Synonym
Glasdegib hydrochloride; Glasdegib HCl
IUPAC/Chemical Name
Urea, N-((2R,4R)-2-(1H-benzimidazol-2-yl)-1-methyl-4-piperidinyl)-N'-(4-cyanophenyl)-, hydrochloride (1:1)
InChi Key
OCHAAZGYSAHXOF-LJLRIERRSA-N
InChi Code
InChI=1S/C21H22N6O.ClH/c1-27-11-10-16(24-21(28)23-15-8-6-14(13-22)7-9-15)12-19(27)20-25-17-4-2-3-5-18(17)26-20;/h2-9,16,19H,10-12H2,1H3,(H,25,26)(H2,23,24,28);1H/t16-,19-;/m1./s1
SMILES Code
Cl.CN1CC[C@H](C[C@@H]1c2nc3ccccc3[nH]2)NC(=O)Nc4ccc(cc4)C#N
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
Preparing Stock Solutions
The following data is based on the
product
molecular weight
410.91
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 |
1: Lin S, Shaik N, Martinelli G, Wagner AJ, Cortes J, Ruiz-Garcia A. Population Pharmacokinetics of Glasdegib in Patients With Advanced Hematologic Malignancies and Solid Tumors. J Clin Pharmacol. 2019 Nov 25. doi: 10.1002/jcph.1556. [Epub ahead of print] PubMed PMID: 31769065.
2: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548156/ PubMed PMID: 31643486.
3: Goldsmith SR, Lovell AR, Schroeder MA. Glasdegib for the treatment of adult patients with newly diagnosed acute myeloid leukemia or high-grade myelodysplastic syndrome who are elderly or otherwise unfit for standard induction chemotherapy. Drugs Today (Barc). 2019 Sep;55(9):545-562. doi: 10.1358/dot.2019.55.9.3020160. PubMed PMID: 31584572.
4: Tremblay G, Westley T, Cappelleri JC, Arondekar B, Chan G, Bell TJ, Briggs A. Overall survival of glasdegib in combination with low-dose cytarabine, azacitidine, and decitabine among adult patients with previously untreated AML: comparative effectiveness using simulated treatment comparisons. Clinicoecon Outcomes Res. 2019 Sep 6;11:551-565. doi: 10.2147/CEOR.S203482. eCollection 2019. PubMed PMID: 31564931; PubMed Central PMCID: PMC6735653.
5: Cortes JE, Dombret H, Merchant A, Tauchi T, DiRienzo CG, Sleight B, Zhang X, Leip EP, Shaik N, Bell T, Chan G, Sekeres MA. Glasdegib plus intensive/nonintensive chemotherapy in untreated acute myeloid leukemia: BRIGHT AML 1019 Phase III trials. Future Oncol. 2019 Nov;15(31):3531-3545. doi: 10.2217/fon-2019-0373. Epub 2019 Sep 13. PubMed PMID: 31516032.
