Basic information Safety Supplier Related

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

Basic information Safety Supplier Related

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

Product Name:
Benzeneacetamide, α-[[6-(4-amino-1-piperidinyl)-3,5-dicyano-4-ethyl-2-pyridinyl]thio]-
Synonyms:
  • 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
CAS:
2170137-61-6
MF:
C22H24N6OS
MW:
420.54
Mol File:
2170137-61-6.mol
More
Less

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

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
More
Less

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

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

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]-Supplier

Shanghai Sphchem Co., Ltd.
Tel
021-56491756 13512199871
Email
2819742715@qq.com
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Email
info@efebio.com
ShangHai Biochempartner Co.,Ltd
Tel
177-54423994 17754423994
Email
2853530910@QQ.com
Shanghai SuperLan Chemcial Technique Centre
Tel
021-2022843681 15618226720
Email
lucy@atkchemical.com