GDC-0084

Product Name: GDC-0084
CAS No.: 1382979-44-3
Chemical Name: GDC-0084
Synonyms: RG7666;CS-2290;RG-7666;GDC-0084;RG 7666);Paxalisib;GDC-0084(RG7666);GDC-0084 (GDC0084;GDC-0084 (Paxalisib;Paxalisib (GDC-0084)
CBNumber: CB93123145
Molecular Formula: C18H22N8O2
Formula Weight: 382.42
MOL File: 1382979-44-3.mol

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GDC-0084 Property

Density: 1.60±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: insoluble in H2O; insoluble in EtOH; ≥2.83 mg/mL in DMSO with ultrasonic
form: Solid
pka: 2.62±0.40(Predicted)

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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.

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

Biosynth Carbosynth

Product number: FD145121
Product name: GDC 0084
Packaging: 1mg
Price: $60
Updated: 2021/12/16

Biosynth Carbosynth

Product number: FD145121
Product name: GDC 0084
Packaging: 2mg
Price: $94
Updated: 2021/12/16

ApexBio Technology

Product number: B7826
Product name: GDC-0084
Packaging: 1mg
Price: $95
Updated: 2021/12/16

AK Scientific

Product number: 4658DN
Product name: Gdc-0084
Packaging: 1mg
Price: $131
Updated: 2021/12/16

ApexBio Technology

Product number: B7826
Product name: GDC-0084
Packaging: 10mM(in 1mL DMSO)
Price: $158
Updated: 2021/12/16

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GDC-0084 Chemical Properties,Usage,Production

Uses

GDC-0084 is an inhibitor of phosphoinositide 3-kinase (PI3K) and mTOR (1,2). Inhibitors of PI3K are useful compounds for developing treatments for brain tumors.

Preparation

Stumpf et al. at Genentech Inc. (Roche group) developed an efficient multikilogram process to synthesize the brain penetrant PI3K inhibitor, GDC?\0084, a potential drug candidate for the treatment of several brain cancers. An efficient Suzuki coupling reaction between a chloropyrimidine and an arylboronic ester using a palladium catalyst at low loading was reported. The optimized conditions were demonstrated on 6.75 kg of a chloropyrimidine intermediate, providing 7.49 kg of crude GDC?\0084 (94% yield, 99.4% HPLC purity). Using the commercially available XPhos Pd G2 catalyst, instead of the usual PdCl2(dppf)·CH2Cl2 catalyst, it was possible to reduce the catalyst loading from 2 to 0.5 mol%. A final scavenging/recrystallization combination from Si?\Thiol (a solid?\supported resin) and acetic acid/water provided the crude GDC?\0084 with the required purity and polymorphic form (off?\white solid, 6.41 kg, 83% yield, 99.7% HPLC purity).

Genentech’s route to GDC?\0084 employing a pivotal Suzuki reaction.

Biological Activity

gdc-0084 is a potent and brain penetrant inhibitor of pi3k and mtor with ki values of 2 nm and 70 nm for pi3kα and mtor, respectively [1].glioblastoma (gbm) is the most common primary brain tumor in adults and aberrant pi3k signaling is associated with more than 80% of cases. the pi3k pathway represents a potential target for the treatment of this disease and the inhibitors would need to freely cross the blood-brain barrier (bbb) [1][2].gdc-0084 is a potent and brain penetrant inhibitor of pi3k and mtor. in vitro kinase assay, gdc-0084 exhibited ki values of 2 nm, 46 nm, 3 nm, 10 nm and 70 nm for pi3kα, pi3kβ, pi3kδ, pi3kγ and mtor, respectively. in five different gbm cell lines, gdc-0084 had antiproliferative activities with ec50 values ranging from 0.3 to 1.1 μm. gdc-0084 has excellent human metabolic stability in microsomal and hepatocyte incubations [1]. in transfected cell lines over-expressing human or mouse p-gp or bcrp, gdc-0084 was a poor substrate of these efflux transporters. in mice brain, gdc-0084 significantly lowered pakt and ps6 levels [2].in rats after a 15 mg/kg dose of gdc-0084, the total brain-to-plasma ratio was 1.9-3.3. in subcutaneous u87 glioblastoma tumor xenograft mice model, gdc-0084 significantly inhibited tumor growth in a dose-dependent way. gdc-0084 also concentration-dependently inhibited pakt [1].[1]. heffron tp1, ndubaku co1, salphati l1, et al. discovery of clinical development candidate gdc-0084, a brain penetrant inhibitor of pi3k and mtor. acs med chem lett. 2016 feb 16;7(4):351-6.[2]. salphati l, alicke b, heffron tp, et al. brain distribution and efficacy of the brain penetrant pi3k inhibitor gdc-0084 in orthotopic mouse models of human glioblastoma. drug metab dispos. 2016 dec;44(12):1881-1889. epub 2016 sep 16.

