Synonym
KO-947; KO 947; KO947.
IUPAC/Chemical Name
1,5,6,8-Tetrahydro-6-(phenylmethyl)-3-(4-pyridinyl)-7H-pyrazolo[4,3-g]quinazolin-7-one
InChi Key
ODIUJYZERXVGEI-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H17N5O/c27-21-23-18-11-19-17(20(25-24-19)15-6-8-22-9-7-15)10-16(18)13-26(21)12-14-4-2-1-3-5-14/h1-11H,12-13H2,(H,23,27)(H,24,25)
SMILES Code
O=C1NC2=CC(NN=C3C4=CC=NC=C4)=C3C=C2CN1CC5=CC=CC=C5
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
KO-947 appears to be differentiated from other published ERK inhibitors by an extended residence time and prolonged pathway inhibition in vitro and in vivo. The data further suggest that the drug properties of KO-947 may allow Kura to maximize the therapeutic window with flexible administration routes and schedules, including intermittent dosing.
Biological target:
KO-947 is a potent and selective inhibitor of ERK1/2 kinases with potential utility in MAPK pathway dysregulated tumors.
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
66.8 |
187.82 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
355.40
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
TBD
1: Deng X, Ren P, Mai W, Wang Y, Zhang Y, Wu H, Xie Y, Chen H. From Lab
Formulation Development to CTM Manufacturing of KO-947 Injectable Drug Products:
a Case Study and Lessons Learned. AAPS PharmSciTech. 2021 Jun 2;22(5):168. doi:
10.1208/s12249-021-02059-x. PMID: 34080070.
2: Schram AM, Boni V, Adjei AA, Olszanski AJ, Vieito M, Francis JH, Kurman M,
Ahsan JM, Tomkinson B, Garralda E. A phase I, first-in-human trial of KO-947, an
ERK1/2 inhibitor, in patients with advanced solid tumors. ESMO Open. 2025
Mar;10(3):104300. doi: 10.1016/j.esmoop.2025.104300. Epub 2025 Feb 21. PMID:
39985888; PMCID: PMC11904481.
