Cat. No.: HY-165606

SB-T-1214

SB-T-1214 (SBT) is a taxane. SB-T-1214 efficiently inhibits expression of stem cell-related genes (Oct4, Sox2, and c-Myc) and induces apoptosis of colon cancer spheroids with drug resistant tumorigenic CD133⁺/CD44⁺ cells. SB-T-1214 strongly represses tumor growth in Pgp+ DLD-1 human colon tumor xenografts mice model. SB-T-1214 can be used for antitumor research, especially against tumors with drug resistance, such as colon, pancreatic and renal cancers.

For research use only. We do not sell to patients.

CAS No.: 178250-23-2
Formula: C₄₅H₅₉NO₁₅
Molecular Weight:853.95

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Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (285 KB)

SB-T-1214 Chemical Structure

CAS No.: 178250-23-2

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Fluorescent Dye

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

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
1A9	IC₅₀	5 nM Compound: SB-T-1214	Cytotoxicity against human 1A9 cells by MTT assay Cytotoxicity against human 1A9 cells by MTT assay	[PMID: 25047938]
1A9/ptx-10	IC₅₀	10.8 nM Compound: SB-T-1214	Cytotoxicity against human 1A9PTX10 cells by MTT assay Cytotoxicity against human 1A9PTX10 cells by MTT assay	[PMID: 25047938]
1A9/ptx-10	IC₅₀	9 nM Compound: 19, SB-T-1214	Cytotoxicity against paclitaxel resistant human 1A9PTX10 cells expressing class 1 beta-tubulin mutant after 72 hrs Cytotoxicity against paclitaxel resistant human 1A9PTX10 cells expressing class 1 beta-tubulin mutant after 72 hrs	[PMID: 18465846]
1A9/ptx-10	IC₅₀	9 nM Compound: SB-T-1214	Cytotoxicity against paclitaxel-resistant human 1A9PTX10 cells harboring point mutation in beta-tubulin after 72 hrs Cytotoxicity against paclitaxel-resistant human 1A9PTX10 cells harboring point mutation in beta-tubulin after 72 hrs	[PMID: 19239240]
1A9/ptx-22	IC₅₀	3.94 nM Compound: 19, SB-T-1214	Cytotoxicity against paclitaxel resistant human 1A9PTX22 cells expressing class 1 beta-tubulin mutant after 72 hrs Cytotoxicity against paclitaxel resistant human 1A9PTX22 cells expressing class 1 beta-tubulin mutant after 72 hrs	[PMID: 18465846]
1A9/ptx-22	IC₅₀	3.94 nM Compound: SB-T-1214	Cytotoxicity against paclitaxel-resistant human 1A9PTX22 cells harboring point mutation in beta-tubulin after 72 hrs Cytotoxicity against paclitaxel-resistant human 1A9PTX22 cells harboring point mutation in beta-tubulin after 72 hrs	[PMID: 19239240]
1A9/ptx-22	IC₅₀	7.9 nM Compound: SB-T-1214	Cytotoxicity against human 1A9PTX22 cells by MTT assay Cytotoxicity against human 1A9PTX22 cells by MTT assay	[PMID: 25047938]
A121	IC₅₀	0.26 nM Compound: 4b	Concentration required to inhibit growth of human tumor A121 (ovarian) cell line. Concentration required to inhibit growth of human tumor A121 (ovarian) cell line.	[PMID: 8831755]
A2780	IC₅₀	0.44 nM Compound: 19, SB-T-1214	Cytotoxicity against human A2780 cells after 72 hrs Cytotoxicity against human A2780 cells after 72 hrs	[PMID: 18465846]
A2780	IC₅₀	0.44 nM Compound: SB-T-1214	Cytotoxicity against human A2780 cells after 72 hrs Cytotoxicity against human A2780 cells after 72 hrs	[PMID: 19239240]
