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PD168393

PD168393 是一种细胞渗透性的选择性 EGFR 酪氨酸激酶和 ErbB2的抑制剂。它不可逆转地失活 EGF 受体，IC50值为 0.7 nM，但对胰岛素受体、PDGFR、FGFR 和 PKC 无作用。

CAS号

194423-15-9

分子式

C17H13BrN4O

主要靶点

Autophagy|Apoptosis|PKC|FGFR|EGFR|IGF-1R|PDGFR

仅限科研使用

Cat No : CM03927

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Synonyms

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  • CAS No.: 194423-15-9

    PD168393
    CAS#: 194423-15-9

产品信息

PD168393 is an irreversible EGFR inhibitor (IC50: 0.70 nM), irreversibly alkylate Cys-773; inactive against PKC, FGFR, PDGFR, and insulin.

CAS号 194423-15-9
分子式 C17H13BrN4O
主要靶点 Autophagy|Apoptosis|PKC|FGFR|EGFR|IGF-1R|PDGFR
主要通路 血管生成|JAK/STAT信号通路|表观遗传|蛋白酪氨酸激酶|凋亡|自噬|细胞骨架
分子量 369.22
纯度 99.13%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

EGFR:0.70 nM

体内活性

PD 168393 produces tumor growth inhibition of 115% in A431 human epidermoid carcinoma xenograft in nude mice, with 50% reduced phosphotyrosine content of EGFR. PD 168393 also shows a low plasma concentration. [1]

体外活性

PD 168393 is docked into the ATP binding pocket of EGFR TK. PD168393 completely suppresses EGF-dependent receptor autophosphorylation in A431 cells during continuous exposure, with continous suppression even after 8 hr in compound-free medium. PD168393 inhibits heregulin-induced tyrosine phosphorylation in MDA-MB-453 cells with IC50 of 5.7 nM. PD168393 is inactive against insulin, PDGF and basic FGFR TKs as well as PKC. PD168393 inhibits EGF-mediated tyrosine phosphorylation in HS-27 human fibroblasts with IC50 of 1-6 nM but has little effect on FGF- or PDGF-mediated tyrosine phosphorylation. [1] PD168393 shows rapid and potent inhibition of Her2-induced tyrosine phosphorylation with IC50 of ~100 nM in 3T3-Her2 cells. D168393 also inhibits phosphorylation of PLCγ1/Stat1/Dok1/δ-catenin in 3T3-Her2 cells, except for Fyb. [2]

溶解度

Ethanol:<1 mg/mL,H2O:<1 mg/mL,DMSO:68 mg/mL (184.2 mM)

参考文献

1.Fry W, et al. Proc Natl Acad Sci U S A. 1998, 95(20), 12022-12027.
2.Bose R, et al. Proc Natl Acad Sci U S A, 2006, 103(26), 9773-9778.

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