| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
Purity: ≥98%
MIK665 (also known as MIK-665; S-64315) is a novel, investigational and specific Mcl-1 inhibitor with an IC50 of 1.81 nM. Potential pro-apoptotic and anti-cancer properties of MIK665. It binds to and prevents the activity of Mcl-1, which causes cells that overexpress Mcl-1 to proliferate. The Bcl-2 family of proteins member Mcl-1, an anti-apoptotic protein, is upregulated in cancer cells and supports the survival of tumor cells. MCL-1, a protein belonging to the BCL-2 family that inhibits apoptosis, is a crucial regulator of mitochondrial homeostasis. MCL-1 is an alluring target for cancer therapy due to its frequent overexpression in human primary cancer cells and drug-resistant cancer cells. Three MCL-1 selective inhibitors have made it to clinical trials as a result of significant advancements in the development of small-molecule MCL-1 inhibitors in recent years.
| Targets |
Mcl-1 (IC50 = 1.81 nM)
|
|---|---|
| ln Vitro |
When paired with ABT-199, MIK665 (S-64315) has synergistic effects akin to those of S63845. Comparable results have been observed in terms of reducing cell viability in typical melanoma cell lines (MB2141, MB3616, MB3961, MB4667, A375, and 1205Lu cells) when S64315 (0.156-10 μM) and ABT-199 (625 nM) are combined. The chemical preparation 13 of patent WO2016207225A1, which contains MIK665, inhibits H929 cells with an IC50 of 250 nM [2].
|
| References |
[1]. Mukherjee N, et al. Simultaneously Inhibiting BCL2 and MCL1 Is a Therapeutic Option for Patients with Advanced Melanoma. Cancers (Basel). 2020;12(8):2182. Published 2020 Aug 5.
[2]. Zoltán SZLÁVIK, et al. New hydroxyester derivatives, a process for their preparation and pharmaceutical compositions containing them. WO2016207225A1. |
| Molecular Formula |
C47H44CLFN6O6S
|
|---|---|
| Molecular Weight |
875.41
|
| Exact Mass |
874.27
|
| Elemental Analysis |
C, 64.49; H, 5.07; Cl, 4.05; F, 2.17; N, 9.60; O, 10.97; S, 3.66
|
| CAS # |
1799631-75-6
|
| Related CAS # |
(R)-MIK665;1799831-02-9
|
| Appearance |
Solid powder
|
| SMILES |
CC1=C(C=CC(=C1Cl)OCCN2CCN(CC2)C)C3=C(SC4=NC=NC(=C34)O[C@H](CC5=CC=CC=C5OCC6=NC(=NC=C6)C7=CC=CC=C7OC)C(=O)O)C8=CC=C(C=C8)F
|
| InChi Key |
PKYIMGFMRFVOMB-LDLOPFEMSA-N
|
| InChi Code |
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
|
| Chemical Name |
(2R)-2-[5-[3-chloro-2-methyl-4-[2-(4-methylpiperazin-1-yl)ethoxy]phenyl]-6-(4-fluorophenyl)thieno[2,3-d]pyrimidin-4-yl]oxy-3-[2-[[2-(2-methoxyphenyl)pyrimidin-4-yl]methoxy]phenyl]propanoic acid
|
| Synonyms |
S 64315; MIK-665; S-64315; MIK665; S64315; MIK 665
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ≥125 mg/mL (~142.8 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (2.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 5%DMSO+40%PEG300+5%Tween80+50%ddH2O: 5 mg/ml |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1423 mL | 5.7116 mL | 11.4232 mL | |
| 5 mM | 0.2285 mL | 1.1423 mL | 2.2846 mL | |
| 10 mM | 0.1142 mL | 0.5712 mL | 1.1423 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04629443 | Active Recruiting |
Drug: S 64315 and azacitidine | Acute Myeloid Leukaemia | Institut de Recherches Internationales Servier |
February 17, 2021 | Phase 1 Phase 2 |
| NCT04702425 | Active Recruiting |
Drug: VOB560 Drug: MIK665 |
Non-Hodgkin Lymphoma (NHL) Multiple Myeloma (MM) |
Novartis Pharmaceuticals | June 23, 2021 | Phase 1 |
| NCT03672695 | Completed | Combination Product: S 64315 and venetoclax |
Acute Myeloid Leukaemia | Institut de Recherches Internationales Servier |
November 28, 2018 | Phase 1 |
| NCT02992483 | Completed | Drug: MIK665 | Multiple Myeloma (MM) Lymphoma Large B-Cell Diffuse (DLBCL) Lymphoma |
Novartis Pharmaceuticals | July 12, 2017 | Phase 1 |
| NCT02979366 | Completed | Drug: S64315 once a week Drug: S64315 twice a week |
Acute Myeloid Leukaemia (AML) Myelodysplastic Syndrome (MDS) |
Institut de Recherches Internationales Servier |
March 15, 2017 | Phase 1 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA