[CAS NO. 1919888-06-4] LY3295668
PRODUCTS SPECIFICATIONS [1919888-06-4]
DESCRIPTION [1919888-06-4]
Overview
| MDL | MFCD31807628 |
|---|---|
| Molecular Weight | 489.95 |
| Molecular Formula | C24H26ClF2N5O2 |
| SMILES | O=C([C@@]1(CC2=NC(NC3=NNC(C)=C3)=CC=C2F)C[C@@H](C)N(CC4=CC=CC(Cl)=C4F)CC1)O |
1 Publications Citing Use of MCE
Summary
LY3295668 (AK-01) is a potent, orally active and highly specific Aurora-A kinase inhibitor, with K i values of 0.8 nM and 1038 nM for AurA and AurB, respectively.
IC50 & Target
|
Aurora A 0.8 nM (IC 50 ) |
In Vitro
LY3295668 is a highly specific Aurora-A kinase inhibitor, with K i values of 0.8 nM and 1038 nM for AurA and AurB, respectively. LY3295668, a highly specific AurA inhibitor, can kill Rb-deficient cancer cells at doses that have minimal effects on normal cells. In a kinome-wide survey, only 5 of 386 kinases are potently inhibited by LY3295668 (<10 nM) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04106219 | Eli Lilly and Company|New Approaches to Neuroblastoma Therapy Consortium (NANT)|Innovative Therapies for Children with Cancer in Europe (ITCC) |
Neuroblastoma
|
June 11, 2020 | Phase 1 |
| NCT04956640 | Eli Lilly and Company|Loxo Oncology, Inc.|Merck Sharp & Dohme LLC |
Carcinoma, Non-Small-Cell Lung|Colorectal Neoplams|Endometrial Neoplasms|Ovarian Neoplasms|Pancreatic Neoplasms
|
July 19, 2021 | Phase 1 |
| NCT03955939 | Eli Lilly and Company |
Metastatic Breast Cancer
|
August 2, 2019 | Phase 1 |
| NCT03898791 | Eli Lilly and Company |
Small Cell Lung Cancer
|
July 16, 2019 | Phase 1 |
| NCT05017025 | M.D. Anderson Cancer Center|National Cancer Institute (NCI) |
Advanced Lung Non-Squamous Non-Small Cell Carcinoma|Metastatic Lung Non-Squamous Non-Small Cell Carcinoma|Stage III Lung Cancer AJCC v8|Stage IIIA Lung Cancer AJCC v8|Stage IIIB Lung Cancer AJCC v8|Stage IIIC Lung Cancer AJCC v8|Stage IV Lung Cancer AJCC v8|Stage IVA Lung Cancer AJCC v8|Stage IVB Lung Cancer AJCC v8
|
February 17, 2022 | Phase 1|Phase 2 |
| NCT03092934 | Eli Lilly and Company|AurKa Pharma Inc. |
Neoplasms|Neoplasm Metastasis|Triple Negative Breast Neoplasms|Head and Neck Neoplasms|Breast Neoplasms|Solid Tumor, Adult|Small Cell Lung Carcinoma
|
May 29, 2017 | Phase 1|Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL ( 204.10 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0410 mL | 10.2051 mL | 20.4102 mL |
| 5 mM | 0.4082 mL | 2.0410 mL | 4.0820 mL |
| 10 mM | 0.2041 mL | 1.0205 mL | 2.0410 mL |
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1.
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2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution
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3.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution
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4.
-
5.
Add each solvent one by one: 1% DMSO >> 99% saline
Solubility: ≥ 0.5 mg/mL (1.02 mM); Clear solution