GDC-0084 Preparation Products And Raw materials

Raw materials

Preparation Products

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GDC-0084 Suppliers

China 84 India 2 United Kingdom 1 United States 12 Global 99

MedChemexpress LLC

Tel: 021-58955995
Fax: 609-228-5909
Email: sales@medchemexpress.cn
Country: United States
ProdList: 4861
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Musechem

Tel: +1-800-259-7612
Fax: +1-800-259-7612
Email: info@musechem.com
Country: United States
ProdList: 4660
Advantage: 60

TargetMol Chemicals Inc.

Tel: +1-781-999-5354 +1-00000000000
Email: marketing@targetmol.com
Country: United States
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InvivoChem

Tel: +1-708-310-1919 +1-13798911105
Fax: 708-557-7486
Email: sales@invivochem.cn
Country: United States
ProdList: 6391
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Cckinase, Inc.

Tel: +1 (732)236-3202
Email: sales@cckinase.com
Country: United States
ProdList: 2738
Advantage: 58

BOC Sciences

Tel: +1-631-485-4226
Fax: 1-631-614-7828
Email: inquiry@bocsci.com
Country: United States
ProdList: 19553
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Aladdin Scientific

Tel: +1-+1(833)-552-7181
Email: sales@aladdinsci.com
Country: United States
ProdList: 57505
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TargetMol Chemicals Inc.

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United States Biological

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ApexBio Technology

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BOC Sciences

Tel: 16314854226
Email: info@bocsci.com
Country: United States
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Cayman Chemical Company

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View Lastest Price from GDC-0084 manufacturers

Career Henan Chemical Co

Product: 5-[6,6-Dimethyl-4-(4-morpholinyl)-8,9-dihydro-6H-[1,4]oxazino[4,3-e]purin-2-yl]-2-pyrimidinamine 1382979-44-3
Price: US $1.00/KG
Min. Order: 1KG
Purity: Min98% HPLC
Supply Ability: g/kg/ton
Release date: 2019-12-20

1382979-44-3, GDC-0084Related Search:

N-Ethyl-N'-[4-[5,6,7,8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(3-oxetanyl)pyrido[3,4-d]pyrimidin-2-yl]phenyl]urea SH-4-54 Osimertinib mesylate Tazemetostat (EPZ-6438) Niraparib Mertansine (S)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-triMethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate Enasidenib Ivosidenib ABBV-075 Ponatinib Selonsertib

GDC-0084

5-[8,9-Dihydro-6,6-dimethyl-4-(4-morpholinyl)-6H-[1,4]oxazino[4,3-e]purin-2-yl]-2-pyrimidinamine

5-(6,6-dimethyl-4-morpholino-8,9-dihydro-6H-[1,4]oxazino[4,3-e]purin-2-yl)pyrimidin-2-amine

2-Pyrimidinamine, 5-[8,9-dihydro-6,6-dimethyl-4-(4-morpholinyl)-6H-[1,4]oxazino[4,3-e]purin-2-yl]-

5-[6,6-Dimethyl-4-(4-morpholinyl)-8,9-dihydro-6H-[1,4]oxazino[4,3-e]purin-2-yl]-2-pyrimidinamine

GDC-0084(RG7666)

CS-2290

GDC-0084 (GDC0084

RG 7666)

RG7666

RG-7666

RG7666; RG-7666; RG 7666; GDC-0084; GDC0084; GDC 0084

GDC-0084;GDC 0084;RG7666;RG-7666;RG 7666

Paxalisib

Paxalisib (GDC-0084)

GDC-0084 (Paxalisib

Paxalisib, GDC-0084, RG7666

GDC-0084|||RG7666|||GDC 0084

1382979-44-3