Synonym
AZ12253801; AZ-12253801; AZ 12253801;
IUPAC/Chemical Name
6-Methyl-N-(5-methyl-1H-pyrazol-3-yl)-2-[(2S)-2-[3-(2-pyridinyl)-5-isoxazolyl]-1-pyrrolidinyl]-4-pyrimidinamine
InChi Key
KHGNDLZELXNRQC-KRWDZBQOSA-N
InChi Code
InChI=1S/C21H22N8O/c1-13-10-19(24-20-11-14(2)26-27-20)25-21(23-13)29-9-5-7-17(29)18-12-16(28-30-18)15-6-3-4-8-22-15/h3-4,6,8,10-12,17H,5,7,9H2,1-2H3,(H2,23,24,25,26,27)/t17-/m0/s1
SMILES Code
CC1=CC(NC2=NC(N3[C@H](C4=CC(C5=NC=CC=C5)=NO4)CCC3)=NC(C)=C2)=NN1
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
>3 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
2934.99.03.00
Preparing Stock Solutions
The following data is based on the
product
molecular weight
402.46
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: Lodhia KA, Gao S, Aleksic T, Esashi F, Macaulay VM. Suppression of homologous recombination sensitizes human tumor cells to IGF-1R inhibition. Int J Cancer. 2015 Jun 15;136(12):2961-6. doi: 10.1002/ijc.29327. Epub 2014 Nov 25. PubMed PMID: 25388513.
2: Gao S, Bajrami I, Verrill C, Kigozi A, Ouaret D, Aleksic T, Asher R, Han C, Allen P, Bailey D, Feller S, Kashima T, Athanasou N, Blay JY, Schmitz S, Machiels JP, Upile N, Jones TM, Thalmann G, Ashraf SQ, Wilding JL, Bodmer WF, Middleton MR, Ashworth A, Lord CJ, Macaulay VM. Dsh homolog DVL3 mediates resistance to IGFIR inhibition by regulating IGF-RAS signaling. Cancer Res. 2014 Oct 15;74(20):5866-77. doi: 10.1158/0008-5472.CAN-14-0806. Epub 2014 Aug 28. PubMed PMID: 25168481.
3: Chitnis MM, Lodhia KA, Aleksic T, Gao S, Protheroe AS, Macaulay VM. IGF-1R inhibition enhances radiosensitivity and delays double-strand break repair by both non-homologous end-joining and homologous recombination. Oncogene. 2014 Nov 6;33(45):5262-73. doi: 10.1038/onc.2013.460. Epub 2013 Nov 4. PubMed PMID: 24186206; PubMed Central PMCID: PMC3997348.
4: Vincent EE, Elder DJ, Curwen J, Kilgour E, Hers I, Tavaré JM. Targeting non-small cell lung cancer cells by dual inhibition of the insulin receptor and the insulin-like growth factor-1 receptor. PLoS One. 2013 Jun 24;8(6):e66963. doi: 10.1371/journal.pone.0066963. Print 2013. PubMed PMID: 23826179; PubMed Central PMCID: PMC3691253.
5: Shaw PH, Maughan TS, Clarke AR. Dual inhibition of epidermal growth factor and insulin-like 1 growth factor receptors reduce intestinal adenoma burden in the Apc(min/+) mouse. Br J Cancer. 2011 Aug 23;105(5):649-57. doi: 10.1038/bjc.2011.291. Epub 2011 Aug 2. PubMed PMID: 21811251; PubMed Central PMCID: PMC3188935.