MIK665
- S64315
Axon 3713
CAS:
1799631-75-6
- Optical Purity: 99% e.e.
- Soluble in DMSO
- MF: C47H44ClFN6O6S
- MW: 875.41
Description
MIK665 is a clinical-stage, BH3-Groove binding Mcl-1 inhibitor, potently and selectively binding to the protein target with Ki in picomolar range. Demonstrate in vitro and in vivo antitumor efficacy in Mcl-1 dependent cancer models. Achieve superior activity and enhanced solid tumor response when applied in combination with Bcl-2 inhibitors such as ABT-199 (Axon 2141) or BCL-201 (Axon 3714).
More Information
| Parent CAS No. | 1799631-75-6 |
|---|---|
| Chemical Name | (R)-2-((S)-5-(3-chloro-2-methyl-4-(2-(4-methylpiperazin-1-yl)ethoxy)phenyl)-6-(4-fluorophenyl)thieno[2,3-d]pyrimidin-4-yloxy)-3-(2-((2-(2-methoxyphenyl)pyrimidin-4-yl)methoxy)phenyl)propanoic acid |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | N1C(O[C@H](CC2C=CC=CC=2OCC2N=C(C3C(OC)=CC=CC=3)N=CC=2)C(O)=O)=C2C(C3C=CC(OCCN4CCN(C)CC4)=C(Cl)C=3C)=C(C3C=CC(F)=CC=3)SC2=NC=1 |&1:3,32,r,wU:3.3,33.35,35.37,(16.39,-10.57,;17.02,-10.21,;17.02,-9.48,;16.39,-9.12,;16.39,-8.39,;15.76,-8.02,;15.13,-8.39,;14.50,-8.02,;14.50,-7.29,;15.13,-6.93,;15.76,-7.29,;16.39,-6.93,;17.02,-7.29,;17.66,-6.93,;17.66,-6.20,;18.29,-5.83,;18.29,-5.10,;17.66,-4.74,;17.02,-5.10,;16.39,-4.74,;17.66,-4.01,;18.29,-3.64,;18.92,-4.01,;18.92,-4.74,;18.92,-6.20,;18.92,-6.93,;18.29,-7.29,;15.76,-9.48,;15.13,-9.12,;15.76,-10.21,;17.66,-10.57,;18.35,-10.35,;18.58,-9.65,;18.09,-9.11,;18.32,-8.42,;19.03,-8.26,;19.26,-7.57,;19.97,-7.42,;20.46,-7.96,;21.17,-7.81,;21.39,-7.11,;22.11,-6.96,;22.60,-7.51,;23.31,-7.35,;22.37,-8.20,;21.66,-8.35,;19.52,-8.81,;20.23,-8.66,;19.29,-9.50,;19.78,-10.04,;18.78,-10.94,;19.51,-10.94,;19.88,-10.31,;20.61,-10.31,;20.97,-10.94,;21.70,-10.94,;20.61,-11.57,;19.88,-11.57,;18.35,-11.53,;17.66,-11.30,;17.02,-11.67,;16.39,-11.30,)| |
| MFCD | N.A. |
| InChi | InChI=1S/C47H44ClFN6O6S/c1-29-34(16-17-38(42(29)48)59-25-24-55-22-20-54(2)21-23-55)40-41-45(51-28-52-46(41)62-43(40)30-12-14-32(49)15-13-30)61-39(47(56)57)26-31-8-4-6-10-36(31)60-27-33-18-19-50-44(53-33)35-9-5-7-11-37(35)58-3/h4-19,28,39H,20-27H2,1-3H3,(H,56,57)/t39-/m1/s1 |
| InChiKey | PKYIMGFMRFVOMB-LDLOPFEMSA-N |
| CID | 118157243 |
| Short Description | BH3-Groove binding Mcl-1 inhibitor |
References
- E. Halilovic, et al, MIK665/S64315, a novel Mcl-1 inhibitor, in combination with Bcl-2 inhibitors exhibits strong synergistic antitumor activity in a range of hematologic malignancies [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2019; 2019 Mar 29-Apr 3; Atlanta, GA. AACR; Cancer Res 2019,; 79(13 Suppl), Abstract nr 4477.
- Z. Szlavik, et al. Discovery of S64315, a Potent and Selective Mcl-1 Inhibitor. J Med Chem. 2020, 63, 13762-13795.
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