TEMSIROLIMUS

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C56H87NO16
Molecular Weight	1030.2871
Optical Activity	UNSPECIFIED
Defined Stereocenters	15 / 15
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[H][C@@]12CC[C@@H](C)[C@@](O)(O1)C(=O)C(=O)N3CCCC[C@@]3([H])C(=O)O[C@@]([H])(CC(=O)[C@H](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)\C=C\C=C\C=C(C)\[C@H](C2)OC)[C@H](C)C[C@@H]4CC[C@@H](OC(=O)C(C)(CO)CO)[C@@H](C4)OC

InChI

InChIKey=CBPNZQVSJQDFBE-FUXHJELOSA-N

InChI=1S/C56H87NO16/c1-33-17-13-12-14-18-34(2)45(68-9)29-41-22-20-39(7)56(67,73-41)51(63)52(64)57-24-16-15-19-42(57)53(65)71-46(30-43(60)35(3)26-38(6)49(62)50(70-11)48(61)37(5)25-33)36(4)27-40-21-23-44(47(28-40)69-10)72-54(66)55(8,31-58)32-59/h12-14,17-18,26,33,35-37,39-42,44-47,49-50,58-59,62,67H,15-16,19-25,27-32H2,1-11H3/b14-12+,17-13+,34-18+,38-26+/t33-,35-,36-,37-,39-,40+,41+,42+,44-,45+,46+,47-,49-,50+,56-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C56H87NO16
Molecular Weight	1030.2871
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	15 / 15
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://www.drugbank.ca/drugs/DB06287
Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_PRNTLBL.pdf

Temsirolimus is an intravenous drug for the treatment of renal cell carcinoma (RCC), developed by Wyeth Pharmaceuticals and approved by the FDA in late May 2007, and was also approved by the European Medicines Agency (EMEA) on November 2007. It is a derivative of sirolimus and is sold as Torisel. Temsirolimus is an inhibitor of mTOR (mammalian target of rapamycin). Temsirolimus binds to an intracellular protein (FKBP-12), and the protein-drug complex inhibits the activity of mTOR that controls cell division. Inhibition of mTOR activity resulted in a G1 growth arrest in treated tumor cells. When mTOR was inhibited, its ability to phosphorylate p70S6k and S6 ribosomal protein, which are downstream of mTOR in the PI3 kinase/AKT pathway was blocked. In in vitro studies using renal cell carcinoma cell lines, temsirolimus inhibited the activity of mTOR and resulted in reduced levels of the hypoxia-inducible factors HIF-1 and HIF-2 alpha, and the vascular endothelial growth factor.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Serine/threonine-protein kinase mTOR 34 Target ID: CHEMBL2842 Sources: http://www.drugbank.ca/drugs/DB06287	Inhibitor 8228		1.76 µM [IC50]
CAKI-1 3 Target ID: CHEMBL614067 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27526062	Inhibitor 8228

Conditions

Condition	Modality	Targets	Highest Phase	Product
Advanced renal cell carcinoma 9 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_PRNTLBL.pdf	Primary		Approved 8360	Torisel Approved Use Treatment of advanced renal cell carcinoma (RCC) Launch Date 1.18039681E12

