Synonym
SKLB4771; SKLB-4771; SKLB 4771. FLT3-IN-1; FLT3-IN1; FLT3-IN 1.
IUPAC/Chemical Name
1-{5-[7-(3- Morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea
InChi Key
LKXFSTAQMOENSC-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H27N7O3S2/c1-17-3-5-18(6-4-17)28-23(33)29-24-30-31-25(37-24)36-22-20-8-7-19(15-21(20)26-16-27-22)35-12-2-9-32-10-13-34-14-11-32/h3-8,15-16H,2,9-14H2,1H3,(H2,28,29,30,33)
SMILES Code
O=C(NC1=CC=C(C)C=C1)NC2=NN=C(SC3=C4C=CC(OCCCN5CCOCC5)=CC4=NC=N3)S2
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
Biological target:
SKLB4771 is a potent and selective Flt3 inhibitor with an IC50 value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue.
In vivo activity:
Of three highly active compounds, SKLB4771 had the highest in vivo activity against antiacute myeloid leukemia (AML). In an AML MV4-11 xenograft mouse model, a once-daily dose of SKLB4771 at 100 mg/kg for 18 days led to complete tumor regression without obvious toxicity.
Reference: J Med Chem. 2012 Apr 26;55(8):3852-66. https://pubmed.ncbi.nlm.nih.gov/22452518/
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| DMSO |
33.3 |
61.99 |
|
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
537.66
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.
| 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. Yan HX, Li WW, Zhang Y, Wei XW, Fu LX, Shen GB, Yin T, Li XY, Shi HS, Wan Y, Zhang QY, Li J, Yang SY, Wei YQ. Accumulation of FLT3(+) CD11c (+) dendritic cells in psoriatic lesions and the anti-psoriatic effect of a selective FLT3 inhibitor. Immunol Res. 2014 Oct;60(1):112-26. doi: 10.1007/s12026-014-8521-4. PMID: 24895100.
2. Li WW, Wang XY, Zheng RL, Yan HX, Cao ZX, Zhong L, Wang ZR, Ji P, Yang LL, Wang LJ, Xu Y, Liu JJ, Yang J, Zhang CH, Ma S, Feng S, Sun QZ, Wei YQ, Yang SY. Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo. J Med Chem. 2012 Apr 26;55(8):3852-66. doi: 10.1021/jm300042x. Epub 2012 Apr 6. PMID: 22452518.
In vivo protocol:
1. Yan HX, Li WW, Zhang Y, Wei XW, Fu LX, Shen GB, Yin T, Li XY, Shi HS, Wan Y, Zhang QY, Li J, Yang SY, Wei YQ. Accumulation of FLT3(+) CD11c (+) dendritic cells in psoriatic lesions and the anti-psoriatic effect of a selective FLT3 inhibitor. Immunol Res. 2014 Oct;60(1):112-26. doi: 10.1007/s12026-014-8521-4. PMID: 24895100.
2. Li WW, Wang XY, Zheng RL, Yan HX, Cao ZX, Zhong L, Wang ZR, Ji P, Yang LL, Wang LJ, Xu Y, Liu JJ, Yang J, Zhang CH, Ma S, Feng S, Sun QZ, Wei YQ, Yang SY. Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo. J Med Chem. 2012 Apr 26;55(8):3852-66. doi: 10.1021/jm300042x. Epub 2012 Apr 6. PMID: 22452518.
Yan, H. X., Li, W. W., Zhang, Y., Wei, X. W., Fu, L. X., Shen, G. B., ... & Wei, Y. Q. (2014). Accumulation of FLT3+ CD11c+ dendritic cells in psoriatic lesions and the anti-psoriatic effect of a selective FLT3 inhibitor. Immunologic research, 60, 112-126.
Wang, J., Zhang, P., Zhang, J., Ma, Z., Tian, X., Liu, Y., ... & Qu, L. (2022). Atractylenolide-1 targets FLT3 to regulate PI3K/AKT/HIF1-α pathway to inhibit osteogenic differentiation of human valve interstitial cells. Frontiers in Pharmacology, 13, 899775.
