GDC-0077 (RG6114)

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库存: 现货

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促销价

数量
5mg

￥4850.00

3880.00

- +
10mg

￥8100.00

6480.00

- +
25mg

￥11337.00

9070.00

- +
50mg

￥17950.00

14360.00

- +
100mg

￥29175.00

23340.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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Background

Inavolisib (GDC-0077, RG6114, RO-7113755) is a potent selective inhibitor of PI3K alpha (PI3Kα) with an IC50 of 0.038 nM. GDC-0077 is >300-fold more selective for PI3K alpha over the other class I PI3K isoforms (beta, delta, and gamma) and >2000-fold more selective over PIK family members. GDC-0077 binds to the ATP binding site of PI3K and inhibits the phosphorylation of PIP2 to PIP3.

GDC-0077 potently inhibits mutant PI3K pathway signaling and cell viability through unique HER2-dependent mutant p110a degradation.[2]

GDC-0077 treatment at the MTD in vivo results in tumor regressions in multiple PIK3CA-mutant xenograft and patient-derived xenograft models.[2]

[1] R Hong, et al. Cancer Research, DOI: 10.1158/1538-7445.SABCS17-PD4-14 [2] Song KW, et al. Cancer Discov. 2022 Jan;12(1):204-219.