C_max

Value	Dose	Co-administered	Analyte	Population
585 ng/mL DRUG LABEL http://secure.healthlinks.net.au/content/pf/retriever.cfm?product=pfptorii10613	25 mg single, intravenous dose: 25 mg route of administration: Intravenous experiment type: SINGLE co-administered:		TEMSIROLIMUS blood	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
1627 ng × h/mL DRUG LABEL http://secure.healthlinks.net.au/content/pf/retriever.cfm?product=pfptorii10613	25 mg single, intravenous dose: 25 mg route of administration: Intravenous experiment type: SINGLE co-administered:		TEMSIROLIMUS blood	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
17.3 h DRUG LABEL http://secure.healthlinks.net.au/content/pf/retriever.cfm?product=pfptorii10613	25 mg single, intravenous dose: 25 mg route of administration: Intravenous experiment type: SINGLE co-administered:		TEMSIROLIMUS blood	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
11% DRUG LABEL http://secure.healthlinks.net.au/content/pf/retriever.cfm?product=pfptorii10613	25 mg single, intravenous dose: 25 mg route of administration: Intravenous experiment type: SINGLE co-administered:		TEMSIROLIMUS blood	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
150 mg/m2 1 times / week multiple, intravenous Dose: 150 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 150 mg/m2, 1 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/21690471	unhealthy, 11 years (range: 4-21 years) n = 7 Health Status: unhealthy Condition: Recurrent/Refractory Solid Tumors Age Group: 11 years (range: 4-21 years) Sex: M+F Population Size: 7 Sources: https://pubmed.ncbi.nlm.nih.gov/21690471	DLT: Anorexia... Dose limiting toxicities: Anorexia (grade 3, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/21690471
220 mg/m2 1 times / week multiple, intravenous Highest studied dose Dose: 220 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 220 mg/m2, 1 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/15136596	unhealthy, 54 years (range: 30-63 years) n = 9 Health Status: unhealthy Condition: solid tumor refractory Age Group: 54 years (range: 30-63 years) Sex: M+F Population Size: 9 Sources: https://pubmed.ncbi.nlm.nih.gov/15136596	DLT: Stomatitis, Asthenia... Other AEs: Mucositis, Mucositis... Dose limiting toxicities: Stomatitis (grade 3, 1 patient) Asthenia (grade 3, 1 patient) Other AEs: Mucositis (grade 1-2, 7 patients) Mucositis (grade 3-4, 1 patient) Nausea (grade 1-2, 5 patients) Thrombocytopenia (grade 1-2, 1 patient) Diarrhea (grade 1-2, 1 patient) Vomiting (grade 1-2, 3 patients) Hypercholesterolemia (grade 3-4, 2 patients) Hypertriglyceridemia (grade 3-4, 1 patient) Peripheral edema (grade 1-2, 2 patients) Weight loss (grade 1-2, 2 patients) Taste perversion (grade 1-2, 2 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/15136596
25 mg 1 times / week steady, intravenous Recommended Dose: 25 mg, 1 times / week Route: intravenous Route: steady Dose: 25 mg, 1 times / week Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022088lbl.pdf	unhealthy, 59 years (range 23-86) n = 208 Health Status: unhealthy Condition: renal cell carcinoma Age Group: 59 years (range 23-86) Sex: M+F Population Size: 208 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022088lbl.pdf	Other AEs: Asthenia, Asthenia... Other AEs: Asthenia (all grades, 51%) Asthenia (grade 3-4, 11%) Edema (all grades, 35%) Edema face (all grades, 35%) Peripheral edema (all grades, 35%) Edema (grade 3-4, 3%) Edema face (grade 3-4, 3%) Peripheral edema (grade 3-4, 3%) Pain (all grades, 28%) Pain (grade 3-4, 5%) Pyrexia (all grades, 24%) Pyrexia (grade 3-4, 1%) Weight loss (all grades, 19%) Weight loss (grade 3-4, 1%) Headache (all grades, 15%) Headache (grade 3-4, 1%) Chest pain (all grades, 16%) Chest pain (grade 3-4, 1%) Chills (all grades, 8%) Chills (grade 3-4, 1%) Aphthous stomatitis (all grades, 41%) Glossitis (all grades, 41%) Mouth ulceration (all grades, 41%) Mucositis (all grades, 41%) Stomatitis (all grades, 41%) Aphthous stomatitis (grade 3-4, 3%) Glossitis (grade 3-4, 3%) Mouth ulceration (grade 3-4, 3%) Mucositis (grade 3-4, 3%) Stomatitis (grade 3-4, 3%) Anorexia (all grades, 32%) Anorexia (grade 3-4, 3%) Nausea (all grades, 37%) Nausea (grade 3-4, 2%) Diarrhea (all grades, 27%) Diarrhea (grade 3-4, 1%) Abdominal pain (all grades, 21%) Abdominal pain (grade 3-4, 4%) Constipation (all grades, 20%) Vomiting (all grades, 19%) Vomiting (grade 3-4, 2%) Infection NOS (all grades, 20%) Abscess (all grades, 20%) Bronchitis (all grades, 20%) Cellulitis (all grades, 20%) Herpes simplex (all grades, 20%) Herpes zoster (all grades, 20%) Infection NOS (grade 3-4, 3%) Abscess (grade 3-4, 3%) Bronchitis (grade 3-4, 3%) Cellulitis (grade 3-4, 3%) Herpes simplex (grade 3-4, 3%) Herpes zoster (grade 3-4, 3%) Cystitis (all grades, 15%) Dysuria (all grades, 15%) Hematuria (all grades, 15%) Urinary frequency (all grades, 15%) Urinary tract infection (all grades, 15%) Cystitis (grade 3-4, 1%) Dysuria (grade 3-4, 1%) Hematuria (grade 3-4, 1%) Urinary frequency (grade 3-4, 1%) Urinary tract infection (grade 3-4, 1%) Pharyngitis (all grades, 12%) Rhinitis (all grades, 10%) Back pain (all grades, 20%) Back pain (grade 3-4, 3%) Arthralgia (all grades, 18%) Arthralgia (grade 3-4, 1%) Myalgia (all grades, 8%) Myalgia (grade 3-4, 1%) Dyspnea (all grades, 28%) Dyspnea (grade 3-4, 9%) Cough (all grades, 26%) Cough (grade 3-4, 1%) Epistaxis (all grades, 12%) Eczema (all grades, 47%) Exfoliative dermatitis (all grades, 47%) Maculopapular rash (all grades, 47%) Pruritic rash (all grades, 47%) Pustular rash (all grades, 47%) Rash NOS (all grades, 47%) Vesiculobullous rash (all grades, 47%) Epistaxis (grade 3-4, 5%) Eczema (grade 3-4, 5%) Exfoliative dermatitis (grade 3-4, 5%) Maculopapular rash (grade 3-4, 5%) Pruritic rash (grade 3-4, 5%) Pustular rash (grade 3-4, 5%) Rash NOS (grade 3-4, 5%) Vesiculobullous rash (grade 3-4, 5%) Pruritus (all grades, 19%) Pruritus (grade 3-4, 1%) Nail disorder (all grades, 14%) Dry skin (all grades, 11%) Dry skin (grade 3-4, 1%) Acne (all grades, 10%) Taste loss (all grades, 20%) Taste perversion (all grades, 20%) Insomnia (all grades, 12%) Insomnia (grade 3-4, 1%) Depression (all grades, 4%) Conjunctivitis (7%) Hypersensitivity reaction (9%) Pneumonia (8%) Upper respiratory tract infection (7%) Healing impaired (1%) Hypertension (7%) Venous thromboembolism (2%) Thrombophlebitis (1%) Hemoglobin decreased (all grades, 94%) Hemoglobin decreased (grade 3-4, 20%) Lymphocyte count decreased (all grades, 53%) Lymphocyte count decreased (grade 3-4, 16%) Neutrophil count decreased (all grades, 19%) Neutrophil count decreased (grade 3-4, 5%) Platelets decreased (all grades, 40%) Platelets decreased (grade 3-4, 1%) Leukocyte count decreased (all grades, 32%) Leukocyte count decreased (grade 3-4, 1%) Alkaline phosphatase increased (all grades, 68%) Alkaline phosphatase increased (grade 3-4, 3%) AST increased (all grades, 38%) AST increased (grade 3-4, 2%) Creatinine increased (all grades, 57%) Creatinine increased (grade 3-4, 3%) Glucose increased (all grades, 89%) Glucose increased (grade 3-4, 16%) Blood phosphorus decreased (all grades, 49%) Blood phosphorus decreased (grade 3-4, 18%) Bilirubin total increased (all grades, 8%) Bilirubin total increased (grade 3-4, 1%) Cholesterol total increased (all grades, 87%) Cholesterol total increased (grade 3-4, 2%) Triglyceride increased (all grades, 83%) Triglyceride increased (grade 3-4, 44%) Potassium decreased (all grades, 21%) Potassium decreased (grade 3-4, 5%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022088lbl.pdf
10 mg/m2 3 times / week multiple, intravenous (starting) Dose: 10 mg/m2, 3 times / week Route: intravenous Route: multiple Dose: 10 mg/m2, 3 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/28295182	unhealthy, 9 years (range: 1-21 years) n = 5 Health Status: unhealthy Condition: acute lymphoblastic leukaemia Age Group: 9 years (range: 1-21 years) Sex: M+F Population Size: 5 Sources: https://pubmed.ncbi.nlm.nih.gov/28295182	DLT: Hypertension, Mucositis... Dose limiting toxicities: Hypertension (grade 3, 1 patient) Mucositis (grade 3, 1 patient) Gamma-glutamyltransferase increased (grade 3, 1 patient) Hypertriglyceridaemia (grade 4, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/28295182
7.5 mg/m2 2 times / week multiple, intravenous Dose: 7.5 mg/m2, 2 times / week Route: intravenous Route: multiple Dose: 7.5 mg/m2, 2 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/28295182	unhealthy, 9 years (range: 1-21 years) n = 5 Health Status: unhealthy Condition: acute lymphoblastic leukaemia Age Group: 9 years (range: 1-21 years) Sex: M+F Population Size: 5 Sources: https://pubmed.ncbi.nlm.nih.gov/28295182	DLT: Hypertriglyceridemia, Gamma-glutamyltransferase increased... Dose limiting toxicities: Hypertriglyceridemia (grade 4, 2 patients) Gamma-glutamyltransferase increased (1 patient) Alkaline phosphatase increased (1 patient) Anorexia (grade 2, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/28295182
7.5 mg/m2 3 times / week multiple, intravenous Dose: 7.5 mg/m2, 3 times / week Route: intravenous Route: multiple Dose: 7.5 mg/m2, 3 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/28295182	unhealthy, 9 years (range: 1-21 years) n = 6 Health Status: unhealthy Condition: acute lymphoblastic leukaemia Age Group: 9 years (range: 1-21 years) Sex: M+F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/28295182	DLT: Sepsis, Mucositis... Dose limiting toxicities: Sepsis (grade 5, 1 patient) Mucositis (grade 5, 1 patient) Acidosis (grade 5, 1 patient) Reversible posterior leukoencephalopathy syndrome (1 patient) Perianal ulcer (grade 2, 1 patient) Gamma-glutamyltransferase increased (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/28295182
25 mg 1 times / week steady, intravenous Recommended Dose: 25 mg, 1 times / week Route: intravenous Route: steady Dose: 25 mg, 1 times / week Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_MedR.pdf Page: p.80	unhealthy n = 208 Health Status: unhealthy Population Size: 208 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_MedR.pdf Page: p.80	Disc. AE: Interstitial lung disease, Asthenia... AEs leading to discontinuation/dose reduction: Interstitial lung disease (grade 5) Asthenia (3 patients) Creatinine increased (3 patients) Anemia (2 patients) Abdominal pain (2 patients) Peripheral edema (2 patients) Cerebrovascular accident (grade 5, 1 patient) Dyspnea (1 patient) Lung infiltration (1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_MedR.pdf Page: p.80

