country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-144777

Copy Link Print Information

FLT3-IN-14

FLT3-IN-14 is a potent FLT3 inhibitor with IC₅₀s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No.: 2620551-45-1
화학식: C₂₅H₂₄N₆O₂S
분자량:472.56

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

FLT3-IN-14 Chemical Structure

CAS No.: 2620551-45-1

사이즈

가격

재고

수량

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

IC₅₀: 1.4 nM (FLT-ITD), 5.6 nM (FLT3-WT)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HL-60	IC₅₀	0.608 μM Compound: 9c	Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
K562	IC₅₀	1.582 μM Compound: 9c	Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
KCL-22	IC₅₀	0.709 μM Compound: 9c	Antiproliferative activity against human KCL-22 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human KCL-22 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
KG-1	IC₅₀	0.265 μM Compound: 9c	Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
KG-1a	IC₅₀	0.904 μM Compound: 9c	Antiproliferative activity against human KG-1a cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human KG-1a cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
MOLM-13	IC₅₀	0.014 μM Compound: 9c	Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
MOLT-4	IC₅₀	0.591 μM Compound: 9c	Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
MV4-11	IC₅₀	0.011 μM Compound: 9c	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
NOMO-1	IC₅₀	1.541 μM Compound: 9c	Antiproliferative activity against human NOMO-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human NOMO-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
OCI-AML2	IC₅₀	0.519 μM Compound: 9c	Antiproliferative activity against human OCI-AML2 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human OCI-AML2 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
PBL	GI₅₀	>10 μM Compound: 9c	Cytotoxicity in human PBL cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Cytotoxicity in human PBL cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 35339838]
PBL	GI₅₀	8.9 μM Compound: 9c	Cytotoxicity in phyto-hematoagglutinin induced human PBL cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Cytotoxicity in phyto-hematoagglutinin induced human PBL cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 35339838]
THP-1	IC₅₀	1.454 μM Compound: 9c	Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]

In Vitro

FLT3-IN-14 (compound 9c) (0-10 μM; 24 hours) inhibits the proliferation of tested twelve haematological cell lines with IC₅₀s of 0.011-1.582 μM^[1].
FLT3-IN-14 (0-10 μM; 72 hours) exhibits low toxicity, with GI₅₀ greater than 10 μM, in resting lymphocytes^[1].
FLT3-IN-14 (1-50 nM; 24 and 48 hours) accumulates annexin-V positive cells in a concentration and time-dependent manner^[1].
FLT3-IN-14 (25-100 nM; 24 and 48 hours) induces a significant G1 arrest in both cell lines^[1].
FLT3-IN-14 (1-50 nM; 24 hours) induces the dephosphorylation of FLT3^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:

MOLT-4 , HL-60, KG-1, KG-1a, MOLM-13, MV4-11, NOMO-1, OCI-AML2, PL-21, THP-1, K-562, KCL-22^[1]
Concentration:

0-10 μM
Incubation Time:

24 hours
Result:

Inhibited the proliferation of these twelve haematological cell lines with IC₅₀s of 0.011-1.582 μM.

Cell Cytotoxicity Assay

Cell Line:

PBL^[1]
Concentration:

0-10 μM
Incubation Time:

72 hours
Result:

Exhibited low toxicity, with GI₅₀ greater than 10 μM, in resting lymphocytes.

Apoptosis Analysis

Cell Line:

MV4-11^[1]
Concentration:

1, 10 and 50 nM
Incubation Time:

24 and 48 hours
Result:

Accumulated annexin-V positive cells in a concentration and time-dependent manner.

Cell Cycle Analysis

Cell Line:

MOLM-13 and MV-14^[1]
Concentration:

25, 50, 75 and 100 nM
Incubation Time:

24 and 48 hours
Result:

Induced a significant G1 arrest in both cell lines.

Western Blot Analysis

Cell Line:

MV-14^[1]
Concentration:

1, 10 and 50 nM
Incubation Time:

24 hours
Result:

Induced the dephosphorylation of FLT3.

In Vivo

FLT3-IN-14 (1.0 and 3.0 mg/kg; IP; daily for 28 days) significantly reduces tumor growth in a dose-dependent manner without sign of toxicity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NOD/SCID female mice (subcutaneously implanted MV4-11)^[1]
Dosage:

1.0 and 3.0 mg/kg
Administration:

IP; daily for 28 days
Result:

Significantly reduced tumor growth by 44.1% and 55.2% at 1 and 3 mg/kg, respectively.

Chemical Information

CAS No. 2620551-45-1
분자량 472.56
화학식 C₂₅H₂₄N₆O₂S
SMILES

CC(C)(C1=CC(NC(NC2=CC=C(C=C2)C3=CN4C5=C(SC4=N3)CCC6=CNC=C65)=O)=NO1)C
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Cilibrasi V, Spanò V, Bortolozzi R, et al. Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. Eur J Med Chem. 2022 [Content Brief]

Calculators

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

Minimum order quantity

100 mg

견적 받기 해외재고보유

Other size

견적 받기