A2780	IC₅₀	20.4 nM Compound: SB-T-1214	Resistance factor, ratio of IC50 for human A2780 cells to IC50 for paclitaxel-resistant human 1A9PTX10 cells harboring point mutation in beta-tubulin Resistance factor, ratio of IC50 for human A2780 cells to IC50 for paclitaxel-resistant human 1A9PTX10 cells harboring point mutation in beta-tubulin	[PMID: 19239240]
A2780	IC₅₀	5.2 nM Compound: SB-T-1214	Cytotoxicity against human A2780 cells by MTT assay Cytotoxicity against human A2780 cells by MTT assay	[PMID: 25047938]
A2780 ADR	IC₅₀	10.9 nM Compound: SB-T-1214	Cytotoxicity against human A2780AD cells by MTT assay Cytotoxicity against human A2780AD cells by MTT assay	[PMID: 25047938]
A549	IC₅₀	0.57 nM Compound: 4b	Concentration required to inhibit growth of human tumor A549 (NSCL) cell line. Concentration required to inhibit growth of human tumor A549 (NSCL) cell line.	[PMID: 8831755]
BXPC-3	IC₅₀	1.04 nM Compound: 19, SB-T-1214	Cytotoxicity against multidrug resistant human BxPC3 cells after 72 hrs by MTT assay Cytotoxicity against multidrug resistant human BxPC3 cells after 72 hrs by MTT assay	[PMID: 18465846]
BXPC-3	IC₅₀	1.04 nM Compound: SB-T-1214	Cytotoxicity against human BxPC3 cells expressing mrp1, mrp2, lrp genes after 72 hrs Cytotoxicity against human BxPC3 cells expressing mrp1, mrp2, lrp genes after 72 hrs	[PMID: 19239240]
CFPAC-1	IC₅₀	0.83 nM Compound: 19, SB-T-1214	Cytotoxicity against multidrug resistant human CFPAC1 cells after 72 hrs by MTT assay Cytotoxicity against multidrug resistant human CFPAC1 cells after 72 hrs by MTT assay	[PMID: 18465846]
CFPAC-1	IC₅₀	0.83 nM Compound: SB-T-1214	Cytotoxicity against human Cf-Pac-1 cells expressing mdr1, mrp1, mrp2, lrp genes after 72 hrs Cytotoxicity against human Cf-Pac-1 cells expressing mdr1, mrp1, mrp2, lrp genes after 72 hrs	[PMID: 19239240]
HCT-116	IC₅₀	0.28 nM Compound: 1; SB-T-1214	Cytotoxicity against CD133 positive human HCT116 cells Cytotoxicity against CD133 positive human HCT116 cells	[PMID: 29468872]
HeLa	IC₅₀	11.2 nM Compound: SB-T-1214	Cytotoxicity against human HeLa cells transfected with wild-type tubulin beta3 by MTT assay Cytotoxicity against human HeLa cells transfected with wild-type tubulin beta3 by MTT assay	[PMID: 25047938]
HeLa	IC₅₀	2.1 nM Compound: SB-T-1214	Cytotoxicity against human HeLa cells by MTT assay Cytotoxicity against human HeLa cells by MTT assay	[PMID: 25047938]
HEY	IC₅₀	0.58 μM Compound: SB-T-1214	Cytotoxicity against human HEY cells after 72 to 120 hrs by sulforhodamine B assay Cytotoxicity against human HEY cells after 72 to 120 hrs by sulforhodamine B assay	[PMID: 29517223]
HT-29	IC₅₀	0.36 nM Compound: 4b	Concentration required to inhibit growth of human tumor HT-29 (colon) cell line. Concentration required to inhibit growth of human tumor HT-29 (colon) cell line.	[PMID: 8831755]
L1210	IC₅₀	2.66 nM Compound: SB-T-1214	Cytotoxicity against folate receptor over-expressing mouse L1210 cells after 72 hrs by MTT assay Cytotoxicity against folate receptor over-expressing mouse L1210 cells after 72 hrs by MTT assay	[PMID: 25819334]
MCF7	IC₅₀	0.2 nM Compound: 19, SB-T-1214	Cytotoxicity against Pgp deficient human MCF7 cells after 72 hrs by sulforhodamine B test Cytotoxicity against Pgp deficient human MCF7 cells after 72 hrs by sulforhodamine B test	[PMID: 18465846]
MCF7	IC₅₀	0.2 nM Compound: 4b	Concentration required to inhibit growth of human tumor MCF-7 (breast) cell line. Concentration required to inhibit growth of human tumor MCF-7 (breast) cell line.	[PMID: 8831755]
MCF7	IC₅₀	0.2 nM Compound: SB-T-1214	Cytotoxicity against P-glycoprotein deficient wild type human MCF7 cells after 72 hrs Cytotoxicity against P-glycoprotein deficient wild type human MCF7 cells after 72 hrs	[PMID: 19239240]
MCF7	IC₅₀	0.2 nM Compound: SB-T-1214	Cytotoxicity against human MCF7 cells by MTT assay Cytotoxicity against human MCF7 cells by MTT assay	[PMID: 25047938]
MCF7	IC₅₀	2.1 nM Compound: 4b	Concentration required to inhibit growth of human tumor MFC7-R (breast) cell line. Concentration required to inhibit growth of human tumor MFC7-R (breast) cell line.	[PMID: 8831755]
MCF7	IC₅₀	80.5 nM Compound: 1; SB-T-1214	Cytotoxicity against human paclitaxel-resistant MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human paclitaxel-resistant MCF7 cells after 72 hrs by MTT assay	[PMID: 29468872]
MCF7R	IC₅₀	2.1 nM Compound: SB-T-1214	Cytotoxicity against human MCF7/R cells by MTT assay Cytotoxicity against human MCF7/R cells by MTT assay	[PMID: 25047938]
MCF7R	IC₅₀	3.9 nM Compound: SB-T-1214	Cytotoxicity against human mammary tumor cell line MCF7-R Cytotoxicity against human mammary tumor cell line MCF7-R	[PMID: 16298526]
MCF7S	IC₅₀	0.2 nM Compound: SB-T-1214	Cytotoxicity against human mammary tumor cell line MCF7-S Cytotoxicity against human mammary tumor cell line MCF7-S	[PMID: 16298526]
MIA PaCa-2	IC₅₀	0.92 nM Compound: 19, SB-T-1214	Cytotoxicity against multidrug resistant human MIAPaCa2 cells after 72 hrs by MTT assay Cytotoxicity against multidrug resistant human MIAPaCa2 cells after 72 hrs by MTT assay	[PMID: 18465846]
MIA PaCa-2	IC₅₀	0.92 nM Compound: SB-T-1214	Cytotoxicity against human MIAPaCa2 cells expressing mrp1, mrp2, lrp genes after 72 hrs Cytotoxicity against human MIAPaCa2 cells expressing mrp1, mrp2, lrp genes after 72 hrs	[PMID: 19239240]
MX1	IC₅₀	1.89 nM Compound: SB-T-1214	Cytotoxicity against folate receptor over-expressing human MX1 cells after 72 hrs by MTT assay Cytotoxicity against folate receptor over-expressing human MX1 cells after 72 hrs by MTT assay	[PMID: 25819334]
PANC-1	IC₅₀	3.68 nM Compound: 19, SB-T-1214	Cytotoxicity against multidrug resistant human PANC1 cells after 72 hrs by MTT assay Cytotoxicity against multidrug resistant human PANC1 cells after 72 hrs by MTT assay	[PMID: 18465846]
PANC-1	IC₅₀	3.68 nM Compound: SB-T-1214	Cytotoxicity against human PANC1 cells expressing mdr1, mrp1, mrp2, lrp genes after 72 hrs Cytotoxicity against human PANC1 cells expressing mdr1, mrp1, mrp2, lrp genes after 72 hrs	[PMID: 19239240]
SK-OV-3	IC₅₀	0.62 nM Compound: SB-T-1214	Cytotoxicity against human SKOV3 cells after 72 to 120 hrs by sulforhodamine B assay Cytotoxicity against human SKOV3 cells after 72 to 120 hrs by sulforhodamine B assay	[PMID: 29517223]
SK-OV-3	IC₅₀	1.44 nM Compound: SB-T-1214	Cytotoxicity against human SKOV3 cells after 72 to 120 hrs in presence of verapamil by sulforhodamine B assay Cytotoxicity against human SKOV3 cells after 72 to 120 hrs in presence of verapamil by sulforhodamine B assay	[PMID: 29517223]
WI-38	IC₅₀	4.89 nM Compound: SB-T-1214	Cytotoxicity against folate receptor deficient human WI38 cells after 72 hrs by MTT assay Cytotoxicity against folate receptor deficient human WI38 cells after 72 hrs by MTT assay	[PMID: 25819334]

