- Li T, .et al. Bruton's tyrosine kinase potentiates ALK signaling and serves as a potential therapeutic target of neuroblastoma, Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
- Joo Sang Lee, .et al. Harnessing synthetic lethality to predict the response to cancer treatment, Nat Commun, 2018, 9: 2546 PMID: 29959327
Biological Activity
GDC-0941 is a potent, selective, orally bioavailable inhibitor of class I PI3 kinase (PI3K) , with IC50 values (nM) of 3, 33, 3, 75, 1230 and 580 for p110 α, β, δ and γ isoforms, DNA-PK and mTOR respectively.
Targets
Target | Value | |
---|---|---|
p110α | IC50: 3nM | |
p110δ | IC50: 3nM | |
p110β | IC50: 33nM | |
p110γ | IC50: 75nM | |
mTOR | Kiapp | 0.58μM |
C2β | IC50: 0.67μM | |
DNA-PK | IC50: 1.23μM | |
Vps34 | IC50: >10μM |
In vitro (25°C) | DMSO | 40 mg/mL (77.87 mM) | |
Water | Insoluble | ||
Ethanol | Insoluble | ||
In vivo | 2% DMSO+30% PEG 300+5% Tween 80+ddH2O | 4 mg/mL | |
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.1 mM | 19.47 mL | 97.35 mL | 194.7 mL |
0.5 mM | 3.89 mL | 19.47 mL | 38.94 mL |
1 mM | 1.95 mL | 9.74 mL | 19.47 mL |
5 mM | 0.39 mL | 1.95 mL | 3.89 mL |
*The above data is based on the productmolecular weight 513.6 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Catalog Num | A10421 |
---|---|
Actions | Inhibitor |
CAS No. | 957054-30-7 |
Formula | C23H27N7O3S2 |
M. Wt | 513.6 |
Purity | >98% |
Synonyms | GDC0941 |
SMILES | CS(=O)(=O)N1CCN(CC1)CC2=CC3=C(S2)C(=NC(=N3)C4=C5C=NNC5=CC=C4)N6CCOCC6 |
Storage | Store lyophilized at -20ºC, keep desiccated. |
Datasheet
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