GDC-0032 (Synonyms: Taselisib) |
رقم الكتالوجGC17967 |
GDC-0032 (GDC-0032) هو مثبط قوي PI3K يستهدف طفرات PIK3CA ، مع Kis 0.12 نانومتر ، 0.29 نانومتر ، 0.97 نانومتر ، و 9.1 نانومتر لـ PI3Kδ ؛ ، PI3Kα ؛ ، PI3Kγ ؛ و PI3Kβ ، على التوالي.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1282512-48-4
Sample solution is provided at 25 µL, 10mM.
GDC-0032 is a novel and potent benzoxepin inhibitor of PI3Kα isoform with the Ki value of 0.29nM for PI3Kα[1].
GDC-0032 has been reported to potently inhibit PI3Kα and have the selectivity over other PI3Ks with the IC50 values of 0.29nM, 0.91nM and 0.97nM for PI3Kα, PI3Kβ and PI3Kγ, respectively. In addition, GDC-0032 has been revealed to suppress the proliferative cellular activity with the EC50 value of 25nM and 571nM in MCF7 cells and PC3 cells, respectively. The IC50 values of GDC-0032 inhibiting cell activity are 4nM and 31nM in MCF7 cells and PC3 cells, respectively. In vivo, GDC-0032 has shown the inhibition of growth in MCF7-neo/Her2 xenograft model grown in nude mice [1].
References:
[1] Ndubaku CO1, Heffron TP, Staben ST, Baumgardner M, Blaquiere N, Bradley E, Bull R, Do S, Dotson J, Dudley D, Edgar KA, Friedman LS, Goldsmith R, Heald RA, Kolesnikov A, Lee L, Lewis C, Nannini M, Nonomiya J, Pang J, Price S, Prior WW, Salphati L, Sideris S, Wallin JJ, Wang L, Wei B, Sampath D, Olivero AG. Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity. J Med Chem. 2013 Jun 13;56(11):4597-610.
Cell experiment [1]: | |
Cell lines |
MCF7-neo/HER2 cells |
Preparation method |
This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
Reacting condition |
2.5 nM |
Applications |
In MCF7-neo/HER2 cells, GDC-0032 inhibited cell proliferation with an IC50 value of 2.5 nM. |
Animal experiment [1]: | |
Animal models |
MCF7-neo/Her2 xenograft model |
Dosage form |
1.4, 2.8, 5.8, 11.25 or 22.5 mg/kg; p.o.; q.d., for 20 days |
Applications |
GDC-0032 dose-dependently increased TGI and tumor regressions. In addition, GDC-0032 was well-tolerated with less than 10% body weight loss observed when compared with the vehicle group. |
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Ndubaku CO1, Heffron TP, Staben ST, Baumgardner M, Blaquiere N, Bradley E, Bull R, Do S, Dotson J, Dudley D, Edgar KA, Friedman LS, Goldsmith R, Heald RA, Kolesnikov A, Lee L, Lewis C, Nannini M, Nonomiya J, Pang J, Price S, Prior WW, Salphati L, Sideris S, Wallin JJ, Wang L, Wei B, Sampath D, Olivero AG. Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity. J Med Chem. 2013 Jun 13;56(11):4597-610. |
Cas No. | 1282512-48-4 | SDF | |
المرادفات | Taselisib | ||
Chemical Name | 2-methyl-2-[4-[2-(5-methyl-2-propan-2-yl-1,2,4-triazol-3-yl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]pyrazol-1-yl]propanamide | ||
Canonical SMILES | CC1=NN(C(=N1)C2=CN3CCOC4=C(C3=N2)C=CC(=C4)C5=CN(N=C5)C(C)(C)C(=O)N)C(C)C | ||
Formula | C24H28N8O2 | M.Wt | 460.53 |
الذوبان | ≥ 23.05mg/mL in DMSO | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
![]() |
1 mg | 5 mg | 10 mg |
1 mM | 2.1714 mL | 10.8571 mL | 21.7141 mL |
5 mM | 0.4343 mL | 2.1714 mL | 4.3428 mL |
10 mM | 0.2171 mL | 1.0857 mL | 2.1714 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5
(Based on Reviews and 37 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *