Cat. No.: HY-111268

FI-700

FI-700 is an orally active FLT3 inhibitor with an IC₅₀ of 20 nM. FI-700 induces G1 phase cell cycle arrest by inhibiting autophosphorylation of mutant FLT3 and the downstream STAT5/MAPK pathway. FI-700 triggers the mitochondrial apoptosis pathway by downregulating anti-apoptotic proteins Mcl-1 and Bcl-XL, altering the conformation of Bax, and activating caspase-3. FI-700 can be used in research related to acute myeloid leukemia.

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CAS No.: 866883-79-6
화학식: C₂₁H₂₉N₉O
분자량:423.51

보관:

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

FI-700 Chemical Structure

CAS No.: 866883-79-6

Amount: USD 0.00

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Use of MCE Products

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^[1]

STAT5

Mcl-1

Caspase-3

Bcl-xL

Bax

All STAT Isoforms :

All Bcl-2 Family Isoforms :

All Caspase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MV4-11	IC50	0.014 μM	Antiproliferative activity against human leukemia MV4;11 (FLT3/ITD) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter96 Proliferation Assay. Antiproliferative activity against human leukemia MV4;11 (FLT3/ITD) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter96 Proliferation Assay.	17671144
MOLM-13	IC50	0.016 μM	Antiproliferative activity against human leukemia MOLM13 (FLT3/ITD) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter96 Proliferation Assay. Antiproliferative activity against human leukemia MOLM13 (FLT3/ITD) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter96 Proliferation Assay.	17671144
Kasumi 1	IC50	0.18 μM	Antiproliferative activity against human leukemia Kasumi-1 (c-KIT mutation) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter96 Proliferation Assay. Antiproliferative activity against human leukemia Kasumi-1 (c-KIT mutation) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter96 Proliferation Assay.	17671144
THP-1	IC50	3.1 μM	Antiproliferative activity against human leukemia THP1 (Wt-FLT3) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter96 Proliferation Assay. Antiproliferative activity against human leukemia THP1 (Wt-FLT3) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter96 Proliferation Assay.	17671144
HL-60	IC50	6.8 μM	Antiproliferative activity against human leukemia HL60 (no FLT3) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter96 Proliferation Assay. Antiproliferative activity against human leukemia HL60 (no FLT3) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter96 Proliferation Assay.	17671144
K562	IC50	5.2 μmol/L	Antiproliferative activity against human leukemia K562 (BCR/ABL) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter96 Proliferation Assay. Antiproliferative activity against human leukemia K562 (BCR/ABL) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter96 Proliferation Assay.	17671144
MEG-01	IC50	6.1 μM	Antiproliferative activity against human leukemia MegO1 (BCR/ABL) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter96 Proliferation Assay. Antiproliferative activity against human leukemia MegO1 (BCR/ABL) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter96 Proliferation Assay.	17671144

In Vitro

FI-700 (0.01-0.1 μM; 72 h) selectively inhibits the growth of mutant FLT3 cells in human leukemia cell lines (MV4;11, MOLM-13, THP1, Kasumi-1, K562)^[1].
FI-700 (0.03-1.0 μM; 6 h) inhibits constitutive phosphorylation of FLT3, STAT5 and MAPK in MOLM-13 cells^[1].
FI-700 (100 nM; 48 h) selectively reduces the growth of primary human AML cells harboring FLT3/ITD or FLT3/D835Y mutations^[1].
FI-700 (0.01-0.3 μM; 24 h) induces G1-phase cell cycle arrest and increases the population of sub-G1 apoptotic cells in MOLM-13 cells^[1].
FI-700 (200-800 nM; 24-72 h) induces apoptosis, reduces Mcl-1 and Bcl-XL expression, induces Bax conformational changes, and activates caspase-3 in MOLM-13 cells^[2].
FI-700 potently inhibits the activity of recombinant human FLT3 kinase with an IC₅₀ of 20 nM, and exhibits relative selectivity against other tyrosine kinases as well as serine/threonine kinases^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

MV4;11, MOLM-13, THP1, Kasumi-1, HL60, K562, MegO1, and 32D transfectants
Concentration:

0.01, 0.03, 0.05, 0.1 μM
Incubation Time:

72 h
Result:

Specifically inhibited the growth of leukemia cell lines carrying FLT3/ITD or FLT3/D835Y mutations, while showing lower sensitivity against cell lines expressing wild-type FLT3 or lacking FLT3.

Western Blot Analysis^[1]

Cell Line:

MOLM-13 cells
Concentration:

0.03, 0.1, 0.3, 1.0 μM
Incubation Time:

6 h
Result:

Dose-dependently inhibited the constitutive autophosphorylation of the target kinase, and concurrently down-regulated the phosphorylation levels of downstream STAT5 and MAPK signals.

