM13, MV4-11
Concentration: 0.1 nM; 0.5 nM; 1 nM
Incubation Time: 48 h
Result: Significantly downregulated the levels of Bcl-2, Bcl-xL, and Mcl-1 in EOL-1 cells, drastically reduced the level of Bcl-xL in MV4-11 cells, and notably decreased the expression of Mcl-1 in MOLM13 cells.
体内研究
(In Vivo)

Ki11502 (50 mg/kg; 灌胃; 每天 2 次,连用 5 天) 完全抑制了 SCID 小鼠中肿瘤异种移植物 EOL-1 细胞的增殖[2]

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

分子量

473.54

Formula

C26H23N3O4S

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
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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.

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产品名称:
Ki11502
目录号:
HY-112417
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