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

GDC-0326
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 206579

CAS#: 1282514-88-8

Description: 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

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 206579
Name: GDC-0326
CAS#: 1282514-88-8
Chemical Formula: C19H22N6O3
Exact Mass: 382.18
Molecular Weight: 382.424
Elemental Analysis: C, 59.67; H, 5.80; N, 21.98; O, 12.55

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 250
25mg	USD 450
50mg	USD 750
100mg	USD 1250
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: GDC-0326; GDC 0326; GDC0326; CAS#1282514-88-8

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/

Solubility Data

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

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:	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.
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.

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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.

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GDC-0326 featured