WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 555980
Description: SAN50900, also known as FLT3-IN-3, is a potent and selective FLT3 inhibitor. SAN50900 displays nanomolar activity in biochem. assays and selectively blocks proliferation of AML cell lines harboring FLT3-ITD mutations, whereas other transformed and normal human cells are several orders of magnitude less sensitive. SAN50900 was first reported in J Med Chem. 2018 May 10;61(9):3855-3869. (compd. 7d). RUN99995 is a potent and orally active MAT2A inhibitor with potential antineoplastic activity. This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming).
MedKoo Cat#: 555980
Chemical Formula: C27H38N8O
Exact Mass: 490.3169
Molecular Weight: 490.656
Elemental Analysis: C, 66.09; H, 7.81; N, 22.84; O, 3.26
Synonym: FLT3-IN-3; FLT3-IN3; FLT3-IN 3; SAN50900; SAN-50900; SAN 50900;
IUPAC/Chemical Name: N2-((1r,4r)-4-aminocyclohexyl)-9-cyclopentyl-N6-(4-(morpholinomethyl)phenyl)-9H-purine-2,6-diamine
InChi Key: SAEGVASGMTZGFI-AQYVVDRMSA-N
InChi Code: InChI=1S/C27H38N8O/c28-20-7-11-22(12-8-20)31-27-32-25(24-26(33-27)35(18-29-24)23-3-1-2-4-23)30-21-9-5-19(6-10-21)17-34-13-15-36-16-14-34/h5-6,9-10,18,20,22-23H,1-4,7-8,11-17,28H2,(H2,30,31,32,33)/t20-,22-
SMILES Code: N[C@H](CC1)CC[C@@H]1NC2=NC3=C(N=CN3C4CCCC4)C(NC5=CC=C(CN6CCOCC6)C=C5)=N2
Appearance: Solid powder
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: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
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
The following data is based on the product molecular weight 490.656 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|
Gucký T, Řezníčková E, Radošová Muchová T, Jorda R, Klejová Z, Malínková V, Berka K, Bazgier V, Ajani H, Lepšík M, Divoký V, Kryštof V. Discovery of N2-(4-Amino-cyclohexyl)-9-cyclopentyl- N6-(4-morpholin-4-ylmethyl-phenyl)- 9H-purine-2,6-diamine as a Potent FLT3 Kinase Inhibitor for Acute Myeloid Leukemia with FLT3 Mutations. J Med Chem. 2018 May 10;61(9):3855-3869. doi: 10.1021/acs.jmedchem.7b01529. Epub 2018 Apr 30. PMID: 29672049.
FLT3 tyrosine kinase is a potential drug target in acute myeloid leukemia (AML) because patients with FLT3-ITD mutations respond poorly to std. cytotoxic agents and there is a clear link between the disease and the oncogenic properties of FLT3. The MV4-11 cells treated with 7d suppressed the phosphorylation of FLT3 and its downstream signaling pathways, with subsequent G1 cell cycle arrest and apoptosis. Addnl., a single dose of 7d in mice with s.c. MV4-11 xenografts caused sustained inhibition of FLT3 and STAT5 phosphorylation over 48 h, in contrast to the shorter effect obsd. after administration of the ref. FLT3 inhibitor quizartinib.