[CAS NO. 1799633-27-4] S63845

Name: S63845
Brand: Arctom Scientific
SKU: SLK-S8383

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PRODUCTS SPECIFICATIONS [1799633-27-4]

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Catalog

SLK-S8383

Brand

Selleck

CAS

1799633-27-4

DESCRIPTION [1799633-27-4]

Overview

MDL	MFCD31382374
Molecular Weight	829.26
Molecular Formula	C39H37ClF4N6O6S
SMILES	O(C(CC1=C(OCC=2N(CC(F)(F)F)N=CC2)C=CC=C1)C(O)=O)C3=C4C(=C(SC4=NC=N3)C5=CC=C(F)O5)C6=C(C)C(Cl)=C(OCCN7CCN(C)CC7)C=C6

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.2059 mL	6.0295 mL	12.0589 mL
5 mM	0.2412 mL	1.2059 mL	2.4118 mL
10 mM	0.1206 mL	0.6029 mL	1.2059 mL
50 mM	0.0241 mL	0.1206 mL	0.2412 mL

Description

S63845 is a new, selective inhibitor with the Kd value of 0.19 nM and has no discernible binding to the other BCL-2 members, BCL-2 or BCL-XL.

Targets

human MCL-1 ^[1]

0.19 nM(Kd)

In vitro

S63845 induces death of cancer cell lines with known reliance on MCL-1, displaying classical hallmarks of apoptosis that are dependent on caspases and BAX/BAK-mediated mitochondrial outer membrane permeabilisation. It has a 6 fold higher affinity for human MCL-1 over mouse MCL-1. S63845 is effective against haematological cancer-derived cell lines in vitro and in vivo and also AML samples, but does not readily kill normal human haematopoietic progenitor cells.

In vivo

In vivo, S63845 shows potent anti-tumour activity with an acceptable safety margin as a single agent in several cancers. S63845 is well tolerated by the mice with no significant weight loss observed. Some of solid tumour models shows sensitivity to S63845 monotherapy, while many others are only killed when treated with a combination of S63845 and inhibitors of oncogenic kinases.

References

[1] Jason A. Powell, et al. Journal of Xiangya Medicine. 2017.
[2] Kotschy A, et al. Nature. 2016, 538(7626):477-482.

Synonyms

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)-

(αR)-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]benzenepropanoic acid

S 63845

S-63845