S63845 (S-63845)

S63845 (S-63845)

$160.00$760.00

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$160.00$760.00

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SKU: APIM050287
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Description

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.

APIM050287: 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.

Additional information

Ship from Country

USA

Size

10 mg, 5 mg, 50 mg

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