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Zelavespib

(Synonyms: PU-H71)

13 Cited Publications

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Based on 13 publication(s) in Google Scholar

Zelavespib (PU-H71) is a potent Hsp90 inhibitor, with an IC₅₀ of 51 nM in MDA-MB-468 cells.

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Pureza: 99.93%
No. CAS: 873436-91-0
Fòrmula: C₁₈H₂₁IN₆O₂S
Peso molecular:512.37

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Zelavespib Chemical Structure

No. CAS: 873436-91-0

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Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (13)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
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Actividad biológica

Descripciòn

Zelavespib (PU-H71) is a potent Hsp90 inhibitor, with an IC₅₀ of 51 nM in MDA-MB-468 cells.

IC₅₀ & Target^[1]

HSP90

51 nM (IC₅₀, MDA-MB-468 cells)

Ver todos los productos específicos de isoformas HSP :

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	GI₅₀	0.513 μM Compound: PU-H71	Cytotoxicity against human 786-0 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human 786-0 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
A498	GI₅₀	0.437 μM Compound: PU-H71	Cytotoxicity against human A498 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human A498 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
A549	GI₅₀	0.087 μM Compound: PU-H71	Cytotoxicity against human A549/ATCC cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human A549/ATCC cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
ACHN	GI₅₀	0.295 μM Compound: PU-H71	Cytotoxicity against human ACHN cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human ACHN cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
BT-549	GI₅₀	1.514 μM Compound: PU-H71	Cytotoxicity against human BT549 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human BT549 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
CAKI-1	GI₅₀	0.525 μM Compound: PU-H71	Cytotoxicity against human Caki1 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human Caki1 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
CCRF-CEM	GI₅₀	0.427 μM Compound: PU-H71	Cytotoxicity against human CCRF-CEM cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human CCRF-CEM cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
COLO 205	GI₅₀	0.048 μM Compound: PU-H71	Cytotoxicity against human COLO205 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human COLO205 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
DU-145	GI₅₀	0.048 μM Compound: PU-H71	Cytotoxicity against human DU145 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human DU145 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
EKVX	GI₅₀	2.512 μM Compound: PU-H71	Cytotoxicity against human EKVX cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human EKVX cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
HCC 2998	GI₅₀	0.282 μM Compound: PU-H71	Cytotoxicity against human HCC2998 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human HCC2998 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
HCT-116	GI₅₀	0.063 μM Compound: PU-H71	Cytotoxicity against human HCT116 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human HCT116 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
HCT-15	GI₅₀	0.437 μM Compound: PU-H71	Cytotoxicity against human HCT15 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human HCT15 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
HeLa	IC₅₀	226.5 nM Compound: 5; PU-H71	Antiproliferative activity against human HeLa cells by MTT assay Antiproliferative activity against human HeLa cells by MTT assay	[PMID: 31839539]
HL-60(TB)	GI₅₀	0.063 μM Compound: PU-H71	Cytotoxicity against human HL-60(TB) cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human HL-60(TB) cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
HOP-62	GI₅₀	0.263 μM Compound: PU-H71	Cytotoxicity against human HOP62 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human HOP62 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
HOP-92	GI₅₀	0.288 μM Compound: PU-H71	Cytotoxicity against human HOP92 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human HOP92 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
Hs-578T	GI₅₀	1.288 μM Compound: PU-H71	Cytotoxicity against human Hs 578T cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human Hs 578T cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
HT-29	GI₅₀	0.038 μM Compound: PU-H71	Cytotoxicity against human HT-29 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human HT-29 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
IGROV-1	GI₅₀	0.089 μM Compound: PU-H71	Cytotoxicity against human IGROV1 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human IGROV1 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
