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Pictilisib

Product Name
Pictilisib
CAS No.
957054-30-7
Chemical Name
Pictilisib
Synonyms
CS-23;RG7321;GDC-01;GNE0941;GDC-0941;GNE 0941;GNE-0941;Pictilisib;pictrelisib;GDC-0941 Base
CBNumber
CB41872141
Molecular Formula
C23H27N7O3S2
Formula Weight
513.64
MOL File
957054-30-7.mol
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Pictilisib Property

Melting point:
>200oC (dec.)
Density 
1.53±0.1 g/cm3(Predicted)
storage temp. 
-20°C
solubility 
Soluble in DMSO (>25 mg/ml)
form 
White powder solid.
pka
12.22±0.40(Predicted)
color 
White/off-white
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
InChIKey
LHNIIDJUOCFXAP-UHFFFAOYSA-N
SMILES
C1(C2=CC=CC3=C2C=NN3)=NC(N2CCOCC2)=C2SC(CN3CCN(S(C)(=O)=O)CC3)=CC2=N1
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Safety

HS Code 
29350090
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
5.09226
Product name
PI 3-K Inhibitor XXI, GDC-0941
Packaging
10 mg
Price
$226
Updated
2025/07/31
Cayman Chemical
Product number
11600
Product name
GDC-0941
Purity
≥98%
Packaging
10mg
Price
$134
Updated
2024/03/01
Cayman Chemical
Product number
11600
Product name
GDC-0941
Purity
≥98%
Packaging
50mg
Price
$333
Updated
2024/03/01
Cayman Chemical
Product number
11600
Product name
GDC-0941
Purity
≥98%
Packaging
100mg
Price
$531
Updated
2024/03/01
Biorbyt Ltd
Product number
orb61040
Product name
GDC-0941, Free Base
Purity
>99% pure
Packaging
50mg
Price
$343.4
Updated
2021/12/16
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Pictilisib Chemical Properties,Usage,Production

Description

GDC-0941/Pictilisib (957054-30-7) is a potent and selective inhibitor of class I phosphatidylinositol-3-kinases (PI3K) with significant antitumor activity – IC50’s: PI3Kα = 3nM, PI3Kβ = 33 nM, PI3Kδ = 3 nM, PI3Kγ = 75 nM.1,2?? GDC-0941 is the chemical probe of choice for the pan-inhibition of class I PI3K’s.3?Currently in clinical trials.4

Uses

GDC-0941 is a potent and selective oral inhibitor of the class I PI3K. GDC-0941 demonstrated broad spectrum of activity in breast, ovarian, lung, and prostate cancer models. Studies has also shown GDC-0941 may enhance anti-tumor activity of Docetaxel (D494420) in human breast cancer models. Potent PI3K inhibitor.

Definition

ChEBI: A sulfonamide composed of indazole, morpholine, and methylsulfonyl-substituted piperazine rings bound to a thienopyrimidine ring.

Synthesis

885618-33-7

885675-66-1

957054-30-7

Step 1: 4-(2-chloro-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)morpholine (Compound 0113, 800 mg, 1.86 mmol), pinacol ester of 1H-indazole-4-boronic acid (0107-3, 500 mg, 2.04 mmol), sodium bicarbonate (470 mg. 5.58 mmol), sodium bicarbonate (470 mg, 5.58 mmol), and bis(triphenylphosphine)palladium(II) chloride (80 mg, 0.093 mmol) were dissolved in a solvent mixture of toluene (20 mL), ethanol (12 mL), and water (5.6 mL). The reaction system was replaced by nitrogen and then heated at 120 °C for 1 h under microwave radiation. After completion of the reaction, the reaction mixture was partitioned between dichloromethane and water. The organic layer was separated, washed with brine, dried over anhydrous magnesium sulfate, filtered and concentrated. The resulting crude product was purified by silica gel column chromatography (eluent: dichloromethane containing 2% methanol, v/v) to afford 2-(1H-indazol-4-yl)-6-(4-methanesulfonylpiperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (Compound 0114, 350 mg, 37% yield) as a white solid with a melting point of 148-149 °C. LC -MS: m/z 514 [M+H]+; 1H NMR (400 MHz, CDCl3): δ 2.70 (t, J = 4.4 Hz, 4H), 2.81 (s, 3H), 3.13 (t, J = 4.4 Hz, 4H), 3.92 (m, 6H), 4.09 (t, J = 5.6 Hz, 4H), 7.41 (s, 1H), 7.50 (m, 1H), 7.59 (d, J = 8.4 Hz, 1H), 8.28 (d, J = 6.8 Hz, 1H), 9.00 (s, 1H), 10.32 (br s, 1H).