Cell Cycle Analysis^[1]

Cell Line:

MOLM-13 cells
Concentration:

0.010, 0.030, 0.100, 0.300 μM
Incubation Time:

24 h
Result:

Led to an increase in the proportion of cells in the G1 phase and a reciprocal reduction in the S-G2 phase, significantly inducing the appearance of sub-G1 apoptotic cell populations at higher concentrations.

Cell Proliferation Assay^[1]

Cell Line:

Primary human AML cells
Concentration:

100 nM
Incubation Time:

48 h
Result:

Significantly reduced the number of primary cells carrying mutations, but did not affect the growth of wild-type cells.

Apoptosis Analysis^[2]

Cell Line:

MOLM-13 cells
Concentration:

200, 400, 800 nM
Incubation Time:

72 h
Result:

Significantly induced apoptosis in leukemia cells, although this apoptosis-inducing effect was partially attenuated in a co-culture system with mesenchymal stromal cells (MSCs).

Apoptosis Analysis^[2]

Cell Line:

MOLM-13 cells
Concentration:

800 nM
Incubation Time:

24 h
Result:

Led to decreased expression levels of anti-apoptotic proteins Mcl-1 and Bcl-XL, and triggered Bax conformational activation and caspase-3 cleavage activation.

In Vivo

FI-700 (100-200 mg/kg; p.o.; twice daily for 5 consecutive days; observation for 10 days) induces tumor regression in a subcutaneous MOLM-13 tumor xenograft mouse model^[1].
FI-700 (200 mg/kg; p.o.; twice daily for 5 consecutive days; survival monitored up to day 60) significantly prolongs the survival of mice in the intravenous MOLM-13 xenograft mouse model^[1].
FI-700 (200 mg/kg; p.o.; twice daily; for 4 consecutive days; sacrificed on day 13) exerts effects of eliminating leukemia cells in peripheral blood and bone marrow without inducing severe myelosuppression in a syngeneic transplanted C3H/Hej mouse model^[1].

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

Animal Model:

SCID (Fox Chase C.B-17/Icr-scidJcl, male, 5 weeks old, s.c. inoculation of MOLM-13 FLT3/ITD-positive leukemia cells, prior i.p. anti-asialo-GM1 antibody treatment)^[1]
Dosage:

100 mg/kg; 200 mg/kg
Administration:

p.o.; b.i.d.; 5 days; for 5 days
Result:

Significantly induced the regression of subcutaneous tumors in a dose-dependent manner.
Caused no significant body weight loss or mortality during the entire treatment course.

Animal Model:

SCID (Fox Chase C.B-17/Icr-scidJcl, male, 5 weeks old, i.v. inoculation of MOLM-13 FLT3/ITD-positive leukemia cells, prior i.p. anti-asialo-GM1 antibody treatment)^[1]
Dosage:

200 mg/kg
Administration:

p.o.; b.i.d.; 5 days
Result:

Significantly prolonged the survival time of the leukemia-bearing mice compared to the conventional chemotherapeutic drug Ara-C treatment.

Animal Model:

C3H/Hej (i.v. inoculation of FLT3/ITD-GFP-32D leukemia cells)^[1]
Dosage:

200 mg/kg
Administration:

p.o.; b.i.d.; 4 days
Result:

Significantly repressed the expansion of leukemia cells in the peripheral blood and bone marrow.
Resulted in significantly less bone marrow suppression (total bone marrow cell counts remained normal) and lighter spleen weight compared to standard chemotherapy (Ara-C).

Chemical Information

CAS No. 866883-79-6
분자량 423.51
화학식 C₂₁H₂₉N₉O
SMILES

CCCNC1=NC(NCCC2=CC=NC=C2)=NC=C1C3=NN=C(CN4CCNCC4)O3
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

Handling Instructions (2659 KB)

References

[1]. Kiyoi H, et al. A novel FLT3 inhibitor FI-700 selectively suppresses the growth of leukemia cells with FLT3 mutations. Clinical cancer research : an official journal of the American Association for Cancer Research. 2007 Aug 01;13(15 Pt 1):4575-82.

[2]. Kojima K, et al. p53 activation of mesenchymal stromal cells partially abrogates microenvironment-mediated resistance to FLT3 inhibition in AML through HIF-1α-mediated down-regulation of CXCL12. Blood. 2011 Oct 20;118(16):4431-9.

Calculators

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

Mass Mass

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Molecular Weight Molecular Weight

농도 희석 계산기

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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.

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FI-700

All STAT Isoforms

All Bcl-2 Family Isoforms

All Caspase Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

FI-700 Related Classifications

HY-111268 Related Classifications

Bioz