K562	GI₅₀	0.071 μM Compound: PU-H71	Cytotoxicity against human K562 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human K562 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
KM12	GI₅₀	0.059 μM Compound: PU-H71	Cytotoxicity against human KM12 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human KM12 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
LOX IMVI	GI₅₀	0.079 μM Compound: PU-H71	Cytotoxicity against human LOXIMVI cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human LOXIMVI cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
M14	GI₅₀	0.234 μM Compound: PU-H71	Cytotoxicity against human M14 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human M14 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
Malme-3M	GI₅₀	0.123 μM Compound: PU-H71	Cytotoxicity against human MALME-3M cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human MALME-3M cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
MCF7	IC₅₀	0.043 μM Compound: 5, PU-H71	Inhibition of Hsp90 in human MCF7 cell lysates assessed as interaction with Cy3b-conjugated geldanamycin by FP assay Inhibition of Hsp90 in human MCF7 cell lysates assessed as interaction with Cy3b-conjugated geldanamycin by FP assay	[PMID: 18571929]
MCF7	IC₅₀	0.06 μM Compound: 5, PU-H71	Inhibition of Hsp90 in human MCF7 cells assessed as Her2 level after 24 hrs by Western blot Inhibition of Hsp90 in human MCF7 cells assessed as Her2 level after 24 hrs by Western blot	[PMID: 18571929]
MCF7	GI₅₀	0.046 μM Compound: PU-H71	Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
MCF7	IC₅₀	90 nM Compound: 16; PU-H71	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 cells	[PMID: 31663736]
MDA-MB-231	GI₅₀	0.479 μM Compound: PU-H71	Cytotoxicity against human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
MDA-MB-435	GI₅₀	0.091 μM Compound: PU-H71	Cytotoxicity against human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
MDA-MB-468	EC₅₀	10.2 nM Compound: 11	Inhibitory activity against Hsp90 in human breast cancer MDA-MB-468 cell line Inhibitory activity against Hsp90 in human breast cancer MDA-MB-468 cell line	[PMID: 16392823]
MDA-MB-468	IC₅₀	58 nM Compound: 11	Growth inhibition in human breast cancer MDA-MB-468 cell line using SRB Growth inhibition in human breast cancer MDA-MB-468 cell line using SRB	[PMID: 16392823]
MDA-MB-468	IC₅₀	70 nM Compound: 11	Antimitotic activity in human breast cancer MDA-MB-468 cell line Antimitotic activity in human breast cancer MDA-MB-468 cell line	[PMID: 16392823]
MDA-MB-468	GI₅₀	0.083 μM Compound: PU-H71	Growth inhibition of human MDA-MB-468 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human MDA-MB-468 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
MOLT-4	GI₅₀	0.091 μM Compound: PU-H71	Cytotoxicity against human MOLT4 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human MOLT4 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
MRC5	IC₅₀	1 μM Compound: 11	Cytotoxicity against normal lung fibroblast MRC5 cell line Cytotoxicity against normal lung fibroblast MRC5 cell line	[PMID: 16392823]
NCI/ADR-RES	GI₅₀	3.631 μM Compound: PU-H71	Cytotoxicity against human NCI-ADR-RES cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human NCI-ADR-RES cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
NCI-H226	GI₅₀	0.759 μM Compound: PU-H71	Cytotoxicity against human NCI-H226 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human NCI-H226 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
NCI-H23	GI₅₀	0.089 μM Compound: PU-H71	Cytotoxicity against human NCI-H23 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human NCI-H23 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
NCI-H322M	GI₅₀	0.17 μM Compound: PU-H71	Cytotoxicity against human NCI-H322M cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human NCI-H322M cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
NCI-H460	GI₅₀	0.058 μM Compound: PU-H71	Cytotoxicity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
NCI-H522	GI₅₀	0.059 μM Compound: PU-H71	Cytotoxicity against human NCI-H522 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human NCI-H522 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
OVCAR-3	GI₅₀	0.589 μM Compound: PU-H71	Cytotoxicity against human OVCAR3 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human OVCAR3 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
OVCAR-4	GI₅₀	33.113 μM Compound: PU-H71	Cytotoxicity against human OVCAR4 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human OVCAR4 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
OVCAR-5	GI₅₀	3.02 μM Compound: PU-H71	Cytotoxicity against human OVCAR5 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human OVCAR5 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
OVCAR-8	GI₅₀	0.155 μM Compound: PU-H71	Cytotoxicity against human OVCAR8 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human OVCAR8 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
PC-3	GI₅₀	0.132 μM Compound: PU-H71	Cytotoxicity against human PC3 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human PC3 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
PC-3	IC₅₀	363 nM Compound: 5; PU-H71	Antiproliferative activity against human PC3 cells by MTT assay Antiproliferative activity against human PC3 cells by MTT assay	[PMID: 31839539]
RPMI-8226	GI₅₀	1.514 μM Compound: PU-H71	Cytotoxicity against human RPMI8226 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human RPMI8226 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
RXF 393	GI₅₀	0.759 μM Compound: PU-H71	Cytotoxicity against human RXF393 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human RXF393 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
SF-268	GI₅₀	2.089 μM Compound: PU-H71	Cytotoxicity against human SF268 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human SF268 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
SF-295	GI₅₀	0.145 μM Compound: PU-H71	Cytotoxicity against human SF295 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human SF295 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
SF-539	GI₅₀	0.851 μM Compound: PU-H71	Cytotoxicity against human SF539 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human SF539 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
SK-BR-3	IC₅₀	50 nM Compound: 11	Growth inhibition in human breast cancer SKBr3 cell line using SRB Growth inhibition in human breast cancer SKBr3 cell line using SRB	[PMID: 16392823]
SK-BR-3	EC₅₀	50 nM Compound: 26, PU-H71	Inhibition of Hsp90 in human SKBR3 cells assessed as Her2 degradation Inhibition of Hsp90 in human SKBR3 cells assessed as Her2 degradation	[PMID: 19017562]
SK-MEL-2	GI₅₀	0.355 μM Compound: PU-H71	Cytotoxicity against human SK-MEL-2 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human SK-MEL-2 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
SK-MEL-28	GI₅₀	0.417 μM Compound: PU-H71	Cytotoxicity against human SK-MEL-28 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human SK-MEL-28 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
SK-MEL-5	GI₅₀	0.457 μM Compound: PU-H71	Cytotoxicity against human SK-MEL-5 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human SK-MEL-5 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
SK-OV-3	GI₅₀	0.045 μM Compound: PU-H71	Cytotoxicity against human SKOV3 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human SKOV3 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
SN12C	GI₅₀	0.174 μM Compound: PU-H71	Cytotoxicity against human SN12C cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human SN12C cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
SNB-19	GI₅₀	0.646 μM Compound: PU-H71	Cytotoxicity against human SNB19 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human SNB19 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
SNB-75	GI₅₀	0.724 μM Compound: PU-H71	Cytotoxicity against human SNB75 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human SNB75 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
SR	GI₅₀	0.06 μM Compound: PU-H71	Cytotoxicity against human SR cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human SR cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
SW-620	GI₅₀	0.059 μM Compound: PU-H71	Cytotoxicity against human SW620 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human SW620 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
T47D	GI₅₀	0.155 μM Compound: PU-H71	Cytotoxicity against human T47D cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human T47D cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
TK-10	GI₅₀	0.162 μM Compound: PU-H71	Cytotoxicity against human TK10 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human TK10 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
U-251	GI₅₀	0.129 μM Compound: PU-H71	Cytotoxicity against human U251 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human U251 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
UACC-257	GI₅₀	0.309 μM Compound: PU-H71	Cytotoxicity against human UACC257 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human UACC257 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
UACC-62	GI₅₀	0.372 μM Compound: PU-H71	Cytotoxicity against human UACC62 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human UACC62 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]
UO-31	GI₅₀	0.324 μM Compound: PU-H71	Cytotoxicity against human UO31 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human UO31 cells after 48 hrs by sulforhodamine B assay	[PMID: 27914802]

