Benzeneacetamide, α-[[6-(4-amino-1-piperidinyl)-3,5-dicyano-4-ethyl-2-pyridinyl]thio]-

Product Name: Benzeneacetamide, α-[[6-(4-amino-1-piperidinyl)-3,5-dicyano-4-ethyl-2-pyridinyl]thio]-
CAS No.: 2170137-61-6
Chemical Name: Benzeneacetamide, α-[[6-(4-amino-1-piperidinyl)-3,5-dicyano-4-ethyl-2-pyridinyl]thio]-
Synonyms: GSK3685032 ，E1046;GSK3685032, 10 mM in DMSO;2-((6-(4-Aminopiperidin-1-yl)-3,5-dicyano-4-ethylpyridin-2-yl)thio)-2-phenylacetamide;Benzeneacetamide, α-[[6-(4-amino-1-piperidinyl)-3,5-dicyano-4-ethyl-2-pyridinyl]thio]-;Inhibitor,GSK 3685032,lymphoma,DNMTs,cancer,DNA MTases,GSK-3685032,inhibit,GSK3685032,DNA Methyltransferase,MV4–11,leukemia,GDM-1,multiple myeloma;Inhibitor,GSK3685032,lymphoma,DNMTs,cancer,DNAMTases,GSK-3685032,inhibit,GSK3685032,DNAMetChemicalbookhyltransferase,MV4–11,leukemia,GDM-1,multiplemyeloma
CBNumber: CB29785450
Molecular Formula: C22H24N6OS
Formula Weight: 420.54
MOL File: 2170137-61-6.mol

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Benzeneacetamide, α-[[6-(4-amino-1-piperidinyl)-3,5-dicyano-4-ethyl-2-pyridinyl]thio]- Property

Boiling point:: 669.4±55.0 °C(Predicted)
Density: 1.33±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO : 25 mg/mL (59.45 mM; Need ultrasonic)
form: Solid
pka: 14.65±0.50(Predicted)
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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Benzeneacetamide, α-[[6-(4-amino-1-piperidinyl)-3,5-dicyano-4-ethyl-2-pyridinyl]thio]- Chemical Properties,Usage,Production

Uses

GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition[1].

Biological Activity

GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition[1]. GSK-3685032 (6 days) has cell growth inhibition of majority cancer cell lines, with a median growth IC50 value of 0.64 μM[1].GSK-3685032 (0.1-1000 nM, 1-6 days) exhibits growth inhibition after 3 days, with decreasing growth IC50 throughout a 6 d time course[1].GSK3685032 (10-10000 nM, day 4) dose-dependently increases the immune-related gene transcription[1].GSK3685032 (3.2-10,000 nM, 2 days) inhibits DNMT1 protein expression[1].GSK3685032 induces DNA hypomethylation and gene activation[1]. GSK-3685032 (1-45 mg/kg; subcutaneous twice daily for 28 days) inhibits tumor growth in the subcutaneous MV4-11 or SKM-1 xenograft models[1]. Summary of mouse pharmacokinetic parameters for GSK-3685032[1] Dose,Route Cmax(ng/mL) AUC0-8hr(h*ng/mL) DNAUC(h*kg*ng/mL/mg) Clearance(mL/min/kg) Volumedss(L/kg) T1/2(h) 2 mg/kg,IV 5103 2418 1209 13 1.3 1.8 2 mg/kg,SC 252 921 461 NA NA 2.8 2 mg/kg,SC 5473 15400 513 NA NA ND

in vivo

GSK-3685032 (1-45 mg/kg; subcutaneous twice daily for 28 days) inhibits tumor growth in the subcutaneous MV4-11 or SKM-1 xenograft models^[1].

Summary of mouse pharmacokinetic parameters for GSK-3685032^[1]

Dose,Route	C_max (ng/mL)	AUC_0-8hr (h*ng/mL)	DNAUC (hkgng/mL/mg)	Clearance (mL/min/kg)	Volume_dss (L/kg)	T_1/2 (h)
2 mg/kg,IV	5103	2418	1209	13	1.3	1.8
2 mg/kg,SC	252	921	461	NA	NA	2.8
2 mg/kg,SC	5473	15400	513	NA	NA	ND

Animal Model:	MV4-11 xenograft models (female CD1-Foxn1 mice, 12 weeks of age) or SKM-1 xenograft models (NOD. CB17-Prkdc1NCrCrl mice, 8-11 weeks of age)^[1]
Dosage:	1, 5, 15, 30, 45 mg/kg (10% captisol adjusted to pH 4.5-5 with 1 M acetic acid, stored for up to 1 week at 4 °C)
Administration:	Subcutaneous injection, twice daily for 4 weeks
Result:	Revealed statistically significant dose-dependent tumor growth inhibition with clear regression at ≥30 mg/kg.

References

[1]. Pappalardi MB, et al. Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia. Nat Cancer. 2021;2(10):1002-1017.

Benzeneacetamide, α-[[6-(4-amino-1-piperidinyl)-3,5-dicyano-4-ethyl-2-pyridinyl]thio]- Preparation Products And Raw materials

Raw materials

Preparation Products

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Benzeneacetamide, α-[[6-(4-amino-1-piperidinyl)-3,5-dicyano-4-ethyl-2-pyridinyl]thio]- Suppliers

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2170137-61-6, Benzeneacetamide, α-[[6-(4-amino-1-piperidinyl)-3,5-dicyano-4-ethyl-2-pyridinyl]thio]-Related 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 GSK778 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

Benzeneacetamide, α-[[6-(4-amino-1-piperidinyl)-3,5-dicyano-4-ethyl-2-pyridinyl]thio]-

Inhibitor,GSK 3685032,lymphoma,DNMTs,cancer,DNA MTases,GSK-3685032,inhibit,GSK3685032,DNA Methyltransferase,MV4–11,leukemia,GDM-1,multiple myeloma

2-((6-(4-Aminopiperidin-1-yl)-3,5-dicyano-4-ethylpyridin-2-yl)thio)-2-phenylacetamide

GSK3685032, 10 mM in DMSO

GSK3685032 ，E1046

Inhibitor,GSK3685032,lymphoma,DNMTs,cancer,DNAMTases,GSK-3685032,inhibit,GSK3685032,DNAMetChemicalbookhyltransferase,MV4–11,leukemia,GDM-1,multiplemyeloma

2170137-61-6