Eltanexor (KPT-8602) | XPO1 Inhibitor

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CAS No. :	1642300-52-4
Formula :	C₁₇H₁₀F₆N₆O
M.W :	428.29
SMILES Code :	O=C(N)/C(C1=CN=CN=C1)=C/N2N=C(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)N=C2
Synonyms :	KPT-8602; ONO-7706,ATG-016
MDL No. :	MFCD30489739
InChI Key :	JFBAVWVBLRIWHM-AWNIVKPZSA-N
Pubchem ID :	86345880

GHS Pictogram:
Signal Word:	Warning
Hazard Statements:	H302-H312-H332
Precautionary Statements:	P280

NCI-N87	500 nM	10 days	Inhibited cell proliferation, disrupted spheroid formation, induced apoptosis	PMC6801932
GBM stem-like cells (2017/74, 2017/151, 2016/175, 2016/240)	1 nM to 10 µM	10 days	Evaluate the therapeutic efficacy of Eltanexor in GBM stem-like cells, IC50 values below 200 nM, significantly reducing cell viability and increasing apoptosis rates	PMC9496210
IMS-M2	50 nM	11 days	Inhibited growth of NPM1-mutated cells and induced differentiation	PMC9701620
U251 GB cells	100 nM	12 hours	Evaluate the effect of Eltanexor on XPO1 gene expression in U251 cells, showing significant upregulation of XPO1 mRNA	PMC11011525
U87 GB cells	100 nM	12 hours	Evaluate the effect of Eltanexor on XPO1 gene expression in U87 cells, showing significant upregulation of XPO1 mRNA	PMC11011525
RPMI-8402	50 nM	14 days	To test the synergistic effect of MRK-560 and KPT-8602, results showed that all NOTCH1-dependent cell lines were sensitive to KPT-8602, and the combination significantly inhibited leukemia proliferation and/or induced cell death	PMC8223323
ALL-SIL	50 nM	14 days	To test the synergistic effect of MRK-560 and KPT-8602, results showed that all NOTCH1-dependent cell lines were sensitive to KPT-8602, and the combination significantly inhibited leukemia proliferation and/or induced cell death	PMC8223323
DND-41	50 nM	14 days	To test the synergistic effect of MRK-560 and KPT-8602, results showed that all NOTCH1-dependent cell lines were sensitive to KPT-8602, and the combination significantly inhibited leukemia proliferation and/or induced cell death	PMC8223323
NALM6	1 μM	16 hours	To assess the sensitivity of SF3B1 mutant cells to XPO1 inhibition, results showed increased sensitivity of SF3B1 mutant cells to eltanexor	PMC11347370
U266-LR6	300 nM	20 hours	XPO1 inhibitors significantly increased sensitivity to MEL	PMC7718436
8226-LR5	300 nM	20 hours	XPO1 inhibitors significantly increased sensitivity to MEL	PMC7718436
U266	300 nM	20 hours	SEL or ELT combined with MEL significantly increased apoptosis compared to MEL alone	PMC7718436
8226	300 nM	20 hours	SEL or KOS-2464 increased apoptosis in a dose-dependent manner	PMC7718436
H929	300 nM	20 hours	SEL or ELT combined with MEL significantly increased apoptosis compared to MEL alone	PMC7718436
GSCs (glioblastoma stem-like cells)	10 nM	48 hours	Evaluate the effect of Eltanexor on XPO1 gene expression in GSCs, showing significant upregulation of XPO1 mRNA	PMC11011525
HEK293	0.01 μM and 0.1 μM	48 hours	Evaluate the inhibitory effect of Eltanexor on HEK293 cell proliferation, showing increased sensitivity of E571K mutant cells to KPT-330 (Selinexor) at 0.01 μM and 0.1 μM doses	PMC7809770
K562	1 μM	48 hours	To validate the sensitivity of DDX19A knockdown to XPO1 inhibition, results showed that DDX19A knockdown increased sensitivity to eltanexor	PMC11347370
Bone marrow-derived macrophages (BMMs)	0, 25, 50, 75, 100 nM	5 days	To evaluate the inhibitory effect of Eltanexor on RANKL-induced osteoclast formation. Results showed that Eltanexor inhibited osteoclast formation in a dose-dependent manner.	PMC9468713
U251	1 nM to 10 µM	5 days	Evaluate the therapeutic efficacy of Eltanexor in GBM cell lines, IC50 values below 100 nM, significantly reducing cell viability and increasing apoptosis rates	PMC9496210
U87	1 nM to 10 µM	5 days	Evaluate the therapeutic efficacy of Eltanexor in GBM cell lines, IC50 values below 100 nM, significantly reducing cell viability and increasing apoptosis rates	PMC9496210
PDX2 and PDX3	50 nM	7 to 9 days	Induced increased CD11b expression in NPM1-mutated primary AML samples	PMC9701620
SNU-16	150 nM	72 hours	Inhibited cell proliferation, induced apoptosis, and halted cell cycle progression at the G1/S phase	PMC6801932
SNU-1	150 nM	72 hours	Inhibited cell proliferation, induced apoptosis, and halted cell cycle progression at the G1/S phase	PMC6801932
Primary MF CD34+ cells	50-100 nM	72 hours	Evaluate the effect of KPT-8602 on primary MF CD34+ cell viability and apoptosis, showing selective suppression of MF cell growth and induction of apoptosis	PMC6445677
HEL-R cells	100 nM	72 hours	Evaluate the effect of KPT-8602 on JAK inhibitor-resistant HEL-R cell viability, showing IC50 ~100 nM	PMC6445677
SET-2 cells	100 nM	72 hours	Evaluate the effect of KPT-8602 on SET-2 cell viability, showing IC50 ~100 nM	PMC6445677
HEL cells	100 nM	72 hours	Evaluate the effect of KPT-8602 on HEL cell viability, showing IC50 ~100 nM	PMC6445677
OCI-AML3	50 nM	72 hours	Induced differentiation of NPM1-mutated AML cells, characterized by HOX/MEIS downregulation and increased CD11b expression	PMC9701620
NB4 cells	264 nM (GI50)	72 hours	To evaluate the growth inhibitory effect of Eltanexor on NB4 cells, the results showed a GI50 of 264 nM.	PMC7013257
U-937 cells	131 nM (GI50)	72 hours	To evaluate the growth inhibitory effect of Eltanexor on U-937 cells, the results showed a GI50 of 131 nM.	PMC7013257
MOLM-16 cells	59 nM (GI50)	72 hours	To evaluate the growth inhibitory effect of Eltanexor on MOLM-16 cells, the results showed a GI50 of 59 nM.	PMC7013257
K-562 cells	104 nM (GI50)	72 hours	To evaluate the growth inhibitory effect of Eltanexor on K-562 cells, the results showed a GI50 of 104 nM.	PMC7013257
MOLM-13 cells	32 nM (GI50)	72 hours	To evaluate the growth inhibitory effect of Eltanexor on MOLM-13 cells, the results showed a GI50 of 32 nM.	PMC7013257
MV-4-11 cells	22 nM (GI50)	72 hours	To evaluate the growth inhibitory effect of Eltanexor on MV-4-11 cells, the results showed a GI50 of 22 nM.	PMC7013257
Human foreskin fibroblasts (HFFs)	0.03762 μM (IC50)	72 hours	To evaluate the inhibitory effect of Eltanexor on HCMV replication. Results showed that Eltanexor inhibits HCMV replication in a dose-dependent manner with an IC50 of 0.03762 μM.	PMC8126617

C57BL/6J female mice	Ovariectomized (OVX) osteoporosis model	Intraperitoneal injection	0.075 mg/kg and 0.15 mg/kg	Every 2 days, continuous treatment	To evaluate the protective effect of Eltanexor on ovariectomy-induced osteoporosis. Results showed that Eltanexor significantly reduced bone loss and increased trabecular bone number.	PMC9468713
Mice	Healthy mouse brain slice culture	In vitro culture	1 µM	48 hours	Evaluate the toxicity of Eltanexor combined with chemotherapy drugs on healthy brain tissue, showing no significant cell death	PMC11011525
ICR-nude female mice	SNU-1 xenograft model	Oral	10 mg/kg	Every other day for three weeks	Significantly enhanced tumor inhibition in combination with nab-paclitaxel	PMC6801932
Mice	Sf3b1 K700E conditional knock-in mice	Oral gavage	10 mg/kg	5 days per week for two weeks	To evaluate the effect of combination therapy of eltanexor with BCL inhibitors, results showed that the combination of eltanexor and venetoclax significantly reduced Sf3b1 mutant cells	PMC11347370
NOD/SCID-γ mice	Human U266 and U266-LR6 MM tumor models	Oral gavage	10 mg/kg	Twice weekly, continuous treatment	SEL or ELT combined with MEL significantly reduced tumor growth and improved survival	PMC7718436
Balb/c mice	JAK2V617F-driven MPN model	Oral	10 mg/kg	Twice weekly for 28 days	Evaluate the effect of KPT-330 alone or in combination with ruxolitinib on the MPN model, showing combination treatment significantly reduced white blood cells, spleen GFP+ cells and spleen weight, and partially restored splenic architecture	PMC6445677
NSG mice	PDX2 and PDX3 models	Oral gavage	10 mg/kg	5 days per week for 4 weeks	Significantly reduced leukemic burden and prolonged survival	PMC9701620
Mice	Wilms tumor PDX models	Oral gavage	15 mg/kg	Five times per week for 4 weeks	Evaluate the anti-tumor activity of eltanexor in Wilms tumor PDX models, showing similar anti-tumor effects as selinexor	PMC9669237
Zebrafish	Tet2-mutant zebrafish embryos	Embryo water immersion	250 nM	From 1 dpf to 5 dpf	Evaluate the selective killing effect of Eltanexor on tet2-mutant zebrafish embryo HSPCs, results showed Eltanexor selectively killed tet2-mutant HSPCs.	PMC10121884
Mice	T-ALL patient-derived xenograft model	Oral	5 mg/kg	Once daily for 14 days	To test the in vivo synergistic effect of MRK-560 and KPT-8602, results showed that combination treatment significantly reduced leukemic burden and prolonged survival	PMC8223323
NSGS mice	MV-4-11 AML xenograft model	Oral gavage	7.5 mg/kg	5 days per week for 3 weeks	To evaluate the anti-leukemic effects of Eltanexor in the MV-4-11 AML xenograft model, the results showed that combination treatment significantly reduced leukemia burden in peripheral blood, bone marrow, and spleen.	PMC7013257

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CAS No.: 1642300-52-4

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CAS No.: 1642300-52-4

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Precautionary Statements-General

Prevention

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Physical hazards

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Preparing Stock Solutions		1mg	5mg	10mg
Preparing Stock Solutions	1 mM 5 mM 10 mM	2.33mL 0.47mL 0.23mL	11.67mL 2.33mL 1.17mL	23.35mL 4.67mL 2.33mL
Dissolving Methods	Animal experiment Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn: in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day; The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound. Protocol 1 Protocol 2