In Vitro

Zelavespib is a potent Hsp90 inhibitor, with an IC₅₀ of 51 nM in MDA-MB-468 cells. Zelavespib inhibits the growth of several tumor cells, such as MDA-MB-468, MDA-MB-231 and HCC-1806 cells, with IC₅₀s of 65 ± 8 nM, 140 ± 5 nM and 87 ± 3 nM, respectively, and such inhibition is associated with a G2-M block arrest. Zelavespib (10-1000 nM) induces significant apoptosis in triple-negative breast cancers (TNBCs). Zelavespib (0.5, 1 μM) also downregulates oncoproteins involved in the invasive potential of TNBCs^[1]. Zelavespib (0.5 μM) decreases and depletes the BCR signaling kinases. Zelavespib (0.25-10 μM) is cytotoxic to CLL cells but shows minimal effects on PBMC or resting B cells. In addition, Zelavespib (0-1 μM) reduces CLL viability via the induction of mitochondrial apoptosis, and antagonizes the survival signals from CLL microenvironment at 0.5 μM^[2]. Zelavespib (0.05 μM) induces apoptosis of MDA-MB-231, BT-474, and MCF7 cells, and such induction is enhanced by TNF-α. Zelavespib (0.05 μM) degradates IKKβ, and down-regulates the NF-κB transcriptional activity induced by TNF-α treatment^[3].

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

In Vivo

Zelavespib (75 mg/kg, i.p.) causes intratumor accumulation, extends down-regulation of anti-tumor driving molecules, completes and retains responses at nontoxic doses in MDA-MB-468 tumor-bearing mice. Zelavespib(75 mg/kg 3×week, i.p.) suppresses the gowth of tumors, and such an effect is associated with down-regulation of several Hsp90-regulated malignancy driving proteins^[1].

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

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 873436-91-0
Appearance Solid
Peso molecular 512.37
Fòrmula C₁₈H₂₁IN₆O₂S
Color White to off-white
SMILES

CC(C)NCCCN1C(SC2=C(C=C3OCOC3=C2)I)=NC4=C(N=CN=C14)N
Synonyms

PU-H71
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (13)

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Journal Impact Factor

Signal Transduct Target Ther

Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]

2025 Dec 15;10(1):406. PMID: 41392286

Zelavespib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Dec 15;10(1):406. [Abstract]

Inoculation of THP-1 cells into 12-well cell culture plates and treated with indicated doses of Pimitespib, IPI-504, PU-H71 (0, 15, 30, 62.5, 125, 250, 500, 1000 nM), or STA-9090 for 18 h. SAMHD1 protein levels were analyzed by western blot.

Zelavespib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Dec 15;10(1):406. [Abstract]

RT-qPCR analysis of SAMHD1 mRNA levels in THP-1 cells treated with indicated concentrations of HSP90 inhibitors (IPI-504 (125, 250, 500 nM), PU-H71, or STA-9090) for 18 h.

Zelavespib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Dec 15;10(1):406. [Abstract]

MTT assay measuring THP-1 cell viability after 18-hour treatment with PU-H71 (0, 125, 250, 500 nM).
Nat Commun

Identification of HSP90 inhibitors as a novel class of senolytics. [Abstract]

2017 Sep 4;8(1):422. PMID: 28871086
Theranostics

Inhibition of HSP90β Improves Lipid Disorders by Promoting Mature SREBPs Degradation via the Ubiquitin-proteasome System. [Abstract]

2019 Aug 12;9(20):5769-5783. PMID: 31534518
Theranostics

Evaluation of [11C]NMS-E973 as a PET tracer for in vivo visualisation of HSP90. [Abstract]

2019 Jan 1;9(2):554-572. PMID: 30809293
J Control Release

The HSP90-dependent bioorthogonal PROTAC prodrug system enables tumor-selective and enhanced protein degradation. [Abstract]

