GDC-0326 | CAS#1282514-88-8 | PI3Kα Inhibitor

MedKoo Cat#: 206579 | Name: GDC-0326

Description:

WARNING: This product is for research use only, not for human or veterinary use.

GDC-0326 is a potent and selective inhibitor of α-Isoform of Phosphoinositide 3-Kinase (PI3Kalpha inhibitor). GDC-0326 achieves a very high level of selectivity over other kinases. GDC-0326 has low plasma CL in human. Within the PI3 kinase family, there are four class I PI3K isoforms (α, β, δ, and γ). Of these isoforms, PI3Kα is the most commonly associated with cancers.

Chemical Structure

GDC-0326

CAS#1282514-88-8

Theoretical Analysis

MedKoo Cat#: 206579

Name: GDC-0326

CAS#: 1282514-88-8

Chemical Formula: C19H22N6O3

Exact Mass: 382.1753

Molecular Weight: 382.42

Elemental Analysis: C, 59.67; H, 5.80; N, 21.98; O, 12.55

Price and Availability

Size	Price	Availability
10mg	USD 250.00	2 Weeks
25mg	USD 450.00	2 Weeks
50mg	USD 750.00	2 Weeks
100mg	USD 1,250.00	2 Weeks

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Related CAS #

No Data

Synonym

GDC-0326; GDC 0326; GDC0326;

IUPAC/Chemical Name

(S)-2-((2-(1-isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide

InChi Key

SIKYDKLGPWRPMZ-LBPRGKRZSA-N

InChi Code

InChI=1S/C19H22N6O3/c1-11(2)25-19(21-10-22-25)15-9-24-6-7-27-16-8-13(28-12(3)17(20)26)4-5-14(16)18(24)23-15/h4-5,8-12H,6-7H2,1-3H3,(H2,20,26)/t12-/m0/s1

SMILES Code

C[C@H](OC1=CC=C2C3=NC(C4=NC=NN4C(C)C)=CN3CCOC2=C1)C(N)=O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

GDC-0326 is a potent and selective PI3Kα inhibitor with a Ki of 0.2 nM.

In vitro activity:

As shown in Figure 1A, GDC-0326 induced the protein expression of RIPK1 and RIPK3 in both LoVo and HT-29 cells. In addition, colony formation assay demonstrated that GDC-0326 caused a decreased in the clonogenic growth of CRC cells; thus, GDC-0326 attenuated cell proliferation (Figure 1B and C). Additionally, immunofluorescence studies revealed accumulation of RIPK1 and RIPK3 after GDC-0326 treatment of the CRC cells (Figure 1D). These results indicate that the effects of GDC-0326 on the growth and viability of CRC cells involved RIPK1 and RIPK3. Reference: Onco Targets Ther. 2021 Apr 13;14:2519-2530. https://pubmed.ncbi.nlm.nih.gov/33880032/

In vivo activity:

Treatment with GDC-0326 abolished AKT phosphorylation in βTC3 cells (Fig. 3B) and in RIP1-Tag2 tumors (Fig. 5A). Reference: Clin Cancer Res. 2016 Dec 1;22(23):5805-5817. https://pubmed.ncbi.nlm.nih.gov/27225693/

	Solvent	mg/mL	mM
Solubility
	DMF	30.0	78.45
	DMSO	68.7	179.56
	Ethanol	19.0	49.68

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 382.42 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Zhang Z, Ju F, Chen F, Wu H, Chen J, Zhong J, Shao L, Zheng S, Wang L, Xue M. GDC-0326 Enhances the Effects of 5-Fu in Colorectal Cancer Cells by Inducing Necroptotic Death. Onco Targets Ther. 2021 Apr 13;14:2519-2530. doi: 10.2147/OTT.S302334. PMID: 33880032; PMCID: PMC8053532. 2. Soler A, Figueiredo AM, Castel P, Martin L, Monelli E, Angulo-Urarte A, Milà-Guasch M, Viñals F, Baselga J, Casanovas O, Graupera M. Therapeutic Benefit of Selective Inhibition of p110α PI3-Kinase in Pancreatic Neuroendocrine Tumors. Clin Cancer Res. 2016 Dec 1;22(23):5805-5817. doi: 10.1158/1078-0432.CCR-15-3051. Epub 2016 May 25. PMID: 27225693; PMCID: PMC5338478.

In vitro protocol:

In vivo protocol:

1. Soler A, Figueiredo AM, Castel P, Martin L, Monelli E, Angulo-Urarte A, Milà-Guasch M, Viñals F, Baselga J, Casanovas O, Graupera M. Therapeutic Benefit of Selective Inhibition of p110α PI3-Kinase in Pancreatic Neuroendocrine Tumors. Clin Cancer Res. 2016 Dec 1;22(23):5805-5817. doi: 10.1158/1078-0432.CCR-15-3051. Epub 2016 May 25. PMID: 27225693; PMCID: PMC5338478.

1: Heffron TP, Heald RA, Ndubaku C, Wei B, Augistin M, Do S, Edgar K, Eigenbrot C, Friedman L, Gancia E, Jackson PS, Jones G, Kolesnikov A, Lee LB, Lesnick JD, Lewis C, McLean N, Mörtl M, Nonomiya J, Pang J, Price S, Prior WW, Salphati L, Sideris S, Staben ST, Steinbacher S, Tsui V, Wallin J, Sampath D, Olivero AG. The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1 ,4]oxazepin-9-yl)oxy)propanamide (GDC-0326). J Med Chem. 2016 Jan 20. [Epub ahead of print] PubMed PMID: 26741947.