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1709 inhibitor 1579 inducer 768	substrate 1010 inducer 383 inhibitor 1752	inhibitor 1837 substrate 1193	inhibitor 1599

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP3A4/5 273 CYP1A2 1509 CYP2C19 1463 CYP2C8 901 P-gp 1437	CYP2E1 648 CYP2C19 985 CYP1A2 1032 P-gp 1527	CYP2C8 168 CYP2C19 290

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP2C8 955	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=28 Page: 28.0	no [IC50 27 uM]
CYP1A2 1673	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=28 Page: 28.0	no
CYP2C19 1537	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=27 Page: 27.0	no
CYP2C19 1537	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=28 Page: 28.0	no
CYP2C8 955	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=27 Page: 27.0	no
CYP2C9 1803	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=27 Page: 27.0	no
CYP3A4 1909	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=27 Page: 27.0	no
CYP2C9 1803	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=28 Page: 28.0	yes [IC50 14 uM]
CYP2D6 1875	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=7 Page: 7.0	yes [IC50 2.2 uM]	no (co-administration study) Comment: To investigate the inhibition potential of temsirolimus, a drug-drug interaction study with desipramine (a CYP2D6 substrate) was completed. The statistical analysis concludes that the 90% CI for the LSGM ratios of Cmax, AUCt and AUC of desipramine were within the range of 80-125%. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=7 Page: 7.0
CYP3A4/5 330	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=28 Page: 28.0	yes [IC50 5.5 uM]
P-gp 1626	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=29 Page: 29.0	yes
CYP3A4 1909	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=7 Page: 7.0	yes	no (co-administration study) Comment: desipramine concentrations were not effected by co-administration with temsirolimus in-vivo, therefore no inhibition of CYP3A4 of expected. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=7 Page: 7.0

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A4 1709	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=7 Page: 7.0	major	yes (co-administration study) Comment: Drug-drug interaction studies indicate an 56% reduction in sirolimus exposure (AUC), and no effect on temsirolimus exposure when administered with rifampin. Coadministration of IV temsirolimus with ketoconazole did not effect the exposure of temsirolimus but increased the exposure (AUC) of sirolimus by 3.1-fold. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=7 Page: 7.0
CYP1A2 1032	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=27 Page: 27.0	no
CYP2C19 985	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=27 Page: 27.0	no
CYP2C9 1010	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=27 Page: 27.0	no
CYP2D6 1193	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=27 Page: 27.0	no
CYP2E1 648	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=27 Page: 27.0	yes
P-gp 1527	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022088s000_ClinPharmR.pdf#page=29 Page: 29.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1632	inhibitor 1613 Sources: https://www.pfizer.ca/sites/default/files/201710/TORISEL_PM_199380_21Dec2016_E.pdf#page=34 Page: 34.0

