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Background Information:
S63845 is the first high affinity MCL-1 inhibitor with in vivo activity, binding to the BH3 groove of human MCL-1 with a KD value of 0.19 nM, highly selective against other BCL family proteins BCL-2 (Ki >10,000nM) and BCL-XL (Ki >10,000nM) (ref 1). S63845 showed the clear-on-target activity killing Mcl-1-dependent cancer cells, including multiple myeloma, leukemia and lymphoma cells. Demonstrated potent in vivo antitumor activity, with an acceptable safety margin, as a single agent in several cancer types (ref 1).
Reference:
1. A. Kotschy, et al, The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models Nature, 538, 477–482 (27 October 2016).
2. Quality is good for I.V. Administration; a. Verified by Chiral HPLC; b. Binding potency (IC50 = 0.7 nM) was measured for its ability to displace BAK peptide from Mcl1-BAK complex.
APIM050063: S63845 (S-63845)
CAS No.: 1799633-27-4.
Molecular Formula: C39H37ClF4N6O6S?H2O.
Molecular Weight: 847.3.
Purity: 99.9-100% by Achiral and Chiral HPLCs.
QC: Achiral and Chiral HPLCs, 1H-NMR, and Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
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