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888216-25-9 (Ganetespib)

1

Identification

Ganetespib Ganetespib
Name Ganetespib
Formula C20H20N4O3
MW 364.4
CAS No. 888216-25-9
EINECS
Smiles CN1C2=CC=C(N3C(NN=C3C4=CC(C(C)C)=C(O)C=C4O)=O)C=C2C=C1
Synonyms STA-9090;STA 9090;STA9090; 3-(2,4-dihydroxy-5-isopropylphenyl)-4-(1-methyl-1H-indol-5-yl)-1H-1,2,4-triazol-5(4H)-one
InChI InChI=1S/C20H20N4O3/c1-11(2)14-9-15(18(26)10-17(14)25)19-21-22-20(27)24(19)13-4-5-16-12(8-13)6-7-23(16)3/h4-11,25-26H,1-3H3,(H,22,27)
2

Introduction

Ganetespib(STA-9090) is a unique triazolone-containing Hsp90 inhibitor with an IC50 of 4 nM in OSA 8 cells.

Background Information

A synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity ......by AOBIOUS INC
Ganetespib (STA-9090) is a potent synthetic small molecule inhibitor of Hsp90 with potential antineoplastic activity. Ganetespib (STA-9090) has shown strong activity in a broad range of preclinical solid and hematologic cancer models, including models highly resistant to treatment. ......by AbMole BioScience
Ganetespib is a potent, synthetic, small molecule inhibitor of Hsp90, a chaperone protein that is essential to the function of certain other proteins that drive the growth, proliferation, and survival of many different types of cancer. ......by AdooQ BioScience, LLC
Description ......by Apexbio Technology LLC
Ganetespib, also known as STA-9090, is a?synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor STA-9090 binds to and inhibits Hsp90, resulting in the proteasomal degradation of oncogeni ......by BOC Sciences
Ganetespib (STA-9090) is a non-Geldanamycin, selective Hsp90 inhibitor that displays antineoplastic activity. downregulates VEGFR, c-MET, HER2, IGF-IR, EGFR, and other Hsp90 client proteins involved in hepatocarcinogenesis, thereby making it an attractive therapy for hepatocellular carcinoma. ......by BioVision, Inc.,
Ganetespib is a unique non-geldanamycin heat shock protein 90 (HSP90) inhibitor, with antitumor activity. ......by MedChemexpress Co., Ltd.
Ganetespib, also known as STA-9090, is a synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor STA-9090 binds to and inhibits Hsp90, resulting in the proteasomal degradation of oncogenic client proteins, the inhibition of cell proliferation and the elevation of heat shock protein 72 (Hsp72); it may inhibit the activity of multiple kinases, such as c-Kit, EGFR, and Bcr-Abl, which as client proteins depend on functional HsP90 for maintenance. ......by MedKoo Biosciences, Inc.
Ganetespib (STA-9090) is an HSP90 inhibitor with IC50 of 4 nM in OSA 8 cells, induces apoptosis of OSA cells while normal osteoblasts are not affected; active metabolite of STA-1474. Phase 3. ......by Selleck Chemicals LLC
Ganetespib(STA-9090) is a unique triazolone-containing Hsp90 inhibitor with an IC50 of 4 nM in OSA 8 cells. ......by Target Molecule Corp.
3

Protocol(Only for Reference)

Cell Experiment

Cell lines OSA cells
Conditions 0.001-1μM; 5 days
Method A total of 1.5 × 103 OSA cells are seeded in 96-well plates in 10% serum-containing complete medium and incubated overnight to determine the 50% inhibitory concentrations. Plates are, harvested at day 5 following 0.001, 0.005, 0.01, 0.05, 0.1, 0.5 and 1 μM Ganetespib, treatment and analyzed. Fluorescence measurements are made using a plate reader with excitation at 485 nm and emission detection at 530 nm. Relative cell number is calculated as a percentage of the control wells: absorbance of sample/absorbance of DMSO treated cells × 100.
Source Selleck Chemicals LLC

Animal Experiment

Animal Models Female severe combined immune-deficient (SCID) mice
Dosage 25 mg/kg/day for 3 days
Formulation In DMSO and diluted 1:10 with 20% Cremophor RH 40
Administration Tail vein injection
Source Selleck Chemicals LLC
4

Physical and Chemical Properties

Appearance:White to off-white solid EBNumber:EB000022580

Storage condition

Storage condition:Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). Stock solution storage:0 - 4 C for short term (days to weeks), or -20 C for long term (months). 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. by MedKoo Biosciences, Inc.

Solubility

DMSO by MedChemexpress Co., Ltd.
Soluble in DMSO, not in water by MedKoo Biosciences, Inc.
(25°C) * In vitro DMSO 40 mg/mL (109.76 mM); Water<1 mg/mL (<1 mM); Ethanol<1 mg/mL (<1 mM); In vivo 1% DMSO+30% polyethylene glycol+1% Tween 8030 mg/mL by Selleck Chemicals LLC
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Mechanism and Indication

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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Ganetespib Synta Pharmaceuticals Corp Metastatic breast cancer 2012/7/31 2013/10/31 Phase 2 Clinical
Ganetespib Synta Pharmaceuticals Corp Metastatic non small cell lung cancer 2012/4/30 2015/9/30 Phase 2 Clinical
Ganetespib Dana-Farber Cancer Institute Inc Metastatic breast cancer 2012/5/31 2014/2/1 Phase 2 Clinical
Ganetespib Dana-Farber Cancer Institute Inc Stage IV melanoma 2011/9/30 2013/11/1 Phase 2 Clinical
Ganetespib Dana-Farber Cancer Institute Inc Prostate tumor 2011/4/30 2012/12/1 Phase 2 Clinical
Ganetespib - Phase 3 Clinical
Ganetespib - Phase 3
7

Safety Data of Ganetespib

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC USA
AbMole BioScience USA
AdooQ BioScience, LLC 10mg/USD240() USA
Aladdin 5mg/RMB3333() China
Apexbio Technology LLC 5mg/USD190(In stock) USA
Ark Pharm, Inc. USA
BOC Sciences
BioVision, Inc., 5mg/USD125() USA
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD84();10mg/USD120() USA
Cayman Chemical Company USA
MedChemexpress Co., Ltd. 5mg/USD84();10mg/USD120() USA
MedKoo Biosciences, Inc. 5mg/USD70() USA
Santa Cruz Biotechnology, Inc. 10mg/USD350() USA
Selleck Chemicals LLC 5mg/USD270(In stock);10mM/1mLIn DMSO/USD302(In stock);10mM(in 1mL DMSO)/USD302(in 1mL DMSO);10mg/USD370(In stock);50mg/USD1070(In stock);200mg/USD2470(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD84();10mg/USD120() China
Target Molecule Corp. 5mg/USD130();10mg/USD179();50mg/USD533() USA
10

Related Products

Other Forms of 888216-25-9

Name CAS No Formula MW

Recommended Compounds in HSP

Name CAS No Formula MW
VER-49009 558640-51-0 C19H18ClN3O4 387.82
VER-50589 747413-08-7 C19H17ClN2O5 388.8
Debio 0932 1061318-81-7 C22H30N6O2S 442.58
17-AAG (Hydrochloride) 911710-03-7 C31H44ClN3O8 622.15
NVP-HSP990 934343-74-5 C20H18FN5O2 379.39
PF-4942847 1207961-29-2 C20H17Cl2F4N7O2 534.29
Apoptozole 1054543-47-3 C33H25F6N3O3 625.5603
AT13387 912999-49-6 C24H31N3O3 409.52
XL888 1149705-71-4 C29H37N5O3 503.64
1134156-31-2
Alvespimycin 467214-20-6 C32H48N4O8 616.75
Retaspimycin (Hydrochloride) 857402-63-2 C31H46ClN3O8 624.17
Retaspimycin 857402-23-4 C31H45N3O8 587.7
Geldanamycin 30562-34-6 C29H40N2O9 560.64
PU-H71 873436-91-0 C18H21IN6O2S 512.37
SNX-2112 908112-43-6 C23H27F3N4O3 464.48
Triptolide 38748-32-2 C20H24O6 360.4
PF-04929113 908115-27-5 C25H30F3N5O4 521.53
NVP-BEP800 847559-80-2 C21H23Cl2N5O2S 480.41
BIIB021 848695-25-0 C14H15ClN6O 318.76

Recommended Compounds in Same Indication

Name CAS No Formula MW
LDK378 1032900-25-6 C28H36ClN5O3S 558.14
Pemetrexed (disodium) 150399-23-8 C20H19N5Na2O6 471.37
Volasertib 755038-65-4 C34H50N8O3 618.81
ALK inhibitor 1 761436-81-1 C23H28BrN7O3S 562.48
Olaparib 763113-22-0 C24H23FN4O3 434.46
Afatinib (dimaleate) 850140-73-7 C32H33ClFN5O11 718.08
Trametinib 871700-17-3 C26H23FIN5O4 615.39
MGCD-265 analog 875337-44-3 C26H20FN5O2S2 517.5977
Ostarine 841205-47-8 C19H14F3N3O3 389.33
AT-101 90141-22-3 C30H30O8 518.55
Bicalutamide 90357-06-5 C18H14F4N2O4S 430.37
Tivantinib 905854-02-6 C23H19N3O2 369.42
IDO5L 914471-09-3 C9H7ClFN5O2 271.6356
SB-590885 405554-55-4 C27H27N5O2 453.54
MK-0752 471905-41-6 C21H21ClF2O4S 442.9
Cyclophosphamide 50-18-0 C7H15Cl2N2O2P 261.09
Sunitinib 557795-19-4 C22H27FN4O2 398.47
Fenretinide 65646-68-6 C26H33NO2 391.55
Leuprolide (Acetate) 74381-53-6 C61H88N16O14 1269.45
Retaspimycin 857402-23-4 C31H45N3O8 587.7
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Route of Synthesis

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References

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More Information

Ganetespib

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