Taselisib (Synonyms: GDC-0032; RG-7604)

Cat. No.: HY-13898 Purity: 99.86%: FAQs
Data Sheet SDS COA Handling Instructions

Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with K_is of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.

For research use only. We do not sell to patients.

Taselisib Chemical Structure

CAS No. : 1282512-48-4

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solution
10 mM * 1 mL in DMSO	USD 78	In-stock	Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL ready for reconstitution	USD 78	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 77	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 121	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 275	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 495	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 825	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 17 publication(s) in Google Scholar

15 Publications Citing Use of MCE Taselisib

: Taselisib purchased from MCE. Usage Cited in: Cell Discov. 2016 Sep 20;2:16030. [Abstract]; Effects of combined inhibition of PI3K and STAT3 pathways on PTEN-mutated T-ALL cells. (a) Short-term treatment of Ba/F3-shPTEN-NTRK2-Tel cells with isoform-selective inhibitors and Pan-PI3K inhibitor GDC-0032. Cells are treated with DMSO, BYL719, KIN193, GS-1101, GDC-0032 (1 μM) or JAK–STAT inhibitor AZD-1480 (1 μM) for 3 h (n=3) for each treatment. (b) Immunoblot analysis of P-Akt and p-S6 in PF382 and JURKAT cells. Cells are treated with the same inhibitors as in a. (c) Combination of siNTRK2

: Taselisib purchased from MCE. Usage Cited in: Br J Cancer. 2016 Jul 26;115(3):303-11. [Abstract]; Effect of the combination of CYC065 and Taselisib in vitro. (A) Uterine serous carcinoma-ARK-1 and USC-ARK-2 are treated with the half-maximal inhibitory concentration (IC₅₀) of CYC065, the IC₅₀ of Taselisib (GDC0032) or the combination of the IC₅₀s of the two compounds for 72 h. Cell counting is then carried. The incubation of USC-ARK-1 and USC-ARK-2 cells with the combination of CYC065 and Taselisib is significantly more effective in inhibiting cells’ growth th

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with K_is of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.

IC₅₀ & Target^[3]

PI3Kδ

0.12 nM (Ki)

PI3Kα

0.29 nM (Ki)

PI3Kγ

0.97 nM (Ki)

PI3Kβ

9.1 nM (Ki)

In Vitro

Taselisib (GDC-0032) (100 nM) inhibits AKT/mTOR signaling in PIK3CA mutant cell lines but not in cells with loss or mutation of PTEN; Taselisib (GDC-0032) enhances radiation-induced apoptosis and inhibits growth in head and neck cancer cell lines that are sensitive to its single-agent activiy^[1]. Taselisib (GDC-0032) enhances the effects of MEK1/2 inhibition on both BRAF^V600E/PTEN^Null human melanoma cells autochthonous mouse melanomas^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Taselisib (GDC-0032) (5 mg/kg, p.o.) potently impairs PI3K signaling and enhances the efficacy of fractionated radiotherapy; Taselisib (GDC-0032) and radiation is more effective than either treatment alone in nude mice implanted with subcutaneous Cal-33 xenografts^[1]. The vehicle-treated BRAFV600E/PTENNull melanoma-bearing mice experiencs initial tumor regression after treatment with Taselisib (GDC-0032) (22.5 mg/kg, p.o.)^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

460.53

Appearance

Solid

Formula

C₂₄H₂₈N₈O₂

CAS No.

1282512-48-4

SMILES

CC(C)N1C(C2=CN3C(C(C(OCC3)=C4)=CC=C4C5=CN(C(C)(C(N)=O)C)N=C5)=N2)=NC(C)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (54.29 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	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

*Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

*All of the co-solvents are available by MCE.

Purity & Documentation

Purity: 99.86%

Select Batch:

Data Sheet (284 KB) SDS (252 KB)

COA (257 KB) LCMS (106 KB)

Handling Instructions (2659 KB)

References

[1]. Zachary S. Zumsteg, et al. Taselisib (GDC-0032), a Potent β-Sparing Small Molecule Inhibitor of PI3K, Radiosensitizes Head and Neck Squamous Carcinomas Containing Activating PIK3CA Alterations. Clin Cancer Res. 2016 Apr 15; 22(8): 2009–2019. [Content Brief]

[2]. Marian M. Deuker, et al. PI3′-Kinase Inhibition Forestalls the Onset of MEK1/2 Inhibitor Resistance in BRAF-Mutated Melanoma. Cancer Discov. 2015 Feb; 5(2): 143–153. [Content Brief]

[3]. Ndubaku CO, et al. 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. [Content Brief]

Cell Assay ^[1]	Cells are seeded in replicates of 6 in 96-well plates with 500 to 5,000 cells/well overnight and then treated with Taselisib (GDC-0032). After 4 days, the media are removed and the cells are fixed with 4% glutaraldehyde for 30 minutes. Fixed cells are stained with 0.1% crystal violet for 2 minutes, then washed, and dissolved in 10% acetic acid. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Six-week-old Nu/Nu mice are injected bilaterally with 5×10⁵ cells resuspended in 200 μL of culture media and Matrigel mixed in a 1:1 ratio. After tumors reache approximately 100 to 200 cm³, mice are randomized into treatment arms with 8 to 10 tumors per group. Taselisib (GDC-0032) (5 mg/kg) is dissolved in a vehicle containing 0.5% methylcellulose with 0.2% TWEEN-80 and is administered via daily oral gavage. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Zachary S. Zumsteg, et al. Taselisib (GDC-0032), a Potent β-Sparing Small Molecule Inhibitor of PI3K, Radiosensitizes Head and Neck Squamous Carcinomas Containing Activating PIK3CA Alterations. Clin Cancer Res. 2016 Apr 15; 22(8): 2009–2019. [Content Brief] [2]. Marian M. Deuker, et al. PI3′-Kinase Inhibition Forestalls the Onset of MEK1/2 Inhibitor Resistance in BRAF-Mutated Melanoma. Cancer Discov. 2015 Feb; 5(2): 143–153. [Content Brief] [3]. Ndubaku CO, et al. 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. [Content Brief]

Taselisib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Taselisib1282512-48-4GDC-0032 RG-7604GDC0032GDC 0032RG7604RG 7604RG-7604PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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Taselisib (Synonyms: GDC-0032; RG-7604)

Customer Review

Taselisib Related Antibodies

15 Publications Citing Use of MCE Taselisib

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•Related Screening Libraries:

•Related Small Molecules:

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View All PI3K Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Taselisib Related Antibodies

Taselisib Related Classifications

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Dilution Calculator

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The dilution calculator equation

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