ChemicalBook > CAS DataBase List > GDC-0941 Bimesylate

GDC-0941 Bimesylate

Description In vitro In vivo

Product Name: GDC-0941 Bimesylate
CAS No.: 957054-33-0
Chemical Name: GDC-0941 Bimesylate
Synonyms: GDC-0941 Bimesylate;Pictilisib mesylate;GDC-0941 dimesylate;Pictilisib (GDC-0941);GDC-0941 (2 MeSO3H salt);GDC 0941 (2 MeSO3H salt);GDC-0941 (diMethanesulfonate);Pictilisib dimethanesulfonate;GDC-0941 Bimesylate USP/EP/BP;GDC-0941 BiMesylate/pictilisib
CBNumber: CB82509226
Molecular Formula: C24H30N7O6S3
Formula Weight: 608.7333
MOL File: 957054-33-0.mol

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GDC-0941 Bimesylate Property

Melting point:: >280°C (dec.)
storage temp.: Refrigerator
solubility: DMSO (Slightly, Heated), Methanol (Sparingly)
form: Solid
color: White to Pale Yellow

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Usbiological

Product number: 012740
Product name: GDC-0941 Bimesylate
Packaging: 10mg
Price: $460
Updated: 2021/12/16

TRC

Product number: G300000
Product name: GDC-0941Bimesylate
Packaging: 50mg
Price: $790
Updated: 2021/12/16

ApexBio Technology

Product number: A3432
Product name: GDC-0941dimethanesulfonate
Packaging: 10mg
Price: $50
Updated: 2021/12/16

ChemScene

Product number: CS-0082
Product name: Pictilisib(dimethanesulfonate)
Purity: 99.31%
Packaging: 10mg
Price: $60
Updated: 2021/12/16

ChemScene

Product number: CS-0082
Product name: Pictilisib(dimethanesulfonate)
Purity: 99.31%
Packaging: 50mg
Price: $90
Updated: 2021/12/16

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GDC-0941 Bimesylate Chemical Properties,Usage,Production

Description

Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Phase 2.

In vitro

GDC-0941 is equipotent against PI3Kα and PI3Kδ as well as PI3Kα mutants E545-K and H1047-R, displaying modest levels of selectivity against PI3Kβ (10-fold) and PI3Kγ (25-fold), and greater levels of selectivity against members of PI3K class II, III, and IV, including C2β, Vps34, DNA-PK, and mTOR. GDC-0941 potently inhibits the phosphorylation of Akt in U87MG, PC3, and MDA-MB-361 cells with IC50 of 46 nM, 37 nM, and 28 nM, respectively. GDC-0941 inhibits the proliferation of U87MG, A2780, PC3, and MDA-MB-361 cells with IC50 of 0.95 μM, 0.14 μM, 0.28 μM, and 0.72 μM, respectively. GDC-0941 treatment potently inhibits the proliferation of both trastuzumab-sensitive and-insensitive HER2-amplified cells with IC50 of 149-944 nM. GDC-0941 inhibits proliferation of HER2-amplified cells that harbor PIK3CA mutations with IC50 of <500 nM, and effectively inhibits both proliferation and viability of HER2-amplified breast cancer cells that are resistant to trastuzumab due to PTEN loss. GDC-0941 significantly inhibits the growth of HCT116, DLD1 and HT29 cells with GI50 of 1081 nM, 1070 nM and 157 nM, respectively. GDC-0941 inhibits tumor cell proliferation, induces apoptosis and suppresses centroblast population.

In vivo

Administration of GDC-0941 at 75 mg/kg/day displays significant inhibitory effect against established human U87MG glioblastoma xenografts in female NCr athymic mice, with tumor growth inhibition of 83%. Oral administration of GDC-0941 at 150 mg/kg/day inhibits the growth of HER2-amplified, trastuzumab-resistant MDA-MB-361.1 xenografts in mice, and significantly delays the tumor progression, in association with potent induced apoptosis in tumors. GDC-0941 (75 mg/kg/day) treatment for 2 weeks induces ~40% reduction in tumor volume of spontaneous B-cell follicular lymphomas developed in PTEN+/-LKB1+/hypo mice, accompanied by ablation of phosphorylation of Akt, S6K and SGK (serum and glucocorticoid protein kinase) protein kinases.

Chemical Properties

Off-White Solid

Uses

Potent inhibitor of Phosphatidylinositol 3-kinase (PI3K)

Biological Activity

gdc-0941 is a novel selective class i phosphatidylinositol-3-kinase (pi3k) inhibitor. activation of pi3k/akt signaling pathway is frequently associated with tumorigenesis. deregulation of this pathway occurs frequently with a variety of cancers and may contribute to the resistance to many anticancer agents. [1] developing novel small molecules that specifically block the pi3k/akt pathway may inhibit tumor growth. gdc-0941 is designed to bind the atp-binding pocket of pi3k and to prevent formation of phosphatidylinositol-3, 4, 5-triphosphate (pip3), a second messenger that transmits pi3k downstream signals. [2, 3] it binds to pi3k in an atp-competitive manner.gdc-0941 is a potent small-molecule thieno [3, 2-d] pyrimidine inhibitor of the class i pi3k. it is highly selective against isoforms p110( and p110( with ic50 of 3 nm, and moderately selective against isoforms p110( and p110( with ic50s of 33 nm and 75 nm, respectively.gdc-0941 inhibits cell proliferation in vitro and in vivo. it causes growth inhibition in a variety of cancer cell lines, including a2780, mda-mb-361, pc3, and u87mg. [2] it also inhibits the growth of trastuzumab–sensitive and –resistant her2-amplied cancer cells which harbor p110( mutations or pten loss. [4] gdc-0941 also reduces tumor volume in different xenograft models. [4]gdc-0941 can be taken orally.

