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MedKoo Cat#: 555980 | Name: SAN50900
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

SAN50900, also known as FLT3-IN-3, is a potent and selective FLT3 inhibitor. SAN50900 displays nanomolar activity in biochemical 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.

Chemical Structure

SAN50900
SAN50900
CAS#2229050-90-0

Theoretical Analysis

MedKoo Cat#: 555980

Name: SAN50900

CAS#: 2229050-90-0

Chemical Formula: C27H38N8O

Exact Mass: 490.3169

Molecular Weight: 490.66

Elemental Analysis: C, 66.09; H, 7.81; N, 22.84; O, 3.26

Price and Availability

Size Price Availability Quantity
5mg USD 650.00 2 Weeks
10mg USD 1,000.00 2 Weeks
25mg USD 1,700.00 2 Weeks
50g USD 2,450.00 2 Weeks
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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
More Info
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.
Product Data
Product Data
Instruction
View handling instruction
Biological target:
SAN50900 is a potent FLT3 inhibitor with IC50s of 13 and 8 nM for FLT3 WT and FLT3 D835Y, respectively.
In vitro activity:
In this study, SAN50900 displayed nanomolar activity in biochemical assays and selectively blocked proliferation of AML cell lines harboring FLT3-ITD mutations. MV4-11 cells treated with SAN50900 suppressed the phosphorylation of FLT3 and its downstream signaling pathways, with subsequent G1 cell cycle arrest and apoptosis. Reference: J Med Chem. 2018 May 10;61(9):3855-3869. https://pubmed.ncbi.nlm.nih.gov/29672049/
In vivo activity:
A single dose of SAN50900 in mice with subcutaneous MV4-11 xenografts caused sustained inhibition of FLT3 and STAT5 phosphorylation over 48 h, in contrast to the shorter effect observed after administration of the reference FLT3 inhibitor quizartinib. Reference: J Med Chem. 2018 May 10;61(9):3855-3869. https://pubmed.ncbi.nlm.nih.gov/29672049/
Solvent mg/mL mM
Solubility
DMSO 250.0 509.54
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 490.66 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.

Recalculate based on batch purity %
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:
1. 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.
In vitro protocol:
1. 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.
In vivo protocol:
1. 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.
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.