There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
10074-G5 is effective in hindering the proliferation of Daudi Burkitt's lymphoma cells and in interfering with the dimerization of c-Myc/Max. It exhibits IC50 values of 15.6 μM for Daudi cells and 13.5 μM for HL-60 cells[1]. 10074-G5 interacts with the Myc peptide Myc353-437, exhibiting a Kd value of 2.8 μM within the Arg363-Ile381 region. It attaches within a pocket formed by a bend (Asp379-Ile381) at the N-terminal end of an induced helical segment (Leu370–Arg378)[2].
10074-G5 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Myc-Cap cells
25 μM
24 h
Evaluate the effect of Myc inhibitors on GFAT1 expression and protein glycosylation. Results showed that 10074-G5 significantly upregulated GFAT1 expression and increased protein glycosylation levels.
Theranostics. 2023 Jan 1;13(2):578-595.
RM1 cells
25 μM
24 h
Evaluate the effect of Myc inhibitors on GFAT1 expression and protein glycosylation. Results showed that 10074-G5 significantly upregulated GFAT1 expression and increased protein glycosylation levels.
Theranostics. 2023 Jan 1;13(2):578-595.
PC3 cells
25 μM
24 h
Evaluate the effect of Myc inhibitors on GFAT1 expression and protein glycosylation. Results showed that 10074-G5 significantly upregulated GFAT1 expression and increased protein glycosylation levels.
Theranostics. 2023 Jan 1;13(2):578-595.
monomeric Aβ40
200 μM
measure heat changes upon 10074-G5 binding to Aβ40 using isothermal titration calorimetry, indicating the interaction is largely entropic
Sci Adv. 2020 Nov 4;6(45):eabb5924.
monomeric Aβ42
20 μM
characterize the binding of 10074-G5 to monomeric Aβ42, finding Aβ42 remains disordered in the bound form
Sci Adv. 2020 Nov 4;6(45):eabb5924.
HL-60 human promyelocytic leukemic cells
13.5 ± 2.1 μM
72 h
To evaluate the growth inhibitory potency of 10074-G5 against HL-60 cells, results showed that 10074-G5 effectively inhibited cell growth
J Pharmacol Exp Ther. 2010 Dec;335(3):715-27.
Daudi Burkitt’s lymphoma cells
15.6 ± 1.5 μM
72 h
To evaluate the growth inhibitory potency of 10074-G5 against Daudi cells, results showed that 10074-G5 effectively inhibited cell growth
J Pharmacol Exp Ther. 2010 Dec;335(3):715-27.
human renal proximal tubule cells (RPTCs)
30 μM
3 h
Pre-treatment with 10074-G5 completely restored FEN-stimulated cAMP accumulation in uRPTCs to normal levels.
Hypertension. 2013 May;61(5):1021-7.
human renal proximal tubule cells (RPTCs)
30 μM
24 h
10074-G5 completely blocked the PMA-mediated increase in GRK4 expression, restoring GRK4 expression to basal levels.
Hypertension. 2013 May;61(5):1021-7.
ALK+ALCL cells
5 μM
24 h
Inhibits MYC-MAX heterodimerization and their DNA binding, significantly abrogating H2O2-induced RU/RR conversion
BMC Cancer. 2018 Apr 2;18(1):361.
10074-G5 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6J mice
RM-1 prostate cancer model
Intravenous injection
10 mg/kg
Once every 3 days, total 5 times
Evaluate the antitumor activity of 10074-DON-loaded PS nanocarrier in vivo. Results showed that PS/10074-DON significantly inhibited tumor growth and improved the tumor immune microenvironment.
Theranostics. 2023 Jan 1;13(2):578-595.
C.B-17 SCID mice
Daudi Burkitt’s lymphoma xenografts
Intravenously
20 mg/kg
Once daily for 5 days
To evaluate the antitumor efficacy of 10074-G5 in vivo, results showed that 10074-G5 did not significantly inhibit the growth of Daudi xenografts
J Pharmacol Exp Ther. 2010 Dec;335(3):715-27.
10074-G5 动物研究
Animal study
In mice administered an intravenous dose of 20 mg/kg of 10074-G5, the plasma half-life is recorded at 37 minutes. The peak plasma concentration reaches 58 μM, a level that is ten times greater than the highest concentration found in tumors[1].
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