in vivo

Pictilisib (GDC-0941) (150 mg/kg, p.o.) leads to tumor stasis in MCF7-neo/HER2-bearing animals model. Pictilisib (GDC-0941) and RP-56976 result in tumor regressions during the treatment period leading to enhanced antitumor responses^[1]. Tumours in the Pictilisib (GDC-0941)-treated mice show a marked non-linear shrinkage, and when the Pictilisib (GDC-0941) treatment ceased, the tumours in the test cohort mice grow again^[2]. GDC-0941Pictilisib (GDC-0941) (25 or 50 mg/kg) reduces tumor growth and PI3K and HIF-1 pathway activity in eGFP-FTC133 tumor-bearing mice^[4].

target

PI3Kα

IC 50

p110α: 3 nM (IC₅₀); p110α-H1047R: 3 nM (IC₅₀); p110α-E545K: 3 nM (IC₅₀); p110δ: 3 nM (IC₅₀); p110β: 33 nM (IC₅₀); p110γ: 75 nM (IC₅₀); mTOR: 0.58 μM (Ki); DNA-PK: 1.23 μM (IC₅₀); Autophagy

References

[1]yuan tl, cantley lc. pi3k pathway alterations in cancer: variations on a theme. oncogene. 2008;27:5497-5510.
[2]folkes aj, ahmadi k, alderton wk, et al. the identification of 2-(1h-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (gdc-0941) as a potent, selective, orally bioavailable inhibitor of class i pi3 kinase for the treatment of cancer. j med chem. 2008; 51: 5522-5532.
[3]knight za, shokat km. chemically targeting the pi3k family. biochem soc trans. 2007; 35: 245-249.
[4]junttila tt, akita rw, parsons k, fields c, lewis phillips gd, friedman ls, sampath d, sliwkowski mx. ligand-independent her2/her3/pi3k complex is disrupted by trastuzumab and is effectively inhibited by the pi3k inhibitor gdc-0941. br j cancer. 2011; 104(7): 1116-25.

GDC-0941 Bimesylate Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from GDC-0941 Bimesylate manufacturers

Career Henan Chemical Co

Product: Pictilisib dimethanesulfonate 957054-33-0
Price: US $9.80/KG
Min. Order: 1KG
Purity: ≥98%
Supply Ability: 20 tons
Release date: 2020-01-02

Career Henan Chemical Co

Product: Pictilisib dimethanesulfonate 957054-33-0
Price: US $9.80/KG
Min. Order: 1KG
Purity: ≥98%
Supply Ability: 20 tons
Release date: 2019-12-31

957054-33-0, GDC-0941 BimesylateRelated Search:

GDC 0941 bismesylate - Pictilisib

Pictilisib dimethanesulfonate

PICTILISIB DIMETHANESULFONATE;GDC-0941 (2 MESO3H SALT);GDC0941 DIMETHANESULFONATE;GDC-0941;GDC0941;GDC 0941

GDC-0941 Bimesylate

GDC-0941 (diMethanesulfonate)

GDC 0941 (2 MeSO3H salt)

GDC-0941 (2 MeSO3H salt)

GDC-0941 BiMesylate/pictilisib

2-(1H-Indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)thieno[3,2-d]pyrimidine methanesulfonate (1:2)

Pictilisib (GDC-0941)

GDC-0941 bimesylate salt, Pictilisib dimethanesulfonate

Pictilisib (GDC-0941) dimethanesulfonate

PICTILISIB DIMETHANESULFONATE;GDC-0941 (2 MESO3H SALT);GDC-0941

Pictilisib mesylate

Thieno[3,2-d]pyrimidine,2-(1H-indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)-,methanesulfonate(1:2)

GDC-0941 Bimesylate USP/EP/BP

Pictilisib (GDC-0941) mesylate

GDC 0941,inhibit,Inhibitor,GDC-0941 2 MeSO3H,Pictilisib,GDC0941,PI3K,Phosphoinositide 3-kinase,GDC-0941,Apoptosis,Pictilisib dimethanesulfonate,Autophagy

GDC-0941 dimesylate

4-(2-(1H-indazol-4-yl)-6-((4-(methylsulfonyl)-piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)-morpholine bis-methanesulfonate

Pictilisib dimethanesulfonate, 10 mM in DMSO

2-(1H-Indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)thieno[3,2-d]pyrimidine methanesulfona

GDC-0941 dimethanesulfonate (Pictilisib dimethanesulfonate)

957054-33-0

C23H27N7O3S22CH4O3S

C25H35N7O9S4

CH4O3SC23H27N7O3S2

Intermediates & Fine Chemicals

Pharmaceuticals

Protein Kinase Inhibitors and Activators