2026 May 10:393:114828. PMID: 41839264
Pharmacol Res

Destabilization of ROR1 enhances activity of Ibrutinib against chronic lymphocytic leukemia in vivo. [Abstract]

2020 Jan;151:104512. PMID: 31726100
Int J Biol Macromol

17-AAG promotes the degradation of HSP90 client METTL3 to suppress MYC RNA m6A modification and expression in colorectal cancer. [Abstract]

2025 Dec 3;337(Pt 1):149421. PMID: 41349747
Br J Pharmacol

Inhibition of heat shock protein (HSP) 90 reverses signal transducer and activator of transcription (STAT) 3-mediated muscle wasting in cancer cachexia mice. [Abstract]

2021 Nov;178(22):4485-4500. PMID: 34265073
Curr Issues Mol Biol

FLT3 and IRAK4 Inhibitor Emavusertib in Combination with BH3-Mimetics in the Treatment of Acute Myeloid Leukemia. [Abstract]

2024 Mar 29;46(4):2946-2960. PMID: 38666914
Curr Issues Mol Biol

HSP90 Inhibitor PU-H71 in Combination with BH3-Mimetics in the Treatment of Acute Myeloid Leukemia. [Abstract]

2023 Aug 23;45(9):7011-7026. PMID: 37754227
Viruses

Deep Transfer Learning Approach for Automatic Recognition of Drug Toxicity and Inhibition of SARS-CoV-2. [Abstract]

2021 Apr 2;13(4):610. PMID: 33918368
Authorea

April 10, 2021.
bioRxiv

2021 Jan 27.

Solvente y solubilidad

In Vitro:

DMSO : ≥ 100 mg/mL (195.17 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9517 mL

9.7586 mL

19.5171 mL

5 mM

0.3903 mL

1.9517 mL

3.9034 mL

10 mM

0.1952 mL

0.9759 mL

1.9517 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
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%
Tween-80 + +
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocolo

Kinase Assay^[1]

Measurements are performed in black 96-well microtiter plates. In short, cell lysates are prepared by rupturing cellular membranes by freezing at -70°C and dissolving the cellular extract in HFB [20 mM Hepes (K), pH 7.3, 50 mM KCl, 5 mM MgCl₂, 20 mM Na₂MoO₄, 0.01% Nonidet P-40] with added protease and phosphatase inhibitors (Zelavespib, etc.). Saturation curves are recorded in which fluorescently labeled geldanamycin (Cy3B-GM) (3 nM) is treated with increasing amounts of cellular lysates. The amount of lysate that results in polarization (mP) readings corresponding to 90%-99% bound ligand is chosen for the competition study. Here, each 96-well plate contains 3 nM Cy3B-GM, cellular lysate and tested Hsp90 inhibitor in a final volume of 100 μL. The plate is left for 24 h on a shaker at 4°C, and the fluorescence polarization (FP) values in mP are recorded. EC₅₀ values are determined as the competitor concentrations at which 50% of the Cy3B-GM is displaced. FP measurements are performed on an Analyst GT microplate reader^[1].

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

Cell Assay^[1]

The antiproliferative effects of select Hsp90 inhibitors is evaluated using the CellTiter-Glo Luminescent Cell Viability Assay kit. Briefly, exponentially growing MDA-MB-468, MDA-MB-231, and HCC-1806 cells are seeded into black 96-well microtiter plates and incubated in medium containing either vehicle control (DMSO) or Zelavespib for the indicated time at 37°C. Plates containing 3 replicate wells per assay condition are seeded at a density of 8 × 10³ cells for each cell line in 100 μL medium. After exposure of cells to the Hsp90 inhibitors, plates are equilibrated to room temperature (20-25°C) for approximately 30 min, and 100 μL CellTiter-Glo reagent are added to each well. Plates are mixed for 2 min on an orbital shaker and then incubated for 15 min to 2 h at room temperature. The luminescence signal in each well is measured in an Analyst GT microplate reader. The percentage cell growth inhibition is calculated by comparing luminescence readings obtained from treated versus control cells, accounting for initial cell population (time 0). The IC₅₀ is calculated as the drug concentration that inhibits cell growth by 50%^[1].

