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Tizaterkib (AZD-0364) is a potent and selective ERK2 inhibitor.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $96 | In Stock | |
2 mg | $139 | In Stock | |
5 mg | $231 | In Stock | |
10 mg | $393 | In Stock | |
25 mg | $658 | In Stock | |
50 mg | $937 | In Stock | |
1 mL x 10 mM (in DMSO) | $242 | In Stock |
Description | Tizaterkib (AZD-0364) is a potent and selective ERK2 inhibitor. |
Targets&IC50 | ERK2:0.6 nM |
In vitro | AZD-0364 is measured in the ERK2 mass spectrometry and A375 phospho-p90RSK assays (IC50s: 0.6 nM and 5.7 nM). AZD-0364 can inhibit the growth of a panel of cancer cell lines (A549, H2122, H2009, and Calu6 cell lines) with KRAS mutations as monotherapy. |
In vivo | In the A549 xenograft model, Selumetinib is dosed twice daily (BiD) 8 hours apart and AZD-0364 ethanesulfonic acid is dosed once daily (QD) 4 hours after the first Selumetinib dose. Both compounds are dosed continuously for 3 weeks. Both vehicles are dosed in the vehicle group. Both Selumetinib and AZD-0364 ethanesulfonic acid reduce tumor growth relative to vehicle-only control. The combination of Selumetinib and AZD-0364 ethanesulfonic acid results in a reduction in tumor growth. |
Alias | AZD-0364 |
Molecular Weight | 494.5 |
Formula | C24H24F2N8O2 |
Cas No. | 2097416-76-5 |
Smiles | COC[C@H]1Cn2cc(nc2C(=O)N1Cc1ccc(F)c(F)c1)-c1nc(Nc2ccnn2C)ncc1C |
Relative Density. | 1.45 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (202.22 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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