1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. BMS-599626

BMS-599626 (AC480) 是一种选择性的口服生物利用度 HER1HER2 抑制剂,其 IC50 分别为 20 和 30 nM。BMS-599626 对 HER4 的 IC50 值为 190 nM,对 VEGFR2、c-Kit、Lck、MEK 的抑制强度降低了100倍。BMS-599626抑制肿瘤细胞增殖,并有可能增加肿瘤对放疗的反应。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 BMS-599626 Hydrochloride 通常具有更好的水溶性和稳定性。

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BMS-599626 Chemical Structure

BMS-599626 Chemical Structure

CAS No. : 714971-09-2

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BMS-599626 的其他形式现货产品:

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Other Forms of BMS-599626:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献


BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy[1][2].

(In Vitro)

BMS-599626 inhibits the proliferation of tumor cells that are dependent on HER1/HER2 signaling. BMS-599626 (0.03-8 μM; 1 huors) results in the inhibition of receptor autophosphorylation, as well as MAPK phosphorylation, with IC50s of 0.3 and 0.22 μM, respectively, in Sal2 cells which express a CD8HER2 fusion protein[1].
BMS-599626 abrogates HER1 and HER2 signaling and inhibited the proliferation of tumor cell lines that are dependent on these receptors, with IC50 in the range of 0.24 to 1 μM.In GEO cells, HER1 phosphorylation is stimulated by treatment with EGF and is inhibited by BMS-599626 (IC50=0. 75 μM).There is also nearly complete inhibition of EGF-dependent MAPK (0. 8 μM) but only partial inhibition of AKT signaling.The latter likely reflects the activation of AKT by multiple upstream signals.Treatment of N87 cells with BMS-599626 leads to the inhibition of HER2 (0. 38 μM), which is expressed to a high level because of gene amplification, as well as MAPK and AKT phosphorylation (0.35 μM for both)[1].
At the molecular level, in HN-5 cells the agent inhibited the expression of pEGFR, pHER2, cyclins D and E, pRb, pAkt, pMAPK, pCDK1 and 2, CDK 6, and Ku70 proteins. The drug also induced accumulation of cells in the G1 cell cycle phase, inhibited cell growth, enhanced radiosensitivity, and prolonged the presence of γ-H AX foci up to 24 h after radiation[2].

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

(In Vivo)

BMS-599626 (60-240 mg/kg; p.o.; daily for 14 days) results in a dose-dependent inhibition of Sal2 tumor growth[1].
BMS599626 treatment results in the inhibition of GEO xenograft tumor growth when given once daily for 14 days. In addition to efficacy in the Sal2, GEO, and KPL4 models, BMS-599626 has similar antitumor activity in other HER2 amplified xenograft models including the BT474 breast and N87 gastric tumors, as well as other HER1-overexpressing non-small-cell lung tumors (A549 and L2987)[1].
BMS599626 given before and during irradiation improved the radioresponse of HN5 tumors in vivo[2].

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

Animal Model: Athymic female nude mice (nu/nu mice, Sal2 tumor model)[1]
Dosage: 60, 120, 240 mg/kg
Administration: Oral; daily for 14 days
Result: Resulted in a dose-dependent inhibition of Sal2 tumor growth.
Clinical Trial





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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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