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
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
N-Bromosuccinimide Price
- 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
- Product number
- CS-6459
- Product name
- GDC-0077
- Purity
- 98.94%
- Packaging
- 5mg
- Price
- $540
- Updated
- 2021/12/16
- Product number
- CS-6459
- Product name
- GDC-0077
- Purity
- 98.94%
- Packaging
- 10mg
- Price
- $900
- Updated
- 2021/12/16
- Product number
- CS-6459
- Product name
- GDC-0077
- Purity
- 98.94%
- Packaging
- 25mg
- Price
- $1260
- Updated
- 2021/12/16
- Product number
- CS-6459
- Product name
- GDC-0077
- Purity
- 98.94%
- Packaging
- 50mg
- Price
- $2020
- Updated
- 2021/12/16
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
GDC-0077 Suppliers
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- 18014399201
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- China
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- China
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- Fax
- +86-21-52996696
- Country
- China
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View Lastest Price from GDC-0077 manufacturers
- 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