Inavolisib | GDC-0077 | CAS#2060571-02-8 | PI3K inhibitor

MedKoo Cat#: 206818 | Name: GDC-0077

Description:

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

Inavolisib, also known as GDC-0077, is a potent and selective PI3K inhibitor. GDC-0077 blocks an enzyme involved in cancer growth called PI3K. GDC0077 binds to and inhibits various members of the PI3K family, including activating mutations in the catalytic alpha isoform PIK3CA. PI3K inhibition prevents the activation of the PI3K-mediated signaling pathway and results in the inhibition of growth and survival of PI3K-overexpressing tumor cells.

Chemical Structure

GDC-0077

CAS#2060571-02-8

Theoretical Analysis

MedKoo Cat#: 206818

Name: GDC-0077

CAS#: 2060571-02-8

Chemical Formula: C18H19F2N5O4

Exact Mass: 407.1405

Molecular Weight: 407.38

Elemental Analysis: C, 53.07; H, 4.70; F, 9.33; N, 17.19; O, 15.71

Price and Availability

Size	Price	Availability
1mg	USD 90.00	Ready to ship
5mg	USD 250.00	Ready to ship
10mg	USD 450.00	Ready to ship
25mg	USD 750.00	Ready to ship
50mg	USD 1,250.00	Ready to ship
100mg	USD 2,150.00	Ready to ship

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Related CAS #

No Data

Synonym

Inavolisib; GDC-0077; GDC 0077; GDC0077; RG6114; RG 6114; RG-6114

IUPAC/Chemical Name

(S)-2-((2-((S)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide

InChi Key

SGEUNORSOZVTOL-CABZTGNLSA-N

InChi Code

InChI=1S/C18H19F2N5O4/c1-9(16(21)26)22-10-2-3-11-13(6-10)28-5-4-24-7-14(23-17(11)24)25-12(15(19)20)8-29-18(25)27/h2-3,6-7,9,12,15,22H,4-5,8H2,1H3,(H2,21,26)/t9-,12-/m0/s1

SMILES Code

C[C@@H](C(N)=O)NC1=CC=C(C2=NC(N3[C@H](C(F)F)COC3=O)=CN2CCO4)C4=C1

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

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

Certificate of Analysis

View CoA: current batch, Lot# T22D12P28

QC Data

View QC data: current batch, Lot#T22D12P28

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

PI3Kα

In vitro activity:

TBD

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMSO	110.0	245.47

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 407.38 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:

TBD

In vitro protocol:

TBD

In vivo protocol:

TBD

1: Hanan EJ, Braun MG, Heald RA, MacLeod C, Chan C, Clausen S, Edgar KA, Eigenbrot C, Elliott R, Endres N, Friedman LS, Gogol E, Gu XH, Thibodeau RH, Jackson PS, Kiefer JR, Knight JD, Nannini M, Narukulla R, Pace A, Pang J, Purkey HE, Salphati L, Sampath D, Schmidt S, Sideris S, Song K, Sujatha-Bhaskar S, Ultsch M, Wallweber H, Xin J, Yeap S, Young A, Zhong Y, Staben ST. Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα. J Med Chem. 2022 Dec 22;65(24):16589-16621. doi: 10.1021/acs.jmedchem.2c01422. Epub 2022 Dec 1. PMID: 36455032. 2: Song KW, Edgar KA, Hanan EJ, Hafner M, Oeh J, Merchant M, Sampath D, Nannini MA, Hong R, Phu L, Forrest WF, Stawiski E, Schmidt S, Endres N, Guan J, Wallin JJ, Cheong J, Plise EG, Lewis Phillips GD, Salphati L, Heffron TP, Olivero AG, Malek S, Staben ST, Kirkpatrick DS, Dey A, Friedman LS. RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy. Cancer Discov. 2022 Jan;12(1):204-219. doi: 10.1158/2159-8290.CD-21-0072. Epub 2021 Sep 20. PMID: 34544753; PMCID: PMC9762331. 3: Turner NC, Im SA, Saura C, Juric D, Loibl S, Kalinsky K, Schmid P, Loi S, Sunpaweravong P, Musolino A, Li H, Zhang Q, Nowecki Z, Leung R, Thanopoulou E, Shankar N, Lei G, Stout TJ, Hutchinson KE, Schutzman JL, Song C, Jhaveri KL. Inavolisib-Based Therapy in PIK3CA-Mutated Advanced Breast Cancer. N Engl J Med. 2024 Oct 31;391(17):1584-1596. doi: 10.1056/NEJMoa2404625. PMID: 39476340. 4: Inavolisib. Am J Health Syst Pharm. 2025 Feb 20;82(5):e213-e215. doi: 10.1093/ajhp/zxae364. PMID: 39719029. 5: Blair HA. Inavolisib: First Approval. Drugs. 2025 Feb;85(2):271-278. doi: 10.1007/s40265-024-02136-y. Epub 2025 Jan 28. PMID: 39873916. 6: Gough SM, Flanagan JJ, Teh J, Andreoli M, Rousseau E, Pannone M, Bookbinder M, Willard R, Davenport K, Bortolon E, Cadelina G, Gordon D, Pizzano J, Macaluso J, Soto L, Corradi J, Digianantonio K, Drulyte I, Morgan A, Quinn C, Békés M, Ferraro C, Chen X, Wang G, Dong H, Wang J, Langley DR, Houston J, Gedrich R, Taylor IC. Oral Estrogen Receptor PROTAC Vepdegestrant (ARV-471) Is Highly Efficacious as Monotherapy and in Combination with CDK4/6 or PI3K/mTOR Pathway Inhibitors in Preclinical ER+ Breast Cancer Models. Clin Cancer Res. 2024 Aug 15;30(16):3549-3563. doi: 10.1158/1078-0432.CCR-23-3465. PMID: 38819400; PMCID: PMC11325148. 7: Kargbo RB. Effective Combination Therapies for the Treatment of HER2 Cancer. ACS Med Chem Lett. 2023 Feb 7;14(3):231-232. doi: 10.1021/acsmedchemlett.2c00544. PMID: 36923923; PMCID: PMC10009784. 8: Jhaveri KL, Accordino MK, Bedard PL, Cervantes A, Gambardella V, Hamilton E, Italiano A, Kalinsky K, Krop IE, Oliveira M, Schmid P, Saura C, Turner NC, Varga A, Cheeti S, Hilz S, Hutchinson KE, Jin Y, Royer-Joo S, Peters U, Shankar N, Schutzman JL, Juric D. Phase I/Ib Trial of Inavolisib Plus Palbociclib and Endocrine Therapy for PIK3CA-Mutated, Hormone Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Advanced or Metastatic Breast Cancer. J Clin Oncol. 2024 Nov 20;42(33):3947-3956. doi: 10.1200/JCO.24.00110. Epub 2024 Sep 5. PMID: 39236276; PMCID: PMC11575912. 9: Salphati L, Pang J, Plise EG, Cheong J, Braun MG, Friedman LS, Hong Thibodeau R, Jaochico A, Johnson R, Liu N, Nannini M, Sampath D, Song K, Hannan EJ, Staben ST. Preclinical assessment of the PI3Kα selective inhibitor inavolisib and prediction of its pharmacokinetics and efficacious dose in human. Xenobiotica. 2024 Oct;54(10):808-820. doi: 10.1080/00498254.2024.2415103. Epub 2024 Dec 4. PMID: 39387185. 10: Vanhaesebroeck B, Burke JE, Madsen RR. Precision Targeting of Mutant PI3Kα in Cancer by Selective Degradation. Cancer Discov. 2022 Jan;12(1):20-22. doi: 10.1158/2159-8290.CD-21-1411. PMID: 35022207; PMCID: PMC7612218.