In Vitro

SB-T-1214 (0.5-5000 nM, 72 h) has potent FR-specific anticancer activity with IC₅₀s of 2.82, 1.89 , 2.66 and 4.89 nM for ID8, MX-1, L1210-FR and WI-38 cells^[1].
SB-T-1214 (0.1-1 μM, 48 h) induces apoptosis in CSC-enriched colon cancer cells and spheroids with a loss of integrity of the floating spheroids and 1.5-3% secondary spheroids production in HCT116, HT29 and DLD-1 cells at 0.1 μM^[2].
SB-T-1214 (0.1 μM, 24-24 h) significantly down-regulates a majority of the stemness genes such as SOX1, ACAN, and COL1A1 and inhibits the protein expression of pluripotency markers Oct4, Sox2, and c-Myc in spheroids from CD133⁺/CD44⁺ HCT116, HT29 and DLD-1 cells ^[2].

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

Western Blot Analysis^[2]

Cell Line:

spheroids from CD133⁺/CD44⁺ HCT116 cells
Concentration:

0.1 μM
Incubation Time:

24 h
Result:

Significantly inhibited the protein expression of pluripotency markers Oct4, Sox2, and c-Myc in spheroids from CD133⁺/CD44⁺ HCT116 cells.

Apoptosis Analysis^[2]

Cell Line:

spheroids from CD133⁺/CD44⁺ HCT116 cells
Concentration:

0.1-1 μM
Incubation Time:

48 h
Result:

Induced a loss of integrity of the floating spheroids and apoptosis in more than 90% of the sphere cells.
Induced 89-96% CSC-enriched colon cancer cells apoptosis.

In Vivo

SB-T-1214 (10-40  mg/kg, i.p., i.v., q3d × 3 (day 5, 8, and 11)) strongly represses tumor growth in Pgp+ DLD-1 human colon tumor xenografts mice model with great efficacy at 20 mg/kg^[2].

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

Animal Model:

SCID mice were injected subcutaneously with Pgp+ DLD-1 cells to induce Pgp+ DLD-1 human colon tumor xenografts mice model^[1].
Dosage:

10, 20, 40 mg/kg
Administration:

i.v., q3d × 3 (day 5, 8, and 11).
Result:

Had profound antitumor activity with 100% DLD-1 tumor regression 20 mg/kg and >201 days tumor growth delay.
Induced no significant toxicity with good tolerance and only a 3-5% weight loss during the period of day 15 to day 20.
Reduced tumor volume without expression human EpCAM and CD133.

Chemical Information

CAS No. 178250-23-2
Molecular Weight 853.95
Formula C₄₅H₅₉NO₁₅
SMILES

CC(O[C@]12[C@@]3([H])[C@@H]([C@]4(C(C)(C([C@H](C([C@@]3([C@H](C[C@@]1([H])OC2)O)C)=O)OC(C5CC5)=O)=C([C@H](C4)OC([C@H](O)[C@H](/C=C(C)\C)NC(OC(C)(C)C)=O)=O)C)C)O)OC(C6=CC=CC=C6)=O)=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 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)
Handling Instructions (2659 KB)

References

[1]. Seitz JD, et al. Design, synthesis and biological evaluation of a highly-potent and cancer cell selective folate-taxoid conjugate. Bioorg Med Chem. 2015 May 1; 23(9):2187-94. [Content Brief]

[2]. Botchkina GI, et al. New-generation taxoid SB-T-1214 inhibits stem cell-related gene expression in 3D cancer spheroids induced by purified colon tumor-initiating cells. Mol Cancer. 2010 Jul 14; 9:192. [Content Brief]

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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.

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