Basic information Safety Supplier Related

S63845

Basic information Safety Supplier Related

S63845 Basic information

Product Name:
S63845
Synonyms:
  • (R)-2-((5-(3-chloro-2-methyl-4-(2-(4-methylpiperazin-1-yl)ethoxy)phenyl)-6-(5-fluorofuran-2-yl)thieno[2,3-d]pyrimidin-4-yl)oxy)-3-(2-((1-(2,2,2-trifluoroethyl)-1H-pyrazol-5-yl)methoxy)phenyl)propanoic acid
  • (2R)-2-(5-(3-chloro-2-methyl-4-(2-(4-methylpiperazin-1-yl)ethoxy)phenyl)-6-(5-fluorofuran-2-yl)thieno[2,3-d]pyrimidin-4-yloxy)-3-(2-((1-(2,2,2-trifluoroethyl)-1H-pyrazol-5-yl)methoxy)phenyl)propanoic acid
  • Benzenepropanoic acid, α-[[(5S)-5-[3-chloro-2-methyl-4-[2-(4-methyl-1-piperazinyl)ethoxy]phenyl]-6-(5-fluoro-2-furanyl)thieno[2,3-d]pyrimidin-4-yl]oxy]-2-[[1-(2,2,2-trifluoroethyl)-1H-pyrazol-5-yl]methoxy]-, (αR)-
  • S63845
  • S 63845;S-63845
  • CS-2477
  • CS-2485
  • S63845 TFA
CAS:
1799633-27-4
MF:
C39H37ClF4N6O6S
MW:
829.26
Product Categories:
  • API
Mol File:
1799633-27-4.mol
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S63845 Chemical Properties

Boiling point:
852.6±65.0 °C(Predicted)
Density 
1.46±0.1 g/cm3(Predicted)
storage temp. 
4°C, protect from light, stored under nitrogen
solubility 
insoluble in H2O; ≥20 mg/mL in MeOH; ≥41.45 mg/mL in DMSO
form 
A crystalline solid
pka
2.54±0.11(Predicted)
color 
White to yellow
InChIKey
ZFBHXVOCZBPADE-JZEPPUFONA-N
SMILES
C1C=C(OCC2=CC=NN2CC(F)(F)F)C(C[C@@H](OC2C3C(C4C=CC(OCCN5CCN(C)CC5)=C(Cl)C=4C)=C(C4=CC=C(F)O4)SC=3N=CN=2)C(=O)O)=CC=1 |&1:17,r|
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Safety Information

HS Code 
2934999090
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S63845 Usage And Synthesis

Description

S63845 is an inhibitor of myeloid cell leukemia 1 (Mcl-1; Ki = 0.19 nM), a pro-survival protein that is overexpressed in many cancers. It induces cell death in multiple myeloma, leukemia, and lymphoma cell lines (IC50s = <0.1-282 nM) via mitochondrial apoptosis. S63845 acts synergistically with trametinib , lapatinib , PLX4032 , and erlotinib to reduce proliferation of SK-MEL-2, BT474, A2058, and PC9 cells, respectively. S63845 (6.25-25 mg/kg) reduces tumor volume in an MV4-11 acute myeloid leukemia mouse xenograft model in a dose-dependent manner.

Uses

S-63845 is used in killing senescent cells and treating senescence-associated diseases or disorders using a combination of a BCL inhibitor and an MCL-1 inhibitor.Potent and selective MCL1 inhibitor

in vivo

S63845 shows potent anti-tumour activity with an acceptable safety margin as a single agent in several cancers. Intravenously injected (i.v.) S63845 exerts dose-dependent anti-tumour activity in human multiple myeloma (H929 and AMO1) xenografts in immunocompromised mice, with maximal tumour growth inhibition of 114% in the AMO1 model and 103% in the H929 model. At 25 mg/kg, S63845 induces complete regression in 7 out of 8 of the mice at 100 days after treatment in the AMO1 model[1].

IC 50

MCL1: 0.19 nM (Kd)

References

[1] ANDRáS KOTSCHY. The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models[J]. Nature, 2016, 538 7626: 477-482. DOI: 10.1038/nature19830

S63845Supplier

Suzhou youruike Chemical Pharmaceutical Technology Co., Ltd Gold
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15317229551
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15151849396@163.com
Chembest Research Laboratories Limited
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+86-21-20908456
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Beijing Ouhe Technology Co., Ltd
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Shanghai Sphchem Co., Ltd.
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021-56491756 13512199871
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ShangHai Caerulum Pharma Discovery Co., Ltd.
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18149758185
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sales-cpd@caerulumpharma.com
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S63845(1799633-27-4)Related Product Information