Sourcing

Vendor/Aggregator	ID	URL
AA Blocks	AA00IMI9	https://www.aablocks.com/goods/Goods/detail?id=AA00IMI9
AK Scientific, Inc. (AKSCI)	66622	http://www.aksci.com/item_detail.php?cat=66622
Aaron Chemicals	AR00INA1	http://www.aaronchem.com/162635-04-3
Achemtek	0102-018264	http://www.achemtek.com/162635-04-3
Acorn PharmaTech	ACN-035838	http://www.acornpharmatech.com/
Adooq BioScience	Temsirolimus - Torisel	http://www.adooq.com/temsirolimus-torisel.html
Alfa Chemistry	AP162635043	https://reagents.alfa-chemistry.com/product/temsirolimus-cas-162635-04-3-6047.html
Alsachim	1796	http://www.alsachim.com/product-C2628-glo.bal-view.html
Ambeed	A642622	https://www.ambeed.com/products/162635-04-3.html
Ambinter	Amb17620340	http://www.ambinter.com/reference/17620340
ApexBio Technology	A8314	http://www.apexbt.com/temsirolimus.html
Ark Pharma Scientific Limited	A-0192	http://www.arkpharmtech.com/product/32143.html
Aurora Fine Chemicals LLC	A17.906.239	http://online.aurorafinechemicals.com/info?ID=A17.906.239
Aurora Fine Chemicals LLC	K16.781.749	http://online.aurorafinechemicals.com/info?ID=K16.781.749
AvaChem Scientific	3349	http://www.avachem.com/productSearch.asp?3349
BLD Pharm	BD152558	http://www.bldpharm.com/products/162635-04-3.html
BOC Sciences	162635-04-3	https://www.bocsci.com/temsirolimus-cas-162635-04-3-item-84-60287.html
BioChemPartner	BCP25281	http://www.biochempartner.com/162635-04-3-BCP25281
BioCrick	BCC3678	http://www.biocrick.com/Temsirolimus-BCC3678.html
BioSynth	J-009958	https://www.biosynth.com/en/products/all-products/products/J-009958.html
BioSynth	J-524319	https://www.biosynth.com/en/products/all-products/products/J-524319.html
Boerchem	BC677694	http://www.boerchem.com/?product_40829.html
CSNpharm	CSN12047	https://www.csnpharm.com/products/temsirolimus.html
Chem Scene	CS-0129	http://www.chemscene.com/162635-04-3.html
ChemMol	30113706	http://www.chemmol.com/chemmol/30113706.html
ChemMol	49400137	http://www.chemmol.com/chemmol/49400137.html
ChemShuttle	109825	http://www.chemshuttle.com/catalogsearch/result/?q=162635-04-3&cat=
Chemspace	CSSB00161189690	https://chem-space.com/CSSB00161189690
Chemspace	CSSB02125554661	https://chem-space.com/CSSB02125554661
Chemspace	CSSB02125604528	https://chem-space.com/CSSB02125604528
Chemspace	CSSS02125607366	https://chem-space.com/CSSS02125607366
Clearsynth	CS-O-02422	https://www.clearsynth.com/en/CSO02422.html
DC Chemicals	DCAPI1488	http://www.dcchemicals.com/product_show-Temsirolimus.html
Excenen	EX-A957	http://www.excenen.com/searchresultlist.php?id=162635-04-3
Finetech	FT-0674847	http://www.finetechnology-ind.com/prod/detail/pub/162635-04-3.html
Glentham Life Sciences	GK7650	http://www.glentham.com/products/product/GK7650/
Hairui	HR115539	http://www.hairuichem.com/en/product/162635-04-3.html
Hello Bio	HB2252	http://www.hellobio.com/cci-779.html
Lab Network	LN01296366	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01296366
Lan Pharmatech	LAN-B70882	http://www.lanpharmatech.com/product-9?_keywords=LAN-B70882
LeadScope	LS-186555	http://www.leadscope.com/structure_search_results.php?ss_string=LS-186555
LeadScope	LS-187004	http://www.leadscope.com/structure_search_results.php?ss_string=LS-187004
LeadScope	LS-187783	http://www.leadscope.com/structure_search_results.php?ss_string=LS-187783
Matrix Scientific	146704	https://www.matrixscientific.com/146704.html
MedChem Express	HY-50910	https://www.medchemexpress.com/Temsirolimus.html
MolPort	MolPort-003-850-408	https://www.molport.com/shop/molecule-link/MolPort-003-850-408
MolPort	MolPort-042-665-740	https://www.molport.com/shop/molecule-link/MolPort-042-665-740
MolPort	MolPort-044-561-110	https://www.molport.com/shop/molecule-link/MolPort-044-561-110
MolPort	MolPort-046-701-794	https://www.molport.com/shop/molecule-link/MolPort-046-701-794
Molcore	MC529058	https://www.molcore.com/product/162635-04-3
OChem	24844	http://www.ocheminc.com/index.php?act=psearch&pid=635T043
Renno Tech	RL02091	http://www.rennotech.com/product_show.asp?id=2340
Selleck Chemicals	S1044	http://www.selleckchem.com/products/Temsirolimus.html
Sigma-Aldrich	PZ0020_SIGMA	https://www.sigmaaldrich.com/catalog/product/sigma/pz0020?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Smolecule	S548071	http://www.smolecule.com/products/s548071
Sun-shine Chemical	Temsirolimus	http://www.sun-shinechem.com/Details/Temsirolimus/1642/162635-04-3.html
TCI (Tokyo Chemical Industry)	T3574	http://www.tcichemicals.com/eshop/en/us/commodity/T3574/index.html
THE BioTek	bt-287412	https://www.thebiotek.com/product/inhibitors/bt-287412
Tocris	5264	https://www.tocris.com/products/temsirolimus_5264
Yuhao Chemical	RT18934	http://www.chemyuhao.com/162635-04-3.html
abcr GmbH	AB352317	http://www.abcr.de/shop/en/AB352317
eNovation Chemicals	D480430	https://www.enovationchem.com/ProductDetails.asp?ProductID=D480430
eNovation Chemicals	Y0973942	https://www.enovationchem.com/ProductDetails.asp?ProductID=Y0973942
iChemical	EBD30128	http://www.ichemical.com/products/162635-04-3.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs

PubMed

Title	Date	PubMed
Dual blockade of PI3K/AKT/mTOR (NVP-BEZ235) and Ras/Raf/MEK (AZD6244) pathways synergistically inhibit growth of primary endometrioid endometrial carcinoma cultures, whereas NVP-BEZ235 reduces tumor growth in the corresponding xenograft models.	2015 Jul	25933683
Targeting Survivin Inhibits Renal Cell Carcinoma Progression and Enhances the Activity of Temsirolimus.	2015 Jun	25808836
Effect of Targeting Clusterin Using OGX-011 on Antitumor Activity of Temsirolimus in a Human Renal Cell Carcinoma Model.	2017 Feb	27526062

Patents

Sample Use Guides

In Vivo Use Guide

Renal Cell Carcinoma General Dosage IV 25 mg once weekly.

Route of Administration: Intravenous

In Vitro Use Guide

Temsirolimus (10uM) inhibited the growth of Human Renal Cell Carcinoma Caki-1 growth approx. by 60%

Substance Class	Chemical Created by `admin` on `Wed Jul 05 23:17:42 UTC 2023` Edited by `admin` on `Wed Jul 05 23:17:42 UTC 2023`
Record UNII	624KN6GM2T
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

TEMSIROLIMUS

Official Name

English

TEMSIROLIMUS [VANDF]

Common Name

English

RAPAMYCIN 42-(2,2-BIS(HYDROXYMETHYL)PROPIONATE)

Common Name

English

TORISEL

Brand Name

English

TEMSIROLIMUS [JAN]

Common Name

English

Temsirolimus [WHO-DD]

Common Name

English

TEMSIROLIMUS [EMA EPAR]

Common Name

English

TEMSIROLIMUS [ORANGE BOOK]

Common Name

English

TEMSIROLIMUS [USAN]

Common Name

English

temsirolimus [INN]

Common Name

English

RAPAMYCIN, 42-(3-HYDROXY-2-(HYDROXYMETHYL)-2-METHYLPROPANOATE)

Common Name

English

CCI-779

Code

English

TEMSIROLIMUS [MI]

Common Name

English

TEMSIROLIMUS [MART.]

Common Name

English

Classification Tree Code System Code

NDF-RT

N0000175076