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]. Pictilisib (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] ADRIAN J. FOLKES*. 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]. Journal of Medicinal Chemistry, 2008, 51 18: 5522-5532. DOI:10.1021/jm800295d
[2] FLORENCE I RAYNAUD. Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941.[J]. Molecular Cancer Therapeutics, 2009, 8 7: 1725-1738. DOI:10.1158/1535-7163.mct-08-1200
[3] STEFAN KNAPP. A public-private partnership to unlock the untargeted kinome[J]. Nature chemical biology, 2012, 9 1: 3-6. DOI:10.1038/nchembio.1113
[4] DEBASHIS SARKER. First-in-human phase I study of pictilisib (GDC-0941), a potent pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor, in patients with advanced solid tumors.[J]. Clinical Cancer Research, 2015, 21 1: 77-86. DOI:10.1158/1078-0432.ccr-14-0947

Pictilisib Preparation Products And Raw materials

Raw materials

Preparation Products

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Pictilisib Suppliers

Canada 1 China 201 Germany 1 India 4 The Netherlands 1 United Kingdom 3 United States 24 Global 235
Changzhou Chenhong Biotechnology Co., Ltd.
Tel
+86-0519-85788828 +86-13775037613
Email
sales@chemrenpharm.com
Country
China
ProdList
3934
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58
Wuhan Shanhai Zhihe Biotechnology Co., Ltd.
Tel
17771424646
Email
shoubull@126.com
Country
China
ProdList
957
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58
Wuhan Chuangshuo Chemical Technology Co., Ltd
Tel
180-62205282 18062205282
Email
turbo_cq@163.com
Country
China
ProdList
34
Advantage
58
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
J & K SCIENTIFIC LTD.
Tel
18210857532; 18210857532
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
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Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6003
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61
Capot Chemical Co., Ltd
Tel
+86 (0) 571 85 58 67 18
Fax
0086-571-85864795
Country
China
ProdList
18207
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JinYan Chemicals(ShangHai) Co.,Ltd.
Tel
13817811078
Fax
86-021-50426522,50426273
Email
sales@jingyan-chemical.com
Country
China
ProdList
9976
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Shanghai Sinch Parmaceuticals Tech. Co. Ltd.
Tel
+86-21-54098501
Fax
+86-21-54096319
Email
sales@sinch.com.cn
Country
China
ProdList
11598
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Shanghai Yuanding Chem. Sci. & Tech. Co., Ltd.
Tel
21-57721279
Fax
QQ：14057904
Email
sales@shydchem.com.cn
Country
China
ProdList
998
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View Lastest Price from Pictilisib manufacturers

Career Henan Chemical Co
Product
Thieno[3,2-d]pyrimidine, 2-(1H-indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)- 957054-30-7
Price
US $2.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
100kg
Release date
2018-12-23

957054-30-7, PictilisibRelated Search:

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  • Pictilisib
  • Thieno[3,2-d]pyrimidine, 2-(1H-indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)-
  • GDC-0941
  • GDC-0941 free base
  • 2-(1H-Indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)thieno[3,2-d]pyrimidine
  • GDC-0941 bismesylate
  • 2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine
  • 4-(2-(1H-Indazol-4-yl)-6-((4-(Methylsulfonyl)piperazin-1-yl)Methyl)thieno[3,2-d]
  • 4-{6-[(4-Methanesulfonylpiperazin-1-yl)Methyl]-4-(Morpholin-4-yl)thieno[3,2-d]pyriMidin-2-yl}-1H-indazole
  • 4-(2-(1H-indazol-4-yl)-6-((4-(Methylsulfonyl)piperazin-1-yl)Methyl)thieno[3,2-d]pyriMidin-4-yl)Morpholine
  • 2-(1H-Indazol-4-yl)-6-(4-methanesulfonylpiperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrim
  • 2-(1H-indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinothieno[3,2-d]pyrimidine
  • RG7321
  • 2-(1H-Indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)thieno[3,2-d]pyrimidine GDC-0941
  • GDC-0941 2-(1H-Indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)thieno[3,2-d]pyrimidine
  • GDC-0941 (Pictilisib)
  • pictrelisib
  • GDC-0941;GDC 0941;GDC0941
  • 2-(1H-Indazol-4-yl)-6-(4-methanesulfonylpiperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]py
  • GDC-0941, >=98%
  • Pictilisib, 98%, a potent inhibitor of PI3Kα/δ
  • GDC0941; GDC 0941; RG7321
  • GDC-0941;GDC 0941
  • CS-23
  • GDC-01
  • Pictilisib (GDC0941, RG7321, GNE0941))
  • 4-[2-(1H-indazol-4-yl)-6-[(4-methylsulfonylpiperazin-1-yl)me...
  • PI 3-K Inhibitor XXI GDC-0941 GDC0941
  • GNE 0941
  • GNE0941
  • GNE-0941
  • GDC-0941 Base
  • Pictilisib, 10 mM in DMSO
  • Mcl-1 Inhibitor III, UMI-77
  • PI 3-K Inhibitor XXI, GDC-0941
  • Pictilisib (GDC-0941) ，S1065
  • 957054-30-7
  • C23H27N7O3S2
  • An inhibitor of class I PI3 kinase (PI3K).
  • Inhibitors
  • Akt
  • mTOR
  • PI3K