Precautionary Statements-General
Code	Phrase
P101	If medical advice is needed,have product container or label at hand.
P102	Keep out of reach of children.
P103	Read label before use
Prevention
Code	Phrase
P201	Obtain special instructions before use.
P202	Do not handle until all safety precautions have been read and understood.
P210	Keep away from heat/sparks/open flames/hot surfaces. - No smoking.
P211	Do not spray on an open flame or other ignition source.
P220	Keep/Store away from clothing/combustible materials.
P221	Take any precaution to avoid mixing with combustibles
P222	Do not allow contact with air.
P223	Keep away from any possible contact with water, because of violent reaction and possible flash fire.
P230	Keep wetted
P231	Handle under inert gas.
P232	Protect from moisture.
P233	Keep container tightly closed.
P234	Keep only in original container.
P235	Keep cool
P240	Ground/bond container and receiving equipment.
P241	Use explosion-proof electrical/ventilating/lighting/equipment.
P242	Use only non-sparking tools.
P243	Take precautionary measures against static discharge.
P244	Keep reduction valves free from grease and oil.
P250	Do not subject to grinding/shock/friction.
P251	Pressurized container: Do not pierce or burn, even after use.
P260	Do not breathe dust/fume/gas/mist/vapours/spray.
P261	Avoid breathing dust/fume/gas/mist/vapours/spray.
P262	Do not get in eyes, on skin, or on clothing.
P263	Avoid contact during pregnancy/while nursing.
P264	Wash hands thoroughly after handling.
P265	Wash skin thouroughly after handling.
P270	Do not eat, drink or smoke when using this product.
P271	Use only outdoors or in a well-ventilated area.
P272	Contaminated work clothing should not be allowed out of the workplace.
P273	Avoid release to the environment.
P280	Wear protective gloves/protective clothing/eye protection/face protection.
P281	Use personal protective equipment as required.
P282	Wear cold insulating gloves/face shield/eye protection.
P283	Wear fire/flame resistant/retardant clothing.
P284	Wear respiratory protection.
P285	In case of inadequate ventilation wear respiratory protection.
P231 + P232	Handle under inert gas. Protect from moisture.
P235 + P410	Keep cool. Protect from sunlight.
Response
Code	Phrase
P301	IF SWALLOWED:
P304	IF INHALED:
P305	IF IN EYES:
P306	IF ON CLOTHING:
P307	IF exposed:
P308	IF exposed or concerned:
P309	IF exposed or if you feel unwell:
P310	Immediately call a POISON CENTER or doctor/physician.
P311	Call a POISON CENTER or doctor/physician.
P312	Call a POISON CENTER or doctor/physician if you feel unwell.
P313	Get medical advice/attention.
P314	Get medical advice/attention if you feel unwell.
P315	Get immediate medical advice/attention.
P320
P302 + P352	IF ON SKIN: wash with plenty of soap and water.
P321
P322
P330	Rinse mouth.
P331	Do NOT induce vomiting.
P332	IF SKIN irritation occurs:
P333	If skin irritation or rash occurs:
P334	Immerse in cool water/wrap n wet bandages.
P335	Brush off loose particles from skin.
P336	Thaw frosted parts with lukewarm water. Do not rub affected area.
P337	If eye irritation persists:
P338	Remove contact lenses, if present and easy to do. Continue rinsing.
P340	Remove victim to fresh air and keep at rest in a position comfortable for breathing.
P341	If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing.
P342	If experiencing respiratory symptoms:
P350	Gently wash with plenty of soap and water.
P351	Rinse cautiously with water for several minutes.
P352	Wash with plenty of soap and water.
P353	Rinse skin with water/shower.
P360	Rinse immediately contaminated clothing and skin with plenty of water before removing clothes.
P361	Remove/Take off immediately all contaminated clothing.
P362	Take off contaminated clothing and wash before reuse.
P363	Wash contaminated clothing before reuse.
P370	In case of fire:
P371	In case of major fire and large quantities:
P372	Explosion risk in case of fire.
P373	DO NOT fight fire when fire reaches explosives.
P374	Fight fire with normal precautions from a reasonable distance.
P376	Stop leak if safe to do so. Oxidising gases (section 2.4) 1
P377	Leaking gas fire: Do not extinguish, unless leak can be stopped safely.
P378
P380	Evacuate area.
P381	Eliminate all ignition sources if safe to do so.
P390	Absorb spillage to prevent material damage.
P391	Collect spillage. Hazardous to the aquatic environment
P301 + P310	IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.
P301 + P312	IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P301 + P330 + P331	IF SWALLOWED: Rinse mouth. Do NOT induce vomiting.
P302 + P334	IF ON SKIN: Immerse in cool water/wrap in wet bandages.
P302 + P350	IF ON SKIN: Gently wash with plenty of soap and water.
P303 + P361 + P353	IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower.
P304 + P312	IF INHALED: Call a POISON CENTER or doctor/physician if you feel unwell.
P304 + P340	IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P304 + P341	IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing.
P305 + P351 + P338	IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing.
P306 + P360	IF ON CLOTHING: Rinse Immediately contaminated CLOTHING and SKIN with plenty of water before removing clothes.
P307 + P311	IF exposed: call a POISON CENTER or doctor/physician.
P308 + P313	IF exposed or concerned: Get medical advice/attention.
P309 + P311	IF exposed or if you feel unwell: call a POISON CENTER or doctor/physician.
P332 + P313	IF SKIN irritation occurs: Get medical advice/attention.
P333 + P313	IF SKIN irritation or rash occurs: Get medical advice/attention.
P335 + P334	Brush off loose particles from skin. Immerse in cool water/wrap in wet bandages.
P337 + P313	IF eye irritation persists: Get medical advice/attention.
P342 + P311	IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician.
P370 + P376	In case of fire: Stop leak if safe to Do so.
P370 + P378	In case of fire:
P370 + P380	In case of fire: Evacuate area.
P370 + P380 + P375	In case of fire: Evacuate area. Fight fire remotely due to the risk of explosion.
P371 + P380 + P375	In case of major fire and large quantities: Evacuate area. Fight fire remotely due to the risk of explosion.
Storage
Code	Phrase
P401
P402	Store in a dry place.
P403	Store in a well-ventilated place.
P404	Store in a closed container.
P405	Store locked up.
P406	Store in corrosive resistant/ container with a resistant inner liner.
P407	Maintain air gap between stacks/pallets.
P410	Protect from sunlight.
P411
P412	Do not expose to temperatures exceeding 50 oC/ 122 oF.
P413
P420	Store away from other materials.
P422
P402 + P404	Store in a dry place. Store in a closed container.
P403 + P233	Store in a well-ventilated place. Keep container tightly closed.
P403 + P235	Store in a well-ventilated place. Keep cool.
P410 + P403	Protect from sunlight. Store in a well-ventilated place.
P410 + P412	Protect from sunlight. Do not expose to temperatures exceeding 50 oC/122oF.
P411 + P235	Keep cool.
Disposal
Code	Phrase
P501	Dispose of contents/container to ...
P502	Refer to manufacturer/supplier for information on recovery/recycling

