GDC-0980 |CAS:1032754-93-0 Probechem Biochemicals

Chemical Structure : GDC-0980

CAS No.: 1032754-93-0

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GDC-0980 (Apitolisib;GNE 390;GDC0980;RG 7422)

货号: PC-43426Not For Human Use, Lab Use Only.

GDC-0980 (Apitolisib, GNE 390, RG 7422) is a potent, selective, orally available class I PI3K/mTOR inhibitor with IC50 of 5 nM/27 nM/7 nM/14 nM for PI3Kα/β/δ/γ, inhibits mTOR inhibitor with Ki of 17 nM.

规格	价格	库存
10 mg	￥1280	In stock
25 mg	￥2180	In stock
50 mg	￥3580	In stock
100 mg	￥5580	In stock
200 mg		Get quote
1 g		Get quote

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生物&药学活性

GDC-0980 (Apitolisib, GNE 390, RG 7422) is a potent, selective, orally available class I PI3K/mTOR inhibitor with IC50 of 5 nM/27 nM/7 nM/14 nM for PI3Kα/β/δ/γ, inhibits mTOR inhibitor with Ki of 17 nM.
GDC-0980 displays remarkably selectivity for several other members of the closely related PIKK family kinases, including C2alpha, C2beta, VPS34 I, PI4Kalpha, PI4Kbeta and DNA-PK.
GDC-0980 potently inhibits signal transduction downstream of both PI3K and mTOR, reduces viability in multiple cancer cell lines by cell-cycle inhibition and induction of apoptosis (prostate IC50<200 nM, NSCLC lines <200 nM).
GDC-0980 potently inhibits tumor growth in xenograft models with activated PI3K, loss of LKB1 or PTEN.

物理化学性质&存储条件

分子量	498.6011
分子式	C23H30N8O3S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-Propanone, 1-[4-[[2-(2-amino-5-pyrimidinyl)-7-methyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-6-yl]methyl]-1-piperazinyl]-2-hydroxy-, (2S)-

参考文献

1. Wallin JJ, et al. Mol Cancer Ther. 2011 Dec;10(12):2426-36.

2. Sutherlin DP, et al. J Med Chem. 2011 Nov 10;54(21):7579-87.

3. Spoerke JM, et al. Clin Cancer Res. 2012 Dec 15;18(24):6771-83.et al.

4. Makhov PB, et al. Mol Cancer Ther. 2012 Jul;11(7):1510-7.

GDC-0980 (Apitolisib;GNE 390;GDC0980;RG 7422)

生物&药学活性

物理化学性质&存储条件

参考文献

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GDC-0980 (Apitolisib;GNE 390;GDC0980;RG 7422)

生物&药学活性

物理化学性质&存储条件

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