Synonym
HM43239; HM-43239; HM 43239; Tuspetinib;
IUPAC/Chemical Name
rel-5-Chloro-N-[3-cyclopropyl-5-[[(3R,5S)-3,5-dimethyl-1-piperazinyl]methyl]phenyl]-4-(6-methyl-1H-indol-3-yl)-2-pyrimidinamine
InChi Key
FZLSDZZNPXXBBB-KDURUIRLSA-N
InChi Code
InChI=1S/C29H33ClN6/c1-17-4-7-24-25(12-31-27(24)8-17)28-26(30)13-32-29(35-28)34-23-10-20(9-22(11-23)21-5-6-21)16-36-14-18(2)33-19(3)15-36/h4,7-13,18-19,21,31,33H,5-6,14-16H2,1-3H3,(H,32,34,35)/t18-,19+
SMILES Code
CC1=CC2=C(C=C1)C(C3=NC(NC4=CC(CN5C[C@@H](C)N[C@@H](C)C5)=CC(C6CC6)=C4)=NC=C3Cl)=CN2
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
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
Biological target:
HM43239 is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively.
In vitro activity:
HM43239 potently inhibited the growth of AML cell lines harboring FLT3 ITD mutation, such as MV4-11 (IC50: 1.3 nM), MOLM-13 (5.1 nM) and MOLM-14 (2.9 nM). Furthermore, HM43239 effectively inhibited the phosphorylation levels of FLT3 and of downstream kinases related with cell proliferation.
Reference: Cancer Res. 2018 July 1;78(13_Supplement):804. https://doi.org/10.1158/1538-7445.AM2018-804
In vivo activity:
Furthermore, the combination treatment of HM43239 with various reagents (e.g., IAP inhibitor, chemotherapy, etc) demonstrated synergistic efficacy in mouse models, xenografted with both MV-4-11 and MOLM-13 cell lines without any significant toxicity.
Reference: Cancer Res. 2019 July 1;79(13_Supplement):1293. https://doi.org/10.1158/1538-7445.AM2019-1293
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| DMSO |
125.0 |
249.47 |
|
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
501.08
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. Kim J, Bae I, Choi J, Kim M, Byun J, Moon M, Lee E, Kim Y, Kang H, Kim E, Jung S, Ahn Y, Kim Y, Suh K. Abstract 1293: HM43239, a novel FLT3 inhibitor in overcoming resistance for acute myeloid leukemia. Cancer Res. 2019 July 1;79(13_Supplement):1293. doi: 10.1158/1538-7445.AM2019-1293.
2. Lee M, Young E, Moon M, Byun J, Yu H, Kang S, Lee J, Lee K, Kim E, Lee H, Kim Y, Ahn Y, Suh K, Kim S. Abstract 804: Antitumor activity of the potent and novel FLT3 inhibitor HM43239 in acute myeloid leukemia. Cancer Res. 2018 July 1;78(13_Supplement):804. doi: 10.1158/1538-7445.AM2018-804.
In vitro protocol:
1. Kim J, Bae I, Choi J, Kim M, Byun J, Moon M, Lee E, Kim Y, Kang H, Kim E, Jung S, Ahn Y, Kim Y, Suh K. Abstract 1293: HM43239, a novel FLT3 inhibitor in overcoming resistance for acute myeloid leukemia. Cancer Res. 2019 July 1;79(13_Supplement):1293. doi: 10.1158/1538-7445.AM2019-1293.
2. Lee M, Young E, Moon M, Byun J, Yu H, Kang S, Lee J, Lee K, Kim E, Lee H, Kim Y, Ahn Y, Suh K, Kim S. Abstract 804: Antitumor activity of the potent and novel FLT3 inhibitor HM43239 in acute myeloid leukemia. Cancer Res. 2018 July 1;78(13_Supplement):804. doi: 10.1158/1538-7445.AM2018-804.
In vivo protocol:
1. Kim J, Bae I, Choi J, Kim M, Byun J, Moon M, Lee E, Kim Y, Kang H, Kim E, Jung S, Ahn Y, Kim Y, Suh K. Abstract 1293: HM43239, a novel FLT3 inhibitor in overcoming resistance for acute myeloid leukemia. Cancer Res. 2019 July 1;79(13_Supplement):1293. doi: 10.1158/1538-7445.AM2019-1293.
2. Lee M, Young E, Moon M, Byun J, Yu H, Kang S, Lee J, Lee K, Kim E, Lee H, Kim Y, Ahn Y, Suh K, Kim S. Abstract 804: Antitumor activity of the potent and novel FLT3 inhibitor HM43239 in acute myeloid leukemia. Cancer Res. 2018 July 1;78(13_Supplement):804. doi: 10.1158/1538-7445.AM2018-804.
1. Kim J, Bae I, Choi J, Kim M, Byun J, Moon M, Lee E, Kim Y, Kang H, Kim E, Jung S, Ahn Y, Kim Y, Suh K. Abstract 1293: HM43239, a novel FLT3 inhibitor in overcoming resistance for acute myeloid leukemia. Cancer Res. 2019 July 1;79(13_Supplement):1293. doi: 10.1158/1538-7445.AM2019-1293.
2. Lee M, Young E, Moon M, Byun J, Yu H, Kang S, Lee J, Lee K, Kim E, Lee H, Kim Y, Ahn Y, Suh K, Kim S. Abstract 804: Antitumor activity of the potent and novel FLT3 inhibitor HM43239 in acute myeloid leukemia. Cancer Res. 2018 July 1;78(13_Supplement):804. doi: 10.1158/1538-7445.AM2018-804.