Physical hazards
Code	Phrase
H200	Unstable explosive
H201	Explosive; mass explosion hazard
H202	Explosive; severe projection hazard
H203	Explosive; fire, blast or projection hazard
H204	Fire or projection hazard
H205	May mass explode in fire
H220	Extremely flammable gas
H221	Flammable gas
H222	Extremely flammable aerosol
H223	Flammable aerosol
H224	Extremely flammable liquid and vapour
H225	Highly flammable liquid and vapour
H226	Flammable liquid and vapour
H227	Combustible liquid
H228	Flammable solid
H229	Pressurized container: may burst if heated
H230	May react explosively even in the absence of air
H231	May react explosively even in the absence of air at elevated pressure and/or temperature
H240	Heating may cause an explosion
H241	Heating may cause a fire or explosion
H242	Heating may cause a fire
H250	Catches fire spontaneously if exposed to air
H251	Self-heating; may catch fire
H252	Self-heating in large quantities; may catch fire
H260	In contact with water releases flammable gases which may ignite spontaneously
H261	In contact with water releases flammable gas
H270	May cause or intensify fire; oxidizer
H271	May cause fire or explosion; strong oxidizer
H272	May intensify fire; oxidizer
H280	Contains gas under pressure; may explode if heated
H281	Contains refrigerated gas; may cause cryogenic burns or injury
H290	May be corrosive to metals
Health hazards
Code	Phrase
H300	Fatal if swallowed
H301	Toxic if swallowed
H302	Harmful if swallowed
H303	May be harmful if swallowed