Home Cart Sign in  
Chemical Structure| 1032754-81-6 Chemical Structure| 1032754-81-6

Structure of GNE-477
CAS No.: 1032754-81-6

Chemical Structure| 1032754-81-6

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

GNE-477 is a potent dual PI3K (IC50=4 nM)/mTOR (Ki=21 nM) inhibitor.

Synonyms: GNE-477

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

Product Details of GNE-477

CAS No. :1032754-81-6
Formula : C21H28N8O3S2
M.W : 504.63
SMILES Code : NC1=NC=C(C2=NC(N3CCOCC3)=C4C(C(C)=C(CN5CCN(S(=O)(C)=O)CC5)S4)=N2)C=N1
Synonyms :
GNE-477
MDL No. :MFCD20527726

Safety of GNE-477

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H317-H319
Precautionary Statements:P280-P305+P351+P338

Related Pathways of GNE-477

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • p110α

    PI3Kα, IC50:4 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
U251 cells 0, 0.125, 0.25, 0.5, 1, 2, 4, 8, 16 or 32 µM 24 or 48 hours To evaluate the inhibitory effect of GNE-477 on the proliferation of U251 cells. The results showed that GNE-477 significantly inhibited the proliferation of U251 cells with an IC50 value of 0.4171 µmol/L. Front Pharmacol. 2021 Jul 26;12:659511
U87 cells 0, 0.125, 0.25, 0.5, 1, 2, 4, 8, 16 or 32 µM 24 or 48 hours To evaluate the inhibitory effect of GNE-477 on the proliferation of U87 cells. The results showed that GNE-477 significantly inhibited the proliferation of U87 cells with an IC50 value of 0.1535 µmol/L. Front Pharmacol. 2021 Jul 26;12:659511
HK-2 renal epithelial cells and primary human renal epithelial cells 50 nM GNE-477 was completely ineffective and non-cytotoxic in HK-2 renal epithelial cells and primary human renal epithelial cells. Aging (Albany NY). 2020 May 18;12(10):9489-9499
RCC2 and RCC3 cells 50 nM GNE-477 potently inhibited cell viability, proliferation, and migration in RCC2 and RCC3 cells. Aging (Albany NY). 2020 May 18;12(10):9489-9499
RCC1 cells 50 nM 24 hours GNE-477 suppressed in vitro cell migration and invasion in RCC1 cells. Aging (Albany NY). 2020 May 18;12(10):9489-9499
RCC1 cells 50 nM 48 hours GNE-477 robustly inhibited EdU incorporation (cell proliferation) and cell cycle progression (decreased S phase, increased G1 phase) in RCC1 cells. Aging (Albany NY). 2020 May 18;12(10):9489-9499
RCC1 cells 1-100 nM 24-96 hours GNE-477 significantly decreased CCK-8 viability in RCC1 cells in a dose- and time-dependent manner. Aging (Albany NY). 2020 May 18;12(10):9489-9499

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice Intracranial xenograft model Tail vein injection 25 mg/kg Every other day for 7 consecutive times To evaluate the inhibitory effect of GNE-477 on intracranial glioblastoma growth. The results showed that GNE-477 significantly inhibited tumor growth and reduced the expression levels of P-AKT, P-mTOR, Bcl-2, and CyclinD1, while increasing the expression of Bax and Bad proteins. Front Pharmacol. 2021 Jul 26;12:659511
Nude mice RCC1 xenograft tumor model Intraperitoneal injection 10 or 50 mg/kg Daily for 3 weeks GNE-477 potently inhibited RCC1 xenograft tumor growth in nude mice with no apparent toxicities. Aging (Albany NY). 2020 May 18;12(10):9489-9499

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.91mL

1.98mL

0.99mL

19.82mL

3.96mL

1.98mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

Historical Records

Categories