SAN50900
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MedKoo CAT#: 555980

CAS#: 2229050-90-0

Description: 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

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SAN50900
CAS# 2229050-90-0

Theoretical Analysis

MedKoo Cat#: 555980
Name: SAN50900
CAS#: 2229050-90-0
Chemical Formula: C27H38N8O
Exact Mass: 490.32
Molecular Weight: 490.660
Elemental Analysis: C, 66.09; H, 7.81; N, 22.84; O, 3.26

Price and Availability

Size Price Availability Quantity
5mg USD 650 2 Weeks
10mg USD 1000 2 Weeks
25mg USD 1700 2 Weeks
50g USD 2450 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:
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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 250.0 509.54

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.

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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.