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

Animal Administration^[1]

Mice^[1]
Mice bearing MDA-MB-468 tumors reaching a volume of 100-150 mm³ are treated i.p. using different doses and schedules: Group 01 (n = 8) PBS; group 02 (n = 8) Zelavespib at 50 mg/kg on alternate days; group 03 (n = 8) Zelavespib at 50 mg/kg 5xqd; group 04 (n = 8) Zelavespib at 75 mg/kg 3 week; group 05 (n = 8) Zelavespib at 75 mg/kg on alternate days. Mice bearing HCC-1806 or MDA-MB-231 xenografted tumors receive Zelavespib at 75 mg/kg on alternate days. Tumor volume is determined by measurement with Vernier calipers, and tumor volume is calculated as the product of its length × width² × 0.4. Tumor volume is expressed on indicated days as the median tumor volume ± SD indicated for groups of mice^[1].

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (285 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Caldas-Lopes E, et al. Hsp90 inhibitor PU-H71, a multimodal inhibitor of malignancy, induces complete responses in triple-negative breast cancer models. Proc Natl Acad Sci U S A. 2009 May 19;106(20):8368-73. [Content Brief]

[2]. Guo A, et al. HSP90 stabilizes B-cell receptor kinases in a multi-client interactome: PU-H71 induces CLL apoptosis in a cytoprotective microenvironment. Oncogene. 2017 Jun 15;36(24):3441-3449. [Content Brief]

[3]. Qu Z, et al. PU-H71 effectively induces degradation of IκB kinase β in the presence of TNF-α. Mol Cell Biochem. 2014 Jan;386(1-2):135-42. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9517 mL	9.7586 mL	19.5171 mL	48.7929 mL
	5 mM	0.3903 mL	1.9517 mL	3.9034 mL	9.7586 mL
	10 mM	0.1952 mL	0.9759 mL	1.9517 mL	4.8793 mL
	15 mM	0.1301 mL	0.6506 mL	1.3011 mL	3.2529 mL
	20 mM	0.0976 mL	0.4879 mL	0.9759 mL	2.4396 mL
	25 mM	0.0781 mL	0.3903 mL	0.7807 mL	1.9517 mL
	30 mM	0.0651 mL	0.3253 mL	0.6506 mL	1.6264 mL
	40 mM	0.0488 mL	0.2440 mL	0.4879 mL	1.2198 mL
	50 mM	0.0390 mL	0.1952 mL	0.3903 mL	0.9759 mL
	60 mM	0.0325 mL	0.1626 mL	0.3253 mL	0.8132 mL
	80 mM	0.0244 mL	0.1220 mL	0.2440 mL	0.6099 mL
	100 mM	0.0195 mL	0.0976 mL	0.1952 mL	0.4879 mL

Keywords

Zelavespib

13 Cited Publications

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Zelavespib

Cell Cycle/DNA Damage Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Endoplasmic Reticulum Stress Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Rare Diseases Drug Library

Anti-Prostate Cancer Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Extracellular Vesicles (EVs) Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Zelavespib

Ver todos los productos específicos de isoformas HSP

Actividad biológica

Chemical Information

Publications (13)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Zelavespib

Cell Cycle/DNA Damage Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Endoplasmic Reticulum Stress Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Rare Diseases Drug Library

Anti-Prostate Cancer Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Extracellular Vesicles (EVs) Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Zelavespib

Ver todos los productos específicos de isoformas HSP

Actividad biológica

Chemical Information

Publications (13)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Zelavespib Related Classifications

HY-11038 Related Classifications