ChemicalBook > CAS DataBase List > GSK778

GSK778

Product Name: GSK778
CAS No.: 2451862-42-1
Chemical Name: GSK778
Synonyms: GSK778;iBET-BD1;GSK778, 10 mM in DMSO;iBET-BD1 dihydrochloride;GSK778|||GSK 778|||GSK-778;GSK778（iBET-BD1 dihydrochloride）;iBET-BD1 dihydrochloride (GSK778);2451862-42-1;7-(3,5-Dimethyl-4-isoxazolyl)-2-(methoxymethyl)-1-[(1R)-1-phenylethyl]-8-[(3S)-3-pyrrolidinylmethoxy]-1H-imidazo[4,5-c]quinoline;4-(2-(methoxymethyl)-1-((R)-1-phenylethyl)-8-(((S)-pyrrolidin-3-yl)methoxy)-1H-imidazo[4,5-c]quinolin-7-yl)-3,5-dimethylisoxazole
CBNumber: CB18140497
Molecular Formula: C30H33N5O3
Formula Weight: 511.61
MOL File: 2451862-42-1.mol

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GSK778 Property

Boiling point:: 679.6±55.0 °C(Predicted)
Density: 1.31±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO : 41.67 mg/mL (81.45 mM; Need ultrasonic)
pka: 9.90±0.10(Predicted)
form: Solid
color: White to light yellow
InChIKey: ZORLJXWXFABTPZ-CTNGQTDRSA-N
SMILES: N1C2C(=CC(OC[C@H]3CCNC3)=C(C3=C(C)ON=C3C)C=2)C2N([C@@H](C3=CC=CC=C3)C)C(COC)=NC=2C=1

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0131693
Product name: GSK778
Purity: 98.58%
Packaging: 5mg
Price: $700
Updated: 2021/12/16

ChemScene

Product number: CS-0131693
Product name: GSK778
Purity: 98.58%
Packaging: 10mg
Price: $1200
Updated: 2021/12/16

ChemScene

Product number: CS-0131693
Product name: GSK778
Purity: 98.58%
Packaging: 25mg
Price: $2500
Updated: 2021/12/16

ChemScene

Product number: CS-0131693
Product name: GSK778
Purity: 98.58%
Packaging: 50mg
Price: $4200
Updated: 2021/12/16

ChemScene

Product number: CS-0131693
Product name: GSK778
Purity: 98.58%
Packaging: 100mg
Price: $6500
Updated: 2021/12/16

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GSK778 Chemical Properties,Usage,Production

Uses

GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models[1].

in vivo

GSK778 (15?mg/kg/BID; i.p. for 30 days) offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model^[1].
? GSK778 (15?mg/kg/BID; s.c. for 14 days) reduces the production of anti-keyhole limpet hemocyanin (KLH) IgM and is well tolerated^[1].
? GSK778 exhibits C_max (85 ng/mL), T_max (1.48 h) and AUC_∞ (132 ng.h/mL) following oral administration (10?mg/kg) in mice^[1].

Animal Model:	6-8 weeks female C57BL/6 mice are injected with MLL-AF9 cells^[1]
Dosage:	15?mg/kg/BID
Administration:	I.p. injections for 30 days
Result:	Increased the survival rate of leukemia mice.

Animal Model:	Male CD1 mice^[1]
Dosage:	10?mg/kg (Pharmacokinetic Analysis)
Administration:	P.o. administration
Result:	C_max (85 ng/mL), T_max (1.48 h); AUC_∞ (132 ng.h/mL).

IC 50

BRD2 BD1: 75 nM (IC₅₀); BRD3 BD1: 41 nM (IC₅₀); BRD4 BD1: 41 nM (IC₅₀); BRDT BD1: 143 nM (IC₅₀)

References

[1] Omer G, et, al. Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation. Science. 2020 Apr 24; 368(6489): 387-394. DOI:10.1126/science.aaz8455

GSK778 Preparation Products And Raw materials

Raw materials

Preparation Products

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2451862-42-1, GSK778Related Search:

GSK2837808A GSK6853 GSK-A1 S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide GSK864 GSK484 GSK J4 HCl GSK 2334470 GSK2982772 GSK2636771 Benzeneacetamide, α-[[6-(4-amino-1-piperidinyl)-3,5-dicyano-4-ethyl-2-pyridinyl]thio]- N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide GSK 2033 2-((4-(benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl dihydrogen phosphate N-((S)-1-(4-((S)-2-(2,4-dichlorophenylsulfonaMido)-3-hydroxypropanoyl)piperazin-1-yl)-4-Methyl-1-oxopentan-2-yl)benzo[b]thiophene-2-carboxaMide GSK-2256098 GSK215

1H-Imidazo[4,5-c]quinoline, 7-(3,5-dimethyl-4-isoxazolyl)-2-(methoxymethyl)-1-[(1R)-1-phenylethyl]-8-[(3S)-3-pyrrolidinylmethoxy]-

iBET-BD1 dihydrochloride

iBET-BD1

GSK778

GSK778（iBET-BD1 dihydrochloride）

iBET-BD1 dihydrochloride (GSK778)

GSK778|||GSK 778|||GSK-778

4-[2-(methoxymethyl)-1-[(1R)-1-phenylethyl]-8-{[(3S)-pyrrolidin-3-yl]methoxy}-1H-imidazo[4,5-c]quinolin-7-yl]-3,5-dimethyl-1,2-oxazole

GSK778, 10 mM in DMSO

4-(2-(methoxymethyl)-1-((R)-1-phenylethyl)-8-(((S)-pyrrolidin-3-yl)methoxy)-1H-imidazo[4,5-c]quinolin-7-yl)-3,5-dimethylisoxazole

4-[2-(methoxymethyl)-1-[(1R)-1-phenylethyl]-8-[[(3S)-pyrrolidin-3-yl]methoxy]imidazo[4,5-c]quinolin-7-yl]-3,5-dimethyl-1,2-oxazole

7-(3,5-Dimethyl-4-isoxazolyl)-2-(methoxymethyl)-1-[(1R)-1-phenylethyl]-8-[(3S)-3-pyrrolidinylmethoxy]-1H-imidazo[4,5-c]quinoline

2451862-42-1