ChemicalBook > CAS DataBase List > GDC-0077

GDC-0077

Product Name
GDC-0077
CAS No.
2060571-02-8
Chemical Name
GDC-0077
Synonyms
RG 6114;CPD1573;GDC-0077;RO 7113755;Inavolisib;GDC-0077 (RG6114);GDC-0077 Inavolisib;Inavolisib (GDC-0077);Inavolisib, 10 mM in DMSO;GDC-0077; RG 6114; RO 7113755
CBNumber
CB43175543
Molecular Formula
C18H19F2N5O4
Formula Weight
407.37
MOL File
2060571-02-8.mol
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GDC-0077 Property

Boiling point:
698.0±65.0 °C(Predicted)
Density 
1.63±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:110.0(Max Conc. mg/mL);245.47(Max Conc. mM)
pka
15.89±0.50(Predicted)
form 
Solid
color 
Off-white to yellow
InChIKey
SGEUNORSOZVTOL-CABZTGNLSA-N
SMILES
C(N)(=O)[C@@H](NC1C=C2OCCN3C=C(N4[C@H](C(F)F)COC4=O)N=C3C2=CC=1)C
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

American Custom Chemicals Corporation
Product number
PRK0000448
Product 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
Purity
95.00%
Packaging
5MG
Price
$451.72
Updated
2021/12/16
ChemScene
Product number
CS-6459
Product name
GDC-0077
Purity
98.94%
Packaging
5mg
Price
$540
Updated
2021/12/16
ChemScene
Product number
CS-6459
Product name
GDC-0077
Purity
98.94%
Packaging
10mg
Price
$900
Updated
2021/12/16
ChemScene
Product number
CS-6459
Product name
GDC-0077
Purity
98.94%
Packaging
25mg
Price
$1260
Updated
2021/12/16
ChemScene
Product number
CS-6459
Product name
GDC-0077
Purity
98.94%
Packaging
50mg
Price
$2020
Updated
2021/12/16
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GDC-0077 Chemical Properties,Usage,Production

Description

Inavolisib, or 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 inhibits the growth and survival of PI3K-overexpressing tumor cells. The IUPAC name of this compound is (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.

Uses

Inavolisib (GDC-0077) is a potent, orally active, and selective PI3Kα inhibitor (IC50=0.038 nM). Inavolisib exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. Inavolisib is more selective for mutant versus wild-type PI3Kα. Inavolisib can be used for the study of breast cancer[1].

in vitro

GDC-0077 (RG6114) is >300-fold more selective for PI3Kα over the other class I PI3K isoforms (β, δ, and γ) and >2000-fold more selective over PIK family members. GDC-0077 selectively degrades mutant PI3Kα in a proteasome-dependent fashion, resulting in a reduction of PI3K pathway activity biomarkers such as pAKT and pPRAS40, inhibition of cell proliferation, and increased apoptosis in human PIK3CA-mutant breast cancer cell lines to a greater extent when compared to PIK3CA wild-type cells.

in vivo

Inavolisib (p.o.) results in tumor regressions, induction of apoptosis, and a reduction of pAKT, pPRAS40, and pS6RP in a dose-dependent fashion in PIK3CA-mutant breast cancer xenograft models[1].

IC 50

PI3Kα: 0.038 nM (IC50)

References

[1] R Hong, Abstract PD4-14: GDC-0077 is a selective PI3Kalpha inhibitor that demonstrates robust efficacy in PIK3CA mutant breast cancer models as a single agent and in combination with standard of care therapies. 2017 San Antonio Breast Cancer Symposium.

GDC-0077 Preparation Products And Raw materials

Raw materials

Preparation Products

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GDC-0077 Suppliers

Shanghai Tachizaki Biomedical Research Center
Tel
18014399201
Email
sales@chemlab-tachizaki.com
Country
China
ProdList
2742
Advantage
58
Nantong Hanfang Biotechnology Co. , Ltd.
Tel
hanfangpharma@126.com; 18616537568
Email
hanfangpharma@126.com
Country
China
ProdList
29965
Advantage
58
Shandong Dongde New Materials Co., Ltd
Tel
13290191024
Email
3887351301@qq.com
Country
China
ProdList
1910
Advantage
58
yimo organism
Tel
15915870272; 15915870272
Email
yimo_bio@163.com
Country
China
ProdList
446
Advantage
58
Jurong Coupling Biotechnology Co., Ltd.
Tel
19231718652
Email
278191416@qq.com
Country
China
ProdList
482
Advantage
58
Wuhan Jingkangen Biomedical Technology Co., Ltd
Tel
13720134139 086-15871494362 13720134139
Email
orders@jknbiochem.com
Country
China
ProdList
6614
Advantage
58
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
15883
Advantage
64
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3506
Advantage
58
Sichuan Wei Keqi Biological Technology Co., Ltd.
Tel
028-81700200 18116577057
Fax
028-81705658
Email
3003855609@qq.com
Country
China
ProdList
7778
Advantage
56
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4757
Advantage
55
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View Lastest Price from GDC-0077 manufacturers

Hubei Chuchang Biotech Co., Ltd.
Product
Inavolisib (Synonyms: GDC-0077; RG6114) 2060571-02-8
Price
US $0.00-0.00/mg
Min. Order
5mg
Purity
98%+ HPLC HNMR
Supply Ability
20g
Release date
2024-03-29

2060571-02-8, GDC-0077Related Search:


  • GDC-0077
  • CPD1573
  • RG 6114
  • RO 7113755
  • GDC-0077; RG 6114; RO 7113755
  • (2S)-2-[[2-[(4S)-4-(difluoromethyl)-2-oxo-1,3-oxazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]amino]propanamide
  • Propanamide, 2-[[2-[(4S)-4-(difluoromethyl)-2-oxo-3-oxazolidinyl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]amino]-, (2S)-
  • Inavolisib
  • Inavolisib (GDC-0077)
  • GDC-0077 Inavolisib
  • Apoptosis,RG 6114,RG-6114,Phosphoinositide 3-kinase,Inhibitor,PI3K,Inavolisib,GDC 0077,GDC0077,inhibit
  • (S)-2-[[2-[(S)-4-(Difluoromethyl)-2-oxo-3-oxazolidinyl]-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]amino]propanamide
  • Inavolisib (Synonyms: GDC-0077
  • (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
  • Inavolisib (RG-6114, RO-7113755)
  • (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 , Inavolisib
  • Inavolisib, 10 mM in DMSO
  • (2S)-2-({4-[(4S)-4-(difluoromethyl)-2-oxo-1,3-oxazolidin-3-yl]-9-oxa-3,6-diazatricyclo[8.4.0.02,?]tetradeca-1(14),2,4,10,12-pentaen-12-yl}amino)propanamide
  • Inavolisib (GDC-0077, RG6114)
  • GDC-0077 (RG6114)
  • (2S)-2-({4-[(4S)-4-(difluoromethyl)-2-oxo-1, 3-oxazolidin-3-yl]-9-oxa-3,6-diazatricyclo[8.4.0.02,]tetradeca-1(14),2,4,10,12-pentaen-12-yl}am
  • 2060571-02